Academic literature on the topic 'Aminopeptidases Synthesis'
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Journal articles on the topic "Aminopeptidases Synthesis"
Kohno, H., and T. Kanno. "Properties and activities of aminopeptidases in normal and mitogen-stimulated human lymphocytes." Biochemical Journal 226, no. 1 (February 15, 1985): 59–65. http://dx.doi.org/10.1042/bj2260059.
Full textCunningham, Eithne, Marcin Drag, Pawel Kafarski, and Angus Bell. "Chemical Target Validation Studies of Aminopeptidase in Malaria Parasites Using α-Aminoalkylphosphonate and Phosphonopeptide Inhibitors." Antimicrobial Agents and Chemotherapy 52, no. 9 (May 5, 2008): 3221–28. http://dx.doi.org/10.1128/aac.01327-07.
Full textSalomon, Emmanuel, Marjorie Schmitt, Anil Marapaka, Athanasios Stamogiannos, Germain Revelant, Céline Schmitt, Sarah Alavi, et al. "Aminobenzosuberone Scaffold as a Modular Chemical Tool for the Inhibition of Therapeutically Relevant M1 Aminopeptidases." Molecules 23, no. 10 (October 11, 2018): 2607. http://dx.doi.org/10.3390/molecules23102607.
Full textBradshaw, Ralph A., and Elizabeth Yi. "Methionine aminopeptidases and angiogenesis." Essays in Biochemistry 38 (October 1, 2002): 65–78. http://dx.doi.org/10.1042/bse0380065.
Full textTeague, Andrea S., Manik A. Amin, Kian-Huat Lim, Albert C. Lockhart, Ashiq Masood, Joel Picus, Preet Paul Singh, Rama Suresh, Benjamin R. Tan, and Andrea Wang-Gillam. "A phase I/II study combining tosedostat with capecitabine in patients with metastatic pancreatic adenocarcinoma." Journal of Clinical Oncology 34, no. 4_suppl (February 1, 2016): TPS471. http://dx.doi.org/10.1200/jco.2016.34.4_suppl.tps471.
Full textBertin, Patrícia B., Silene P. Lozzi, Jerrilyn K. Howell, Glória Restrepo-Cadavid, David Neves, Antonio R. L. Teixeira, Marcelo V. de Sousa, Steven J. Norris, and Jaime M. Santana. "The Thermophilic, Homohexameric Aminopeptidase of Borrelia burgdorferi Is a Member of the M29 Family of Metallopeptidases." Infection and Immunity 73, no. 4 (April 2005): 2253–61. http://dx.doi.org/10.1128/iai.73.4.2253-2261.2005.
Full textOcain, Timothy D., and Daniel H. Rich. "Synthesis of sulfur-containing analogs of bestatin. Inhibition of aminopeptidases by .alpha.-thiolbestatin analogs." Journal of Medicinal Chemistry 31, no. 11 (November 1988): 2193–99. http://dx.doi.org/10.1021/jm00119a022.
Full textWanat, Weronika, Michał Talma, Błażej Dziuk, and Paweł Kafarski. "Synthesis and Inhibitory Studies of Phosphonic Acid Analogues of Homophenylalanine and Phenylalanine towards Alanyl Aminopeptidases." Biomolecules 10, no. 9 (September 14, 2020): 1319. http://dx.doi.org/10.3390/biom10091319.
Full textWęglarz-Tomczak, Ewelina, Katarzyna Staszewska, Michał Talma, and Artur Mucha. "Enantiomeric α,β-diaminoethylphosphonic acids as potent inhibitors of aminopeptidases—stereoselective synthesis and biological activity." Tetrahedron Letters 57, no. 43 (October 2016): 4812–14. http://dx.doi.org/10.1016/j.tetlet.2016.09.051.
Full textHebert, Elvira M., Raul R. Raya, and Graciela S. De Giori. "Nutritional Requirements and Nitrogen-Dependent Regulation of Proteinase Activity of Lactobacillus helveticus CRL 1062." Applied and Environmental Microbiology 66, no. 12 (December 1, 2000): 5316–21. http://dx.doi.org/10.1128/aem.66.12.5316-5321.2000.
Full textDissertations / Theses on the topic "Aminopeptidases Synthesis"
Andersson, Hanna. "Design and Synthesis of Angiotensin IV Peptidomimetics Targeting the Insulin-Regulated Aminopeptidase (IRAP)." Doctoral thesis, Uppsala : Acta Universitatis Upsaliensis, 2010. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-122218.
Full textCamberlein, Virgyl. "Target-guided synthesis of metalloenzymes ligands with therapeutic applications." Thesis, Université de Lille (2022-....), 2022. http://www.theses.fr/2022ULILS004.
Full textTarget-guided synthesis of protein ligands is an innovative strategy to discover bioactive compounds. In particular, the Kinetic Target-Guided Synthesis (KTGS) and the Dynamic Combinatorial Chemistry (DCC) have allowed, in recent years, the discovery of novel ligands for poorly explored therapeutic targets, which has enabled drug-discovery projects. This thesis project aims at using KTGS to discover and optimize ligands for two classes of metalloenzymes, namely endoplasmic reticulum aminopeptidases (ERAPs) and elastase LasB from the bacterium Pseudomonas aeruginosa. ERAPs (1 and 2) are involved in the process of antigen maturation. These enzymes cleave peptide precursors into mature antigenic peptides so that they have an optimal size for their complexation to the major histocompatibility complex of class I and thus initiate or not the adaptive immune response. The expression levels of these proteases as well as single nucleotide polymorphisms have been associated with the development of cancers and autoimmune diseases. Thus, the modulation of these enzymes would allow to fight against pathologies associated with the immune system. P. aeruginosa is a Gram-negative bacterium with remarkable virulence and antimicrobial resistance. Today, antibiotic resistance represents a major public health issue and there is an urgent need for new therapeutics. In order to meet this need, new strategies have emerged such as targeting the virulence of bacteria to "disarm" them. LasB represents a therapeutic target of choice due to its extracellular localization and its physiopathological implications (colonization, invasion, evasion of immune response, biofilm formation, etc.). Although there is a clear unmet medical need in these two therapeutic areas, no modulator of ERAPs or LasB has reached the market. Thus, the use of the KTGS strategy followed by optimization phases allowed us to identify and optimize new families of ligands for these enzymes. These compounds can be considered as promising lead compounds since they present nanomolar affinities for their respective targets, selectivity and toxicity profiles as well as remarkable physicochemical properties
Rigby, Annette. "Synthesis of new aminopeptidase sensitive substrates." Thesis, Northumbria University, 2004. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.410375.
Full textAgalo, Faith. "Synthesis of Insulin-Regulated Aminopeptidase (IRAP) inhibitors." Thesis, Uppsala universitet, Analytisk kemi, 2015. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-257559.
Full textYOSHPE-BESANCON, IRIS. "Purification et caracterisation de nouvelles aminopeptidases; utilisation en synthese peptidique." Paris 7, 1993. http://www.theses.fr/1993PA077316.
Full textMnkandhla, Dumisani. "Synthesis of silver nanoparticles and their role against human and Plasmodium falciparum leucine aminopeptidase." Thesis, Rhodes University, 2015. http://hdl.handle.net/10962/d1017911.
Full textRoux, Lionel. "Conception et synthèse d'inhibiteurs de l'Aminopeptidase membranaire N ([EC. 3.4.11.2], APN ou CD13)." Thesis, Mulhouse, 2010. http://www.theses.fr/2010MULH4691/document.
Full textThe fight against the cancer is one of the most important struggles of this century. For the development of the tumors inside the body, they need to receive nutriments by the blood vessels and they use the angiogenic process. During this process, the endothelial cells being shown on the wall of the blood vessel will multiply and design new blood vessel, which will allow the tumor's vascularisation. Today, the angiogenesis is an axis of research for the fight against the cancer. During the tumoral development, the aminopeptidase N (APN) is overexpressed on the wall of endothelial cells. Various studies have shown that the inhibition of this enzyme stops the tumoral progression. My work in the Pr. Céline Tarnus Team consists in the conception and the synthesis of APN's inhibitors. In a first time, a structure activity relationship has been realized. Syntheses of a subnamolar compound have been developed, and then the synthesis of APN's inhibitors with the use of BNCT has been got onto
Schneider, Magdalena [Verfasser], Tanja [Gutachter] Schirmeister, and Samuel [Gutachter] Samnick. "Synthese, Radiomarkierung und biochemische sowie präklinische Evaluierung neuer Aminopeptidase N- und Fibroblasten-Aktivierungs-Protein alpha- affiner Verbindungen für die molekulare Bildgebung mittels Positronen-Emissions-Tomographie / Magdalena Schneider. Gutachter: Tanja Schirmeister ; Samuel Samnick." Würzburg : Universität Würzburg, 2014. http://d-nb.info/1102827592/34.
Full textOcain, Timothy D. "Synthetic and mechanistic studies of aminopeptidase inhibitors." 1986. http://catalog.hathitrust.org/api/volumes/oclc/13988895.html.
Full textTypescript. Vita. eContent provider-neutral record in process. Description based on print version record. Includes bibliographical references (leaves 143-149).
Schneider, Magdalena. "Synthese, Radiomarkierung und biochemische sowie präklinische Evaluierung neuer Aminopeptidase N- und Fibroblasten-Aktivierungs-Protein alpha- affiner Verbindungen für die molekulare Bildgebung mittels Positronen-Emissions-Tomographie." Doctoral thesis, 2014. https://nbn-resolving.org/urn:nbn:de:bvb:20-opus-102562.
Full textAfter myocardial infarction, processes of wound healing are initiated in order to regain perfusion and to replace necrotic muscle tissue with soft tissue. The sprouting of new capillaries from the vasculature is called angiogenesis. During Angiogenesis, Aminopeptidase N (APN) plays an important role in the sprouting of endothelial cells. Cardiac remodeling is the process of replacement of necrotic myocytes with soft tissue through invasion of fibroblasts. For this cause, also a lot of proteases are activated. During the process of cardiac remodeling, fibroblast activation protein alpha (FAP) is involved in proliferation and migration of cardiac fibroblasts. Due to their increased expression during remodeling processes after myocardial infarction, the metalloprotease APN and the serine protease FAP have been identified as potential molecular targets for diagnosis and therapy. Diagnosis of the heart by nuclear imaging techniques is a well established method in clinical cardiology. Most of all positron emission tomopgraphy (PET) provides information on biochemical processes in vivo using specific radiotracers in real time. This imaging probe is labeled with a positron emitting radionuclide and is called radiopharmaceutical or tracer. In case of an enzyme, the tracer might for example be a labeled substrate or inhibitor of the enzyme. To visualize the protease APN with PET, NOTA-NGR (chelating agent + peptide sequence incl. asparagine-glycine-arginine), a compound that shows high affinity for APN, was labeled with the positron emitting nuclide Gallium-68 (68Ga). 68Ga-NOTA-NGR was developed including an improved synthesis, isolation and formulation of the tracer. Its potential as a PET-tracer was assessed in vivo using micro-PET and compared to the established tracer 68Ga-NOTA-RGD, used to visualize the integrin alphavbeta3 in angiogenesis. Studies in rats with ischemia/reperfusion showed high uptake of the new radiopharmaceutical 68Ga-NOTA-NGR in myocardial infarction area being used in diagnostic PET imaging of APN. The new tracer shows even a slightly higher uptake in angiogenetic areas compared with results obtained with 68Ga-NOTA-RGD. 68Ga-NOTA-NGR was also examined ex vivo using autoradiography, confirming the significant higher accumulation of the tracer in the ischemic area compared with the healthy myocardium. The different areas of the tissue were displayed by HE staining. For the purpose of immunohistochemistry, the expression of the enzyme APN was verified using antibody staining. Additionally several other factors that are involved in angiogenesis were stained. Through antibody staining APN was shown to be a suitable target for the evidence of angiogenesis. With 68Ga-NOTA-NGR, the development of a new PET-tracer for diagnosis of the expression of APN during angiogenesis after myocardial infarction was successful. In order to develop an imaging probe suitable for investigation of the protease FAP using PET, several peptidomimetic inhibitors containing the dipeptide motif glycine-proline and the electrophilic moiety carbonitrile were designed. With N-Acetylglycine-pyrrolidine-(2S)-carbonitrile being the basic structure, modifications were introduced through a benzoylic residue at the N-terminus. In addition, some well-known inhibitors were synthesized for comparison to the new ones in enzymatic assay. To evaluate their inhibitory effect, the new inhibitors were tested in enzymatic assays using FAP and dipeptidyl peptidase IV, a prolyl peptidase from the same family in order to compare the results with regard to selectivity. None of the new compounds showed a KI-value in the nanomolar range, required for visualization of an enzyme expression using PET. In order to investigate a PET-Tracer, the best inhibitors against FAP had to be labeled with a positron emitter. The radioactive analogues of the inhibitors were obtained using isotopic exchange of the natural iodine-nuclide by iodine-124 (124I), resulting in 1-(2-[124I]Iodohippuric acid)-pyrrolidine-(2S)-carbonitrile und 1-(4-[124I]Iodohippuric acid)-pyrrolidine-(2S)-carbonitrile. 1-(2-[124I]Iodohippuric acid)-pyrrolidine-(2S)-carbonitrile was tested in vivo using microPET in rats with myocardial infarction. Very low uptake of the radiopharmaceutical was observed in the ischemic area of the rat´s heart. Locations of ischemic and surviving parts of the myocardium were confirmed using HE staining. To our knowledge, 1-(2-[124I]Iodohippuric acid)-pyrrolidine-(2S)-carbonitrile is the first FAP-affine tracer developed for PET investigation. However, its potential as tracer for the FAP-expression within the myocardial infarction in vivo using PET could not be proven in the present study. Therefore, developments based on the structure of 1-(2-[124I]Iodohippuric acid)-pyrrolidine-(2S)-carbonitrile are going on, with view to identify a PET-tracer suitable for in-vivo-investigation of FAP in healing processes and remodeling after myocardial infarction using PET
Books on the topic "Aminopeptidases Synthesis"
Rigby, Annette. Synthesis of new aminopeptidase sensitive substrates. 2004.
Find full textBook chapters on the topic "Aminopeptidases Synthesis"
Tzougraki, C., C. Noula, R. Geiger, and G. Kokotos. "Synthesis and study of fluorogenic substrates containing 7-amino-4-methyl-2-quinolinone for aminopeptidase M, chymotrypsin, elastase and trypsin." In Peptides 1994, 889–90. Dordrecht: Springer Netherlands, 1995. http://dx.doi.org/10.1007/978-94-011-1468-4_409.
Full textConference papers on the topic "Aminopeptidases Synthesis"
Mucha, Artur, Jolanta Grembecka, Tomasz Cierpicki, and Paweł Kafarski. "The synthesis of phosphonamidate and phosphinic dipeptide analogues - Inhibitors of leucine aminopeptidase." In VIIth Conference Biologically Active Peptides. Prague: Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, 2001. http://dx.doi.org/10.1135/css200104028.
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