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Journal articles on the topic 'Internalization inhibitors'

Author: Grafiati

Published: 19 July 2023

Last updated: 31 July 2025

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1

DiCello, Jesse J., Pradeep Rajasekhar, Emily M. Eriksson та ін. "Clathrin and GRK2/3 inhibitors block δ-opioid receptor internalization in myenteric neurons and inhibit neuromuscular transmission in the mouse colon". American Journal of Physiology-Gastrointestinal and Liver Physiology 317, № 2 (2019): G79—G89. http://dx.doi.org/10.1152/ajpgi.00085.2019.

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Endocytosis is a major mechanism through which cellular signaling by G protein-coupled receptors (GPCRs) is terminated. However, recent studies demonstrate that GPCRs are internalized in an active state and continue to signal from within endosomes, resulting in effects on cellular function that are distinct to those arising at the cell surface. Endocytosis inhibitors are commonly used to define the importance of GPCR internalization for physiological and pathophysiological processes. Here, we provide the first detailed examination of the effects of these inhibitors on neurogenic contractions o

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Bigby, M., P. Wang, J. F. Fierro, and M. S. Sy. "Phorbol myristate acetate-induced down-modulation of CD4 is dependent on calmodulin and intracellular calcium." Journal of Immunology 144, no. 8 (1990): 3111–16. http://dx.doi.org/10.4049/jimmunol.144.8.3111.

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Abstract PMA causes rapid down-modulation of CD4 molecules on murine immature thymocytes, human PBL, and CD4-positive human tumor cell lines, but not on murine peripheral lymphocytes. The mechanisms of phorbol ester-induced down modulation of CD4 molecules, however, have not been elucidated. To determine how PMA down-modulates CD4 expression by T lymphocytes, we studied the ability of inhibitors of protein kinase C, calmodulin, actin, and tubulin to block PMA-induced modulation of CD4 in several murine and human cell types. We also tested the ability of intracellular and extracellular calcium

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van Kerkhof, P., and G. J. Strous. "The ubiquitin-proteasome pathway regulates lysosomal degradation of the growth hormone receptor and its ligand." Biochemical Society Transactions 29, no. 4 (2001): 488–93. http://dx.doi.org/10.1042/bst0290488.

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The growth hormone (GH) receptor (GHR) is a mammalian plasma membrane protein whose internalization is mediated by the ubiquitin-proteasome pathway. GH internalization and degradation are inhibited when cells are treated with proteasome inhibitors. Here we show that a GHR truncated at residue 369 can enter the cells in the presence of a proteasome inhibitor, but that the subsequent lysosomal degradation of GH is blocked. Lysosomal inhibitors prolong the half-life of both receptor and ligand. Experiments with antibodies against different receptor tail sections show that degradation of the GHR c

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Luton, F., M. Buferne, J. Davoust, A. M. Schmitt-Verhulst, and C. Boyer. "Evidence for protein tyrosine kinase involvement in ligand-induced TCR/CD3 internalization and surface redistribution." Journal of Immunology 153, no. 1 (1994): 63–72. http://dx.doi.org/10.4049/jimmunol.153.1.63.

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Abstract Triggering of the TCR/CD3 complex can lead to its internalization and modulation from the cell surface. In the present study, we address the question of the dependence of internalization on protein tyrosine kinase (PTK) activation. With use of an activating anti-clonotypic (anti-Ti) mAb on a CTL clone, we have shown that the PTK inhibitors genistein and tyrphostin 25 delayed anti-Ti-induced internalization, but did not affect fluid phase protein uptake or transferrin receptor cycling. Confocal microscopy with use of fluorescent anti-Ti mAb revealed that the inhibition of TCR internali

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Chen, Yang, Shan Wang, Xinan Lu, Haoran Zhang, Yan Fu, and Yongzhang Luo. "Cholesterol sequestration by nystatin enhances the uptake and activity of endostatin in endothelium via regulating distinct endocytic pathways." Blood 117, no. 23 (2011): 6392–403. http://dx.doi.org/10.1182/blood-2010-12-322867.

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Abstract Specific internalization of endostatin into endothelial cells has been proved to be important for its biologic functions. However, the mechanism of endostatin internalization still remains elusive. In this study, we report for the first time that both caveolae/lipid rafts and clathrin-coated pits are involved in endostatin internalization. Inhibition of either the caveolae pathway or the clathrin pathway with the use of chemical inhibitors, small interfering RNAs, or dominant-negative mutants alters endostatin internalization in vitro. Intriguingly, cholesterol sequestration by nystat

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Lazari, Maria de Fatima M., Xuebo Liu, Kazuto Nakamura, Jeffrey L. Benovic, and Mario Ascoli. "Role of G Protein-Coupled Receptor Kinases on the Agonist-Induced Phosphorylation and Internalization of the Follitropin Receptor." Molecular Endocrinology 13, no. 6 (1999): 866–78. http://dx.doi.org/10.1210/mend.13.6.0289.

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Abstract The experiments presented herein were designed to identify members of the G protein-coupled receptor kinase (GRK) family that participate in the agonist-induced phosphorylation and internalization of the rat FSH receptor (rFSHR). Western blots of human kidney 293 cells (the cell line used in transfection experiments) and MSC-1 cells (a cell line derived from Sertoli cells that displays many of the differentiated functions of their normal counterparts) reveal the presence of GRK2 and GRK6 in both cell lines as well as GRK4 in MSC-1 cells. Cotransfection of 293 cells with the rFSHR and

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7

Almeida, Raul A., John R. Dunlap, and Stephen P. Oliver. "Binding of Host Factors Influences Internalization and Intracellular Trafficking ofStreptococcus uberisin Bovine Mammary Epithelial Cells." Veterinary Medicine International 2010 (2010): 1–8. http://dx.doi.org/10.4061/2010/319192.

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We showed that internalization ofStreptococcus uberisinto bovine mammary epithelial cells occurred through receptor- (RME) and caveolae-mediated endocytosis (CME). We reported also that treatment ofS. uberiswith host proteins including lactoferrin (LF) enhanced its internalization into host cells. Since the underlying mechanism(s) involved in such enhancement was unknown we investigated if preincubation ofS. uberiswith host proteins drives internalization of this pathogen into host cells through CME. Thus, experiments involving coculture of collagen-, fibronectin-, and LF-pretreatedS. uberiswi

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Van Hamme, Evelien, Hannah L. Dewerchin, Els Cornelissen, Bruno Verhasselt, and Hans J. Nauwynck. "Clathrin- and caveolae-independent entry of feline infectious peritonitis virus in monocytes depends on dynamin." Journal of General Virology 89, no. 9 (2008): 2147–56. http://dx.doi.org/10.1099/vir.0.2008/001602-0.

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Feline infectious peritonitis virus (FIPV), a coronavirus that causes a lethal chronic disease in cats, enters feline monocytes via endocytosis. In this study, the pathway of internalization is characterized by evaluating the effect of chemical inhibitors and/or expression of dominant-negative (DN) proteins on the percentage of internalized virions per cell and infection. Further, co-localization studies were performed to determine the involvement of certain cellular internalization proteins. FIPV is not internalized through a clathrin-mediated pathway, as chlorpromazine, amantadine and DN eps

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Pan, Weiling, Yongxian Zhang, Fangfei Qi, et al. "Abstract 2039: Cellular characterization of small molecule PD-L1 inhibitors reveal their novel mechanisms of action." Cancer Research 84, no. 6_Supplement (2024): 2039. http://dx.doi.org/10.1158/1538-7445.am2024-2039.

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Abstract Introductions: Immune checkpoint inhibitors, including PD-1/L1, are key regulators of immune response and promising targets in cancer immunotherapy. Like anti-PD-1/L1 antibodies, small molecule PD-L1 inhibitors that have been discovered by us and others could also efficiently block PD-1 and PD-L1 interaction and exhibit anti-tumor efficacy in preclinical and clinically settings. In this study, we explore the cellular mechanism of small molecule PD-L1 inhibitors, unveiling their novel mechanisms of action in the regulation of PD-L1 and its functions. Materials and Methods: The cellular

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Goretzki, L., and B. M. Mueller. "Receptor-mediated endocytosis of urokinase-type plasminogen activator is regulated by cAMP-dependent protein kinase." Journal of Cell Science 110, no. 12 (1997): 1395–402. http://dx.doi.org/10.1242/jcs.110.12.1395.

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Internalization of the urokinase-type plasminogen activator (uPA) requires two receptors, the uPA receptor (uPAR) and the low density lipoprotein receptor-related protein (LRP)/alpha2-macroglobulin (alpha2M) receptor. Here, we address whether protein kinases are involved in the internalization of uPA by human melanoma cells. Initially, we found that the internalization of uPA was significantly inhibited by the serine/threonine protein kinase inhibitors staurosporine, K-252a and H-89, but not by the tyrosine kinase inhibitors, genistein and lavendustin A. Internalization of uPA was also inhibit

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Huang, Dianshuai, Qingjie Fan, Zhiyi Liu, et al. "An Epitope on EGFR Loading Catastrophic Internalization Serve as a Novel Oncotarget for Hepatocellular Carcinoma Therapy." Cancers 12, no. 2 (2020): 456. http://dx.doi.org/10.3390/cancers12020456.

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The precise role of Epidermal Growth Factor Receptor (EGFR) in Hepatocellular carcinoma (HCC) cells is unknown and EGFR inhibitors have not achieved positive clinical results. The rapid and drastic internalization of EGFR has been proved to successfully treat EGFR inhibitor-resistant patients in recent clinical trials. Here, the anti-tumor efficacy of a protein (rLZ-8) from Ganoderma lucidum was evaluated, it was demonstrated that rLZ-8 could bind to EGFR specifically, drastically enter into Hepatoma cells, abrogate endosomal recycling and induce HCC cell death. Surprisingly, we screened a mon

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Narazaki, Masashi, Marta Segarra, Xu Hou, Toshio Tanaka, Xuri Li, and Giovanna Tosato. "Oligo-guanosine nucleotide induces neuropilin-1 internalization in endothelial cells and inhibits angiogenesis." Blood 116, no. 16 (2010): 3099–107. http://dx.doi.org/10.1182/blood-2010-01-265801.

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Abstract Ligand interaction with cognate cell-surface receptor often promotes receptor internalization, protecting cells from prolonged or excessive signaling from extracellular ligands. Compounds that induce internalization of surface receptors prevent ligand binding to cognate cell-surface receptors serving as inhibitors. Here, we show that synthetic polyriboguanosine (poly G) and oligo-deoxyriboguanosine (oligo G) reduce endothelial levels of surface neuropilin-1 (NRP1), a receptor shared by semaphorin 3A and vascular endothelial growth factor (VEGF), which plays critical roles in angiogene

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Broad, Amanda J., Monette Aujay, Stefan D. Gross, Li Ren, Samuel Kintz, and Joseph P. Lyssikatos. "Abstract 4712: ELVN-002; a potent, selective HER2 inhibitor with a differentiated binding mode conferring the potential for enhanced efficacy in combination with HER2-targeting antibody-drug conjugates." Cancer Research 85, no. 8_Supplement_1 (2025): 4712. https://doi.org/10.1158/1538-7445.am2025-4712.

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Abstract Overexpression, amplification or mutation of human epidermal growth factor receptor 2 (HER2) is observed in up to 30% of solid tumors resulting in increased downstream signaling and oncogenic transformation. While trastuzumab deruxtecan (T-DXd), a HER2-targeting antibody-drug conjugate (ADC) recently approved for HER2 altered cancer types, has resulted in improved outcomes there remains a substantial unmet need for patients who either progress on T-DXd or discontinue treatment due to adverse events. The advent of small molecule HER2 inhibitors represents an opportunity to provide mean

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14

Orloff, G. M., S. L. Orloff, M. S. Kennedy, P. J. Maddon, and J. S. McDougal. "Penetration of CD4 T cells by HIV-1. The CD4 receptor does not internalize with HIV, and CD4-related signal transduction events are not required for entry." Journal of Immunology 146, no. 8 (1991): 2578–87. http://dx.doi.org/10.4049/jimmunol.146.8.2578.

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Abstract Receptor binding of HIV to the CD4 molecule is required for efficient infection of T cells, but the post-binding steps that result in penetration of HIV are not well understood. CD4 is induced to internalize upon T cell activation, and mAb to CD4 modify signal transduction and T cell activation as does HIV in some systems. It is not known whether HIV binding triggers CD4 endocytosis or whether signal transduction events are required for penetration. Selected inhibitors of signal transduction were evaluated for their effects on penetration using two assays that are dependent on penetra

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15

Xi, Chunhua, Xuan Liang, Chunhua Chen, Hasan Babazada, Tianzuo Li та Renyu Liu. "Hypoxia Induces Internalization of κ-Opioid Receptor". Anesthesiology 126, № 5 (2017): 842–54. http://dx.doi.org/10.1097/aln.0000000000001571.

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Abstract Background It has been demonstrated that κ-opioid receptor agonists can reduce hypoxia–ischemia brain injury in animal models. However, it is unclear how the κ-opioid receptor responds to hypoxia–ischemia. In the current study, the authors used an in vitro model of oxygen–glucose deprivation and reoxygenation to explore how κ-opioid receptors respond to hypoxia and reoxygenation. Methods Mouse neuroblastoma Neuro2A cells were stably transfected with mouse κ-opioid receptor–tdTomato fusion protein or Flag-tagged mouse κ-opioid receptor, divided into several groups (n = 6 to 12), and us

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Mueller, Anja, Eamonn Kelly, and Philip G. Strange. "Pathways for internalization and recycling of the chemokine receptor CCR5." Blood 99, no. 3 (2002): 785–91. http://dx.doi.org/10.1182/blood.v99.3.785.

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Abstract M-tropic human immunodeficiency virus (HIV-1) strains enter the cell after interaction with their receptors, CD4 and the G-protein–coupled chemokine receptor CCR5. The number of cell surface CCR5 molecules is thought to be important in determining the infection rate for HIV. Cell surface CCR5 is dependent on the rate of receptor internalization and recycling. Internalization of G-protein–coupled receptors after agonist activation is thought to occur either through clathrin-coated pits or through caveolae. In this study, the role of these different pathways was investigated in Chinese

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Zhang, Yaguang, Hongmei Shu, Jing Hu, et al. "Binding Affinity, Cellular Uptake, and Subsequent Intracellular Trafficking of the Nano-Gene Vector P123-PEI-R13." Journal of Nanomaterials 2016 (2016): 1–8. http://dx.doi.org/10.1155/2016/7064246.

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A nano-gene vector PEI-P123-R13 was synthesized by cross-linking low molecular weight PEI with P123 and further coupling bifunctional peptide R13 to the polymer for targeting tumor and increasing cellular uptake. The binding assessment of R13 toαvβ3 positive cells was performed by HRP labeling. The internalization pathways of P123-PEI-R13/DNA complexes were investigated based on the effect of specific endocytic inhibitors on transfection efficiency. The mechanism of intracellular trafficking was investigated based on the effect of endosome-lysosome acidification inhibitors, cytoskeleton, and d

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18

Tompkins, John D., Todd A. Clason, Thomas R. Buttolph, et al. "Src family kinase inhibitors blunt PACAP-induced PAC1 receptor endocytosis, phosphorylation of ERK, and the increase in cardiac neuron excitability." American Journal of Physiology-Cell Physiology 314, no. 2 (2018): C233—C241. http://dx.doi.org/10.1152/ajpcell.00223.2017.

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Pituitary adenylate cyclase activating polypeptide (PACAP, Adcyap1) activation of PAC1 receptors ( Adcyap1r1) significantly increases excitability of guinea pig cardiac neurons. This modulation of excitability is mediated in part by plasma membrane G protein-dependent activation of adenylyl cyclase and downstream signaling cascades. However, additional mechanisms responsible for the enhanced excitability are activated following internalization of the PAC1 receptor and endosomal signaling. Src family kinases play critical roles mediating endocytosis of many trophic factor and G protein-coupled

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Chou, Hsien-Yeh, Namasivayam Elangovan, Ying-Chu Lee, Hsiou Hsia Lin, and Sin-Tak Chu. "Internalization and trafficking of mouse 24p3 protein in L929 cells." Journal of Endocrinology 191, no. 1 (2006): 239–47. http://dx.doi.org/10.1677/joe.1.06909.

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It has been shown that mouse 24p3 protein is a dexamethasone-inducible secretory protein which suggests the involvement of an autocrine mechanism in the L929 cell line. The aim of this study was to investigate the possibilityof this mechanism in L929 cells and to also demonstrate further processing of this protein after association with L929 cells. We have characterized the internalization of 24p3 protein in L929 cells with fluorescein isothiocyanate- and Alexa555-labeled protein supplement instead of secreted 24p3 protein. As endocytotic inhibitors could reveal the inhibition of protein inter

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Matsuoka, Hidetada, and Masumi Inoue. "Src mediates endocytosis of TWIK-related acid-sensitive K+ 1 channels in PC12 cells in response to nerve growth factor." American Journal of Physiology-Cell Physiology 309, no. 4 (2015): C251—C263. http://dx.doi.org/10.1152/ajpcell.00354.2014.

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TWIK-related acid-sensitive K+ (TASK) channels produce background K+ currents. We elucidated that TASK1 channels in rat adrenal medullary cells and PC12 cells are internalized in a clathrin-dependent manner in response to nerve growth factor (NGF). Here, the molecular mechanism for this internalization in PC12 cells was explored. The combination of enzyme inhibitors with tropomyosin receptor kinase A mutants revealed that the internalization was mediated by both phospholipase C and phosphatidylinositol 3-kinase pathways that converge on protein kinase C with the consequent activation of Src, a

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Matsumoto, Sonoko, Takashi Shimizu, Akihiko Uda, Kenta Watanabe, and Masahisa Watarai. "Role of the JAK2/STAT3 pathway on infection of Francisella novicida." PLOS ONE 19, no. 9 (2024): e0310120. http://dx.doi.org/10.1371/journal.pone.0310120.

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Francisella tularensis is a causative agent of the zoonotic disease tularemia, and is highly pathogenic to humans. The pathogenicity of this bacterium is largely attributed to intracellular growth in host cells. Although several bacterial factors important for the intracellular growth have been elucidated, including the type VI secretion system, the host factors involved in the intracellular growth of F. tularensis are largely unknown. To identify the host factors important for F. tularensis infection, 368 compounds were screened for the negative regulation of F. tularensis subsp. novicida (F.

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Jochen, A. L., and P. Berhanu. "Chymotrypsin substrate analogues inhibit endocytosis of insulin and insulin receptors in adipocytes." Journal of Cell Biology 103, no. 5 (1986): 1807–16. http://dx.doi.org/10.1083/jcb.103.5.1807.

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To explore the possible role of proteolytic step(s) in receptor-mediated endocytosis of insulin, the effects of inhibitors of various classes of proteases on the internalization process were studied in isolated rat adipocytes. Intracellular accumulation of receptor-bound 125I-insulin at 37 degrees C was quantitated after rapidly dissociating surface-bound insulin with an acidic buffer (pH 3.0). Of the 23 protease inhibitors tested, only chymotrypsin substrate analogues inhibited insulin internalization. Internalization was decreased 62-90% by five different chymotrypsin substrate analogues: N-

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Nedellec, Rebecca, Mia Coetzer, Michael M. Lederman, Robin E. Offord, Oliver Hartley, and Donald E. Mosier. "“Resistance” to PSC-RANTES Revisited: Two Mutations in Human Immunodeficiency Virus Type 1 HIV-1SF162 or Simian-Human Immunodeficiency Virus SHIVSF162-p3 Do Not Confer Resistance." Journal of Virology 84, no. 11 (2010): 5842–45. http://dx.doi.org/10.1128/jvi.01907-09.

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ABSTRACT Resistance of human immunodeficiency virus type 1 (HIV-1) to small-molecule CCR5 inhibitors is well demonstrated, but resistance to macromolecular CCR5 inhibitors (e.g., PSC-RANTES) that act by both CCR5 internalization and receptor blockade had not been reported until recently (3). The report of a single simian-human immunodeficiency virus SHIVSF162-p3 variant with one V3 and one gp41 sequence change in gp160 that conferred both altered replicative fitness and resistance to PSC-RANTES was therefore surprising. We introduced the same two mutations into both the parental HIV-1SF162 and

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Janes, Mandy E., K. M. Emily Chu, Adrian J. L. Clark, and Peter J. King. "Mechanisms of Adrenocorticotropin-Induced Activation of Extracellularly Regulated Kinase 1/2 Mitogen-Activated Protein Kinase in the Human H295R Adrenal Cell Line." Endocrinology 149, no. 4 (2008): 1898–905. http://dx.doi.org/10.1210/en.2007-0949.

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The role of ACTH in stimulating or inhibiting growth of adrenal cells has been a subject of some controversy. Reports that ACTH may stimulate ERK/MAPK in Y1 cells have suggested a role for cAMP in this process. In attempting to extend this work, the ACTH responses in the human H295R cell line have been studied. This cell line makes only a very modest cAMP response to ACTH, yet the ERK1/2 response is highly reproducible and immediate but not prolonged. It is minimally reduced by the protein kinase A inhibitor, H89, but unaffected by protein kinase C and calcium inhibitors. Inhibition of epiderm

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Kierbel, A., A. Gassama-Diagne, K. Mostov, and J. N. Engel. "The Phosphoinositol-3-Kinase–Protein Kinase B/Akt Pathway Is Critical forPseudomonas aeruginosaStrain PAK Internalization." Molecular Biology of the Cell 16, no. 5 (2005): 2577–85. http://dx.doi.org/10.1091/mbc.e04-08-0717.

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Several Pseudomonas aeruginosa strains are internalized by epithelial cells in vitro and in vivo, but the host pathways usurped by the bacteria to enter nonphagocytic cells are not clearly understood. Here, we report that internalization of strain PAK into epithelial cells triggers and requires activation of phosphatidylinositol 3-kinase (PI3K) and protein kinase B/Akt (Akt). Incubation of Madin-Darby canine kidney (MDCK) or HeLa cells with the PI3K inhibitors LY294002 (LY) or wortmannin abrogated PAK uptake. Addition of the PI3K product phosphatidylinositol 3,4,5-trisphosphate [PtdIns(3,4,5)P

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Sneddon, John M., and Wanda M. Wenman. "The effect of ions on the adhesion and internalization of Chlamydia trachomatis by HeLa cells." Canadian Journal of Microbiology 31, no. 4 (1985): 371–74. http://dx.doi.org/10.1139/m85-071.

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The adhesion and internalization of Chlamydia trachomatis by HeLa cells was unaffected by removal of K+, Mg2+, or glucose from the incubation medium, slightly reduced by removal of Na+, and significantly reduced by omission of Ca2+. Sr2+, Mg2+, and Mn2+ could replace Ca2+ in the adhesion but only Sr2+ supported internalization, and La3+, Co2+, Fe3+, Ba2+, and Zn2+ all reduced internalization more than adhesion. During initial infection there was no measurable difference in the uptake or release of 45Ca2+ or 86Rb+ between infected and noninfected HeLa monolayers. Infection was not prevented by

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Khandaker, Masud H., Gordon Mitchell, Luoling Xu, et al. "Metalloproteinases Are Involved in Lipopolysaccharide– and Tumor Necrosis Factor-–Mediated Regulation of CXCR1 and CXCR2 Chemokine Receptor Expression." Blood 93, no. 7 (1999): 2173–85. http://dx.doi.org/10.1182/blood.v93.7.2173.

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Abstract The neutrophil-specific G-protein–coupled chemokine receptors, CXCR1 and CXCR2, bind with high affinity to the potent chemoattractant interleukin-8 (IL-8). The mechanisms of IL-8 receptor regulation are not well defined, although previous studies have suggested a process of ligand-promoted internalization as a putative regulatory pathway. Herein, we provide evidence for two distinct processes of CXCR1 and CXCR2 regulation. Confocal microscopy data showed a redistribution of CXCR1 expression from the cell surface of neutrophils to internal compartments after stimulation with IL-8, wher

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Khandaker, Masud H., Gordon Mitchell, Luoling Xu, et al. "Metalloproteinases Are Involved in Lipopolysaccharide– and Tumor Necrosis Factor-–Mediated Regulation of CXCR1 and CXCR2 Chemokine Receptor Expression." Blood 93, no. 7 (1999): 2173–85. http://dx.doi.org/10.1182/blood.v93.7.2173.407a06_2173_2185.

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The neutrophil-specific G-protein–coupled chemokine receptors, CXCR1 and CXCR2, bind with high affinity to the potent chemoattractant interleukin-8 (IL-8). The mechanisms of IL-8 receptor regulation are not well defined, although previous studies have suggested a process of ligand-promoted internalization as a putative regulatory pathway. Herein, we provide evidence for two distinct processes of CXCR1 and CXCR2 regulation. Confocal microscopy data showed a redistribution of CXCR1 expression from the cell surface of neutrophils to internal compartments after stimulation with IL-8, whereas stimu

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Rabehi, Lila, Théano Irinopoulou, Béatrice Cholley, Nicole Haeffner-Cavaillon, and Marie-Paule Carreno. "Gram-Positive and Gram-Negative Bacteria Do Not Trigger Monocytic Cytokine Production through Similar Intracellular Pathways." Infection and Immunity 69, no. 7 (2001): 4590–99. http://dx.doi.org/10.1128/iai.69.7.4590-4599.2001.

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ABSTRACT Toll-like receptors (TLRs) are involved in human monocyte activation by lipopolysaccharide (LPS) and Staphylococcus aureus Cowan (SAC), suggesting that gram-positive and gram-negative bacteria may trigger similar intracellular events. Treatment with specific kinase inhibitors prior to cell stimulation dramatically decreased LPS-induced cytokine production. Blocking of the p38 pathway prior to LPS stimulation decreased interleukin-1α (IL-1α), IL-1ra, and tumor necrosis factor alpha (TNF-α) production, whereas blocking of the ERK1/2 pathways inhibited IL-1α, IL-1β, and IL-1ra but not TN

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Tang, Hongbo, Mengyao Wu, Weijie Jiang, et al. "Endocytosis and Transport of Silica Nanoparticles in BeWo b30 Cells." International Internal Medicine Journal 2, no. 8 (2024): 01–11. http://dx.doi.org/10.33140/iimj.02.08.07.

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An understanding of the transport of silica nanoparticles (NPs) across the placental barrier is important in perinatal medicine. The cytotoxicity of silica NPs was investigated in this study. In up-take assays, we examined the size of NPs, as well as the effects of various inhibitors, on the internalization of silica NPs in BeWo b30 cells. The expression levels of PI3K, AKT and GSK3β were assessed after the cells were treated with silica NPs and/or the PI3K/ AKT signaling pathway inhibitor LY294002. The integrity of the cell monolayer was assessed by culturing cells on Transwell inserts and me

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Kwon, Yong-Jun, Weontae Lee, Auguste Genovesio, and Neil Emans. "A High-Content Subtractive Screen for Selecting Small Molecules Affecting Internalization of GPCRs." Journal of Biomolecular Screening 17, no. 3 (2011): 379–85. http://dx.doi.org/10.1177/1087057111427347.

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G-protein–coupled receptors (GPCRs) are pivotal in cellular responses to the environment and are common drug targets. Identification of selective small molecules acting on single GPCRs is complicated by the shared machinery coupling signal transduction to physiology. Here, we demonstrate a high-content screen using a panel of GPCR assays to identify receptor selective molecules acting within the kinase/phosphatase inhibitor family. A collection of 88 kinase and phosphatase inhibitors was screened against seven agonist-induced GPCR internalization cell models as well as transferrin uptake in hu

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Zlotnikov, Igor D., Alexander A. Ezhov, and Elena V. Kudryashova. "Receptor-Mediated Internalization of L-Asparaginase into Tumor Cells Is Suppressed by Polyamines." International Journal of Molecular Sciences 26, no. 14 (2025): 6749. https://doi.org/10.3390/ijms26146749.

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L-asparaginase (L-ASNase) remains a vital chemotherapeutic agent for acute lymphoblastic leukemia (ALL), primarily due to its mechanism of depleting circulating asparagine essential for leukemic cell proliferation. However, existing ASNases (including pegylated ones) face limitations including immunogenicity, rapid clearance, and off-target toxicities. Earlier, we have shown that the conjugation of L-ASNase with the polyamines and their copolymers results in significant enhancement of the antiproliferative activity due to accumulation in tumor cells. We suggested that this effect is probably m

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Gemei, Marica, Carmine Talarico, Laura Brandolini, et al. "Binding Mode Exploration of B1 Receptor Antagonists’ by the Use of Molecular Dynamics and Docking Simulation—How Different Target Engagement Can Determine Different Biological Effects." International Journal of Molecular Sciences 21, no. 20 (2020): 7677. http://dx.doi.org/10.3390/ijms21207677.

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The kinin B1 receptor plays a critical role in the chronic phase of pain and inflammation. The development of B1 antagonists peaked in recent years but almost all promising molecules failed in clinical trials. Little is known about these molecules’ mechanisms of action and additional information will be necessary to exploit the potential of the B1 receptor. With the aim of contributing to the available knowledge of the pharmacology of B1 receptors, we designed and characterized a novel class of allosteric non-peptidic inhibitors with peculiar binding characteristics. Here, we report the bindin

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Mortensen, Ole Valente, Mads Breum Larsen, Balakrishna M. Prasad, and Susan G. Amara. "Genetic Complementation Screen Identifies a Mitogen-activated Protein Kinase Phosphatase, MKP3, as a Regulator of Dopamine Transporter Trafficking." Molecular Biology of the Cell 19, no. 7 (2008): 2818–29. http://dx.doi.org/10.1091/mbc.e07-09-0980.

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The antidepressant and cocaine sensitive plasma membrane monoamine transporters are the primary mechanism for clearance of their respective neurotransmitters and serve a pivotal role in limiting monoamine neurotransmission. To identify molecules in pathways that regulate dopamine transporter (DAT) internalization, we used a genetic complementation screen in Xenopus oocytes to identify a mitogen-activated protein (MAP) kinase phosphatase, MKP3/Pyst1/DUSP6, as a molecule that inhibits protein kinase C–induced (PKC) internalization of transporters, resulting in enhanced DAT activity. The involvem

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Baidya, Gaurav, Rameshvar Tiwary, Madeeha Mudassir, et al. "Passive internalization and active extrusion determines PLGA-nanoparticle concentration in cancer cell lines." Nanomedicine 15, no. 23 (2020): 2229–39. http://dx.doi.org/10.2217/nnm-2020-0229.

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Background: Poly(lactic-co-glycolic) acid nanoparticle (PLGA-NP) trafficking across cell membranes was investigated to confirm preliminary results that contradicted existing studies. Materials & methods: Uptake and retention of PLGA-NPs at 37 and 4°C in the presence and absence of metabolic inhibitors in various cell lines was estimated. Results: Pulse experiments with metabolic inhibitors and culturing at 4°C demonstrated the predominantly passive nature of PLGA-NP uptake. Chase experiments with metabolic inhibitors indicated the role of active exocytosis in the extrusion of these NPs. PL

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Morinelli, Thomas A., Mi-Hye Lee, Ryan T. Kendall, Louis M. Luttrell, Linda P. Walker та Michael E. Ullian. "Angiotensin II activates NF-κB through AT1A receptor recruitment of β-arrestin in cultured rat vascular smooth muscle cells". American Journal of Physiology-Cell Physiology 304, № 12 (2013): C1176—C1186. http://dx.doi.org/10.1152/ajpcell.00235.2012.

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Activation of the angiotensin type 1A receptor (AT1AR) in rat aorta vascular smooth muscle cells (RASMC) results in increased synthesis of the proinflammatory enzyme cyclooxygenase-2 (COX-2). We previously showed that nuclear localization of internalized AT1AR results in activation of transcription of the gene for COX-2, i.e., prostaglandin-endoperoxide synthase-2. Others have suggested that ANG II stimulation of COX-2 protein synthesis is mediated by NF-κB. The purpose of the present study was to examine the interrelationship between AT1AR activation, β-arrestin recruitment, and NF-κB activat

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Apirakaramwong, A., Perayot Pamonsinlapatham, S. Techaarpornkul, Praneet Opanasopit, Suwannee Panomsuk, and S. Soksawatmaekhin. "Mechanisms of Cellular Uptake with Chitosan/DNA Complex in Hepatoma Cell Line." Advanced Materials Research 506 (April 2012): 485–88. http://dx.doi.org/10.4028/www.scientific.net/amr.506.485.

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Chitosan (CS) has a high potential for gene delivery into mammalian cells. However, its uptake mechanism is not well clarified. We investigated the effects of inhibitors of clathrin-mediated endocytosis (chlorpromazine), caveolae-mediated endocytosis (genistein), macropinocytosis (LY 29004 and wortmannin), microtubuli polymerization (nocodazole) and of membrane cholesterol recycle (methyl-β-cyclodextrin) on the transfection efficiency with CS/pEGFP complexes and on the internalization of CS/rhodamine-labeled pEGFP complexes by hepatoma cell line (Huh 7 cells). The transfection was blocked by n

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Kansra, Sanjay, Stefan W. Stoll, Jessica L. Johnson, and James T. Elder. "Autocrine Extracellular Signal-regulated Kinase (ERK) Activation in Normal Human Keratinocytes: Metalloproteinase-mediated Release of Amphiregulin Triggers Signaling from ErbB1 to ERK." Molecular Biology of the Cell 15, no. 9 (2004): 4299–309. http://dx.doi.org/10.1091/mbc.e04-03-0233.

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ErbB signaling through extracellular signal-regulated kinase (ERK) has been implicated in regulating the expression of ErbB ligands in hyperproliferative skin disorders and wound healing. Here, we characterize the process of autocrine ERK activation in cultured normal human keratinocytes (NHKs) subjected to growth factor (GF) deprivation. Basal ERK phosphorylation was lower after 48 h than after 24 h of GF deprivation, and lowest at 30–60 min after an additional medium change. ERK phosphorylation was markedly increased by low concentrations of epidermal growth factor (EGF) (0.2–1 ng/ml) that p

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Casartelli, M., G. Cermenati, S. Rodighiero, F. Pennacchio, and B. Giordana. "A megalin-like receptor is involved in protein endocytosis in the midgut of an insect (Bombyx mori, Lepidoptera)." American Journal of Physiology-Regulatory, Integrative and Comparative Physiology 295, no. 4 (2008): R1290—R1300. http://dx.doi.org/10.1152/ajpregu.00036.2008.

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The mechanism responsible for fluorescein isothiocyanate (FITC)-albumin internalization by columnar cells in culture obtained from the midgut of Bombyx mori larvae was examined by confocal laser scanning microscopy. Protein uptake changed over time, and it appeared to be energy dependent, since it was strongly reduced by both low temperatures and metabolic inhibitors. Labeled albumin uptake as a function of increasing protein concentration showed a saturation kinetics with a Michaelis constant value of 2.0 ± 0.6 μM. These data are compatible with the occurrence of receptor-mediated endocytosis

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Xu, Yi, Betty Revon Liu, Han-Jung Lee, et al. "Nona-Arginine Facilitates Delivery of Quantum Dots into Cells via Multiple Pathways." Journal of Biomedicine and Biotechnology 2010 (2010): 1–11. http://dx.doi.org/10.1155/2010/948543.

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Semiconductor quantum dots (QDs) have recently been used to deliver and monitor biomolecules, such as drugs and proteins. However, QDs alone have a low efficiency of transport across the plasma membrane. In order to increase the efficiency, we used synthetic nona-arginine (SR9), a cell-penetrating peptide, to facilitate uptake. We found that SR9 increased the cellular uptake of QDs in a noncovalent binding manner between QDs and SR9. Further, we investigated mechanisms of QD/SR9 cellular internalization. Low temperature and metabolic inhibitors markedly inhibited the uptake of QD/SR9, indicati

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Estall, Jennifer L., Bernardo Yusta, and Daniel J. Drucker. "Lipid Raft-dependent Glucagon-like Peptide-2 Receptor Trafficking Occurs Independently of Agonist-induced Desensitization." Molecular Biology of the Cell 15, no. 8 (2004): 3673–87. http://dx.doi.org/10.1091/mbc.e03-11-0825.

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The intestinotrophic and cytoprotective actions of glucagon-like peptide-2 (GLP-2) are mediated by the GLP-2 receptor (GLP-2R), a member of the class II glucagon-secretin G protein-coupled receptor superfamily. Although native GLP-2 exhibits a short circulating half-life, long-acting degradation-resistant GLP-2 analogues are being evaluated for therapeutic use in human subjects. Accordingly, we examined the mechanisms regulating signaling, internalization, and trafficking of the GLP-2R to identify determinants of receptor activation and desensitization. Heterologous cells expressing the transf

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Pratt, Jonathan, Khadidja Haidara, and Borhane Annabi. "MT1-MMP Expression Levels and Catalytic Functions Dictate LDL Receptor-Related Protein-1 Ligand Internalization Capacity in U87 Glioblastoma Cells." International Journal of Molecular Sciences 23, no. 22 (2022): 14214. http://dx.doi.org/10.3390/ijms232214214.

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Modulations in cell surface receptor ectodomain proteolytic shedding impact on receptor function and cancer biomarker expression. As such, heavily pursued therapeutic avenues have exploited LDL receptor-related protein-1 (LRP-1)-mediated capacity in internalizing Angiopep-2 (An2), a brain-penetrating peptide that allows An2–drug conjugates to cross the blood–brain tumor barrier (BBTB). Given that LRP-1 is proteolytically shed from the cell surface through matrix metalloproteinase (MMP) activity, the balance between MMP expression/function and LRP-1-mediated An2 internalization is unknown. In t

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Soltész, Dóra, Ildikó Szabó, and Zoltán Bánóczi. "The Balance between Hydrophobicity/Aromaticity and Positively Charged Residues May Influence the Cell Penetration Ability." Pharmaceutics 15, no. 4 (2023): 1267. http://dx.doi.org/10.3390/pharmaceutics15041267.

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Cell-penetrating peptides (CPPs) are commonly modified to increase their cellular uptake, alter the mechanism of penetration or enhance their endosomal release. Earlier, we described the internalization enhancement ability of the 4-((4-(dimethylamino)phenyl)azo)benzoyl (Dabcyl) group. We proved that this modification on the N-terminus of tetra- and hexaarginine enhanced their cellular uptake. The introduction of an aromatic ring 4-(aminomethyl) benzoic acid, AMBA) into the peptide backbone has a synergistic effect with Dabcyl, and the tetraarginine derivatives had outstanding cellular uptake.

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Klimovich, Maria, Latifa Zekri, Gundram Jung, and Helmut R. Salih. "Abstract 2886: Antigen internalization and its prevention during treatment with bispecific antibodies." Cancer Research 82, no. 12_Supplement (2022): 2886. http://dx.doi.org/10.1158/1538-7445.am2022-2886.

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Abstract Antigen-mediated antibody internalization is an important factor influencing kinetics and efficacy of antibody-based therapeutics. Antibodies directed against HER2, CD20, FLT3, EGFR, CD10 and CD22 have been shown to undergo internalization upon binding to their target antigens. Although antibody-induced internalization may be desirable under some circumstances, for example in case of antibody-drug conjugates, it can subvert the therapeutic efficacy of ADCC-inducing antibodies and bispecific antibodies (bsAbs) aiming to mobilize T cells against cancer. Here we examined the turnover of

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Alam, Syed Benazir, and Marianna Kulka. "Internalization of benzylisoquinoline alkaloids by resting and activated bone marrow-derived mast cells utilizes energy-dependent mechanisms." Inflammation Research 71, no. 3 (2022): 343–56. http://dx.doi.org/10.1007/s00011-021-01526-2.

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Abstract Objective and design Drug delivery to inflammatory cells is dependent upon poorly understood, complex endocytic processes. Berberine (BBR), a benzylisoquinoline alkaloid, binds to heparin and targets glycosaminoglycan-rich granules in mast cells (MC), but the mechanism of BBR internalization is unknown. Methods BMMC were treated with various concentrations of BBR for different amounts of time and BBR internalization was assessed by flow cytometry and fluorescence microscopy. BMMC were pretreated with endocytic inhibitors or a growth factor (IL-3) prior to BBR exposure to access mechan

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Setiadi, Hendra, and Rodger P. McEver. "Signal-dependent distribution of cell surface P-selectin in clathrin-coated pits affects leukocyte rolling under flow." Journal of Cell Biology 163, no. 6 (2003): 1385–95. http://dx.doi.org/10.1083/jcb.200307178.

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Flowing leukocytes roll on P-selectin that is mobilized from secretory granules to the surfaces of endothelial cells after stimulation with histamine or thrombin. Before it is internalized, P-selectin clusters in clathrin-coated pits, which enhances its ability to support leukocyte rolling. We found that thrombin and histamine induced comparable exocytosis of P-selectin on endothelial cells. However, compared with histamine, thrombin decreased the recruitment of P-selectin into clathrin-coated pits, slowed the internalization of P-selectin, and reduced the number and stability of neutrophils r

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Basagiannis, Dimitris, Sofia Zografou, Evangeli Goula, Despoina Gkeka, Evangelos Kolettas, and Savvas Christoforidis. "Chemical Inhibitors of Dynamin Exert Differential Effects in VEGF Signaling." Cells 10, no. 5 (2021): 997. http://dx.doi.org/10.3390/cells10050997.

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VEGFR2 is the main receptor and mediator of the vasculogenic and angiogenic activity of VEGF. Activated VEGFR2 internalizes through clathrin-mediated endocytosis and macropinocytosis. As dynamin is a key regulator of the clathrin pathway, chemical inhibitors of dynamin are commonly used to assess the role of the clathrin route in receptor signaling. However, drugs may also exert off-target effects. Here, we compare the effects of three dynamin inhibitors, dynasore, dyngo 4a and dynole, on VEGFR2 internalization and signaling. Although these drugs consistently inhibit clathrin-mediated endocyto

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Snyers, Luc, Hannes Zwickl, and Dieter Blaas. "Human Rhinovirus Type 2 Is Internalized by Clathrin-Mediated Endocytosis." Journal of Virology 77, no. 9 (2003): 5360–69. http://dx.doi.org/10.1128/jvi.77.9.5360-5369.2003.

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ABSTRACT Using several approaches, we investigated the importance of clathrin-mediated endocytosis in the uptake of human rhinovirus serotype 2 (HRV2). By means of confocal immunofluorescence microscopy, we show that K+ depletion strongly reduces HRV2 internalization. Viral uptake was also substantially reduced by extraction of cholesterol from the plasma membrane with methyl-β-cyclodextrin, which can inhibit clathrin-mediated endocytosis. In accordance with these data, overexpression of dynamin K44A in HeLa cells prevented HRV2 internalization, as judged by confocal immunofluorescence microsc

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Li, Ruifang, Chen Chen, Sha Zhu, et al. "CGA-N9, an antimicrobial peptide derived from chromogranin A: direct cell penetration of and endocytosis by Candida tropicalis." Biochemical Journal 476, no. 3 (2019): 483–97. http://dx.doi.org/10.1042/bcj20180801.

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Abstract CGA-N9 is a peptide derived from the N-terminus of human chromogranin A comprising amino acids 47–55. Minimum inhibitory concentration (MIC) assays showed that CGA-N9 had antimicrobial activity and exhibited time-dependent inhibition activity against Candida tropicalis, with high safety in human red blood cells (HRBCs) and mouse brain microvascular endothelial cells (bEnd.3). According to the results of transmission electron microscopy (TEM), flow cytometry and confocal microscopy, CGA-N9 accumulated in cells without destroying the integrity of the cell membrane; the peptide was initi

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Jochen, Albert, and Paulos Berhanu. "Effects of metalloendoprotease inhibitors on insulin binding, internalization and processing in adipocytes." Biochemical and Biophysical Research Communications 142, no. 1 (1987): 205–12. http://dx.doi.org/10.1016/0006-291x(87)90472-4.

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