Academic literature on the topic 'Folate receptor α'

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Journal articles on the topic "Folate receptor α"

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Boss, Silvan D., and Simon Mensah Ametamey. "Development of Folate Receptor−Targeted PET Radiopharmaceuticals for Tumor Imaging—A Bench-to-Bedside Journey." Cancers 12, no. 6 (June 9, 2020): 1508. http://dx.doi.org/10.3390/cancers12061508.

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The folate receptor-α (FR-α) is overexpressed in many epithelial cancers, including ovary, uterus, kidneys, breast, lung, colon and prostate carcinomas, but shows limited expression in normal tissues such as kidneys, salivary glands, choroid plexus and placenta. FR-α has therefore emerged as a promising target for the delivery of therapeutic and imaging agents to FR-positive tumors. A series of folate-based PET (positron emission tomography) radiopharmaceuticals have been developed for the selective targeting of FR-positive malignancies. This review provides an overview on the research progress made so far regarding the design, radiosynthesis and the utility of the folate-derived PET radioconjugates for targeting FR-positive tumors. For the most part, results from folate radioconjugates labeled with fluorine-18 (t1/2 = 109.8 min) and gallium-68 (t1/2 = 67.7 min) have been presented but folates labeled with “exotic” and new PET radionuclides such as copper-64 (t1/2 = 12.7 h), terbium-152 (t1/2 = 17.5 h), scandium-44 (t1/2 = 3.97 h), cobalt-55 (t1/2 = 17.5 h) and zirconium-89 (t1/2 = 78.4 h) are also discussed. For tumor imaging, none of the reported PET radiolabeled folates reported to date has made the complete bench-to-bedside journey except [18F]AzaFol, which made it to patients with metastatic ovarian and lung cancers in a multicenter first-in-human trial. In the near future, however, we expect more clinical trials with folate-based PET radiopharmaceuticals given the increasing clinical interest in imaging and the treatment of FR-related malignancies.
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Høier-Madsen, Mimi, Jan Holm, and Steen I. Hansen. "α Isoforms of soluble and membrane-linked folate-binding protein in human blood." Bioscience Reports 28, no. 3 (June 1, 2008): 153–60. http://dx.doi.org/10.1042/bsr20070033.

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The high-affinity FBP/FR (folate-binding protein/folate receptor) is expressed in three isoforms. FRα and FRβ are attached to cell membranes by hydrophobic GPI (glycosylphosphatidylinositol) anchors, whereas FBPγ is a secretory protein. Mature neutrophil granulocytes contain a non-functional FRβ on the surface, and, in addition, nanomolar concentrations of a secretory functional FBP (29 kDa) can be present in the secondary granules. A statistically significant correlation between the concentrations of functional FBP, probably a γ isoform, in granulocytes and serum supported the hypothesis that serum FBP (29 kDa) mainly originates from neutrophils. The presence of FBP/FRα isoforms were established for the first time in human blood using antibodies specifically directed against human milk FBPα. The α isoforms identified on erythrocyte membranes, and in granulocytes and serum, only constituted an almost undetectable fraction of the functional FBP. The FBPα in neutrophil granulocytes was identified as a cytoplasmic component by indirect immunofluorescence. Gel filtration of serum revealed a peak of FBPα (>120 kDa), which could represent receptor fragments from decomposed erythrocytes and granulocytes. The soluble FBPs may exert bacteriostatic effects and protect folates in plasma from biological degradation, whereas FRs on the surface of blood cells could be involved in intracellular folate uptake or serve as signal proteins. The latter receptors have also been used for therapeutic targeting in malignancy.
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Scaranti, Mariana, Elena Cojocaru, Susana Banerjee, and Udai Banerji. "Exploiting the folate receptor α in oncology." Nature Reviews Clinical Oncology 17, no. 6 (March 9, 2020): 349–59. http://dx.doi.org/10.1038/s41571-020-0339-5.

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Bremer, Ryan E., Tatiana S. Scoggin, Elizabeth B. Somers, Daniel J. O'Shannessy, and David E. Tacha. "Interobserver Agreement and Assay Reproducibility of Folate Receptor α Expression in Lung Adenocarcinoma: A Prognostic Marker and Potential Therapeutic Target." Archives of Pathology & Laboratory Medicine 137, no. 12 (April 9, 2013): 1747–52. http://dx.doi.org/10.5858/arpa.2013-0039-oa.

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Context.—Lung cancer is the leading cause of cancer deaths in the United States and globally. Folate-targeted drugs are among the promising new targeted therapies for lung cancer, provided predictive biomarkers can be identified for optimal patient selection. Objective.—To evaluate the interobserver agreement and reproducibility of an immunohistochemistry assay for folate receptor α as a potential predictive marker for folate-targeted therapies. Design.—Immunohistochemistry using anti–folate receptor α antibody 26B3 was performed on formalin-fixed, paraffin-embedded tissues. The M-score, a semiquantitative measure of staining intensity and proportion of tumor cells staining, was determined for each specimen. Interobserver agreement was assessed using lung adenocarcinoma specimens stained at a single site and evaluated by 3 independent pathologists. Interinstrument reproducibility assessed 20 specimens stained by 3 different automated stainers. Interlaboratory agreement was determined on 5 specimens, repeatedly stained on each of 5 days, at 3 different study sites. Results.—Folate receptor α expression was identified in 39 of 54 cases of lung adenocarcinoma (72%) and 4 of 37 cases of lung squamous cell carcinoma (11%). Agreement among 3 pathologists was found in 24 of 26 cases (92%). Interinstrument reproducibility was observed in 19 of 20 cases (95%). Agreement among 3 laboratories was found for 49 of 50 specimens (98%). Conclusions.—Immunostaining of folate receptor α in lung adenocarcinomas is reproducible across staining platforms and among laboratories. Agreement among pathologists is achieved using a semiquantitative scoring method. An accurate and convenient method for determining folate receptor α expression offers a potentially invaluable tool for selecting patients for folate-targeted therapies.
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Bartouskova, Marie, Bohuslav Melichar, and Beatrice Mohelnikova-Duchonova. "Folate receptor: a potential target in ovarian cancer." Pteridines 26, no. 1 (March 1, 2015): 1–12. http://dx.doi.org/10.1515/pterid-2014-0013.

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AbstractOvarian cancer is the most frequent cause of gynecological cancer-related death. Unfortunately, many patients are diagnosed at an advanced stage and have a poor prognosis. The standard treatment for advanced disease involves maximal cytoreductive surgery and chemotherapy based on platinum compounds and taxanes. Patients presenting at an advanced stage have a higher risk of recurrence. The development of drug resistance currently represents a major obstacle in the systematic treatment and, therefore, the discovery of new anticancer agents and approaches should improve the poor prognosis of these patients. Folate receptor α is overexpressed in epithelial ovarian cancer (EOC), but has limited expression in nonmalignant human tissues. The degree of folate receptor expression corresponds with the stage and grade of the disease. Because of this, folate receptor α seems to be a potential therapeutic target for the treatment of ovarian cancer. Currently, several approaches have been studied to target this protein in ovarian cancer treatment. This review summarizes current knowledge about the potential usage of folate receptors as prognostic and predictive biomarkers as well as their role in the management and targeted therapy of ovarian cancer.
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Miotti, S., M. Bagnoli, A. Tomassetti, M. I. Colnaghi, and S. Canevari. "Interaction of folate receptor with signaling molecules lyn and G(alpha)(i-3) in detergent-resistant complexes from the ovary carcinoma cell line IGROV1." Journal of Cell Science 113, no. 2 (January 15, 2000): 349–57. http://dx.doi.org/10.1242/jcs.113.2.349.

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Using as a model the ovary carcinoma cell line IGROV1, we analyzed the partitioning of the glycosyl-phosphatidylinositol-anchored folate receptor into lipid rafts based on its relative detergent insolubility, with a focus on physically and functionally associated signaling molecules. A variable amount (40-60%) of folate receptor was found in low-density Triton X-100 insoluble complexes together with subunits of heterotrimeric G-proteins and the src-family non-receptor tyrosine kinases p53-56 lyn. In the same fraction the structural component of caveolae, caveolin, was not detected at the protein level, although the corresponding mRNA was detected in trace amounts. Comodulation of folate receptor and signalling molecules was observed in the detergent-insoluble complexes during cell proliferation or induced by phosphatidylinositol-specific phospholipase C treatment or by interaction with anti-folate receptor monoclonal antibodies. Moreover, complexes of folate receptor, lyn and the G(α)(i-3) subunit were immunoprecipitated using either anti-folate receptor or anti-lyn antibodies. In vitro kinase assay of the immunoprecipitates revealed stimulation of phosphorylation of common and specific proteins. In particular, the p53 form of lyn appeared to be enriched and phosphorylated in the anti-folate receptor MOv19 monoclonal antibody immunoprecipitate, whereas a 40 kDa band common to anti-folate receptor and anti-lyn immunoprecipitates was the phosphorylated form of the G(α)(i-3) subunit. These findings point to the functional interaction between folate receptor and associated signaling molecules.
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Nogueira, Eugénia, Marisa P. Sárria, Nuno G. Azoia, Egipto Antunes, Ana Loureiro, Diana Guimarães, Jennifer Noro, Alexandra Rollett, Georg Guebitz, and Artur Cavaco-Paulo. "Internalization of Methotrexate Conjugates by Folate Receptor-α." Biochemistry 57, no. 49 (November 19, 2018): 6780–86. http://dx.doi.org/10.1021/acs.biochem.8b00607.

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Cagle, Philip T., Qihui “Jim” Zhai, Linda Murphy, and Philip S. Low. "Folate Receptor in Adenocarcinoma and Squamous Cell Carcinoma of the Lung: Potential Target for Folate-Linked Therapeutic Agents." Archives of Pathology & Laboratory Medicine 137, no. 2 (February 1, 2013): 241–44. http://dx.doi.org/10.5858/arpa.2012-0176-oa.

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Context.— Lung cancer is the number one cause of cancer deaths in the United States and globally. The advent of targeted therapies has offered a new treatment paradigm for lung cancer, but currently validated and emerging drugs are effective in only a small minority of lung cancers, predominantly adenocarcinomas. Folate receptors can serve as targets for drugs attached to folate and are overexpressed in many cancers. Objective.— To determine the frequency of folate receptor overexpression in lung cancers of different cell types as potential targets for folate-linked therapy. Design.— High-density tissue microarrays were constructed from archival formalin-fixed, paraffin-embedded resection specimens from 188 primary stage I or stage II adenocarcinomas or squamous cell carcinomas of the lung with three 0.1-cm cores from each tumor. Tissue microarrays were immunostained for folate receptor α with mAb343 and the results scored (0 to 1+ = weak expression, 2+ to 3+ = strong expression). Results.— Eighty-four of 117 (72%) of the adenocarcinomas were strongly positive for the folate receptor, and 36 of 71 (51%) of the squamous cell carcinomas were strongly positive for the folate receptor. Conclusions.— Our data indicate that a large percentage of lung cancers, including squamous cell carcinomas in addition to adenocarcinomas, strongly express folate receptor. This suggests that folate-linked targeted therapy can potentially be used to treat the majority of lung cancers, both adenocarcinomas and, particularly, squamous cell carcinomas, that do not respond to current targeted therapies.
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Kim, Hye Won, Yun Jung Choi, Ki Nam Kim, Tsunenobu Tamura, and Namsoo Chang. "Effect of paternal folate deficiency on placental folate content and folate receptor α expression in rats." Nutrition Research and Practice 5, no. 2 (2011): 112. http://dx.doi.org/10.4162/nrp.2011.5.2.112.

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Samodelov, Sophia L., Zhibo Gai, Gerd A. Kullak-Ublick, and Michele Visentin. "Renal Reabsorption of Folates: Pharmacological and Toxicological Snapshots." Nutrients 11, no. 10 (October 2, 2019): 2353. http://dx.doi.org/10.3390/nu11102353.

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Folates are water-soluble B9 vitamins that serve as one-carbon donors in the de novo synthesis of thymidylate and purines, and in the conversion of homocysteine to methionine. Due to their key roles in nucleic acid synthesis and in DNA methylation, inhibiting the folate pathway is still one of the most efficient approaches for the treatment of several tumors. Methotrexate and pemetrexed are the most prescribed antifolates and are mainly used in the treatment of acute myeloid leukemia, osteosarcoma, and lung cancers. Normal levels of folates in the blood are maintained not only by proper dietary intake and intestinal absorption, but also by an efficient renal reabsorption that seems to be primarily mediated by the glycosylphosphatidylinositol- (GPI) anchored protein folate receptor α (FRα), which is highly expressed at the brush-border membrane of proximal tubule cells. Folate deficiency due to malnutrition, impaired intestinal absorption or increased urinary elimination is associated with severe hematological and neurological deficits. This review describes the role of the kidneys in folate homeostasis, the molecular basis of folate handling by the kidneys, and the use of high dose folic acid as a model of acute kidney injury. Finally, we provide an overview on the development of folate-based compounds and their possible therapeutic potential and toxicological ramifications.
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Dissertations / Theses on the topic "Folate receptor α"

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Sivakumaran, Suneethi. "Role of Androgen Receptor in Folate Receptor α Regulation and in Prostate Cancer." University of Toledo Health Science Campus / OhioLINK, 2012. http://rave.ohiolink.edu/etdc/view?acc_num=mco1345570201.

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AMBROSI, Emanuele. "Expression, purification and structural characterization of three human proteins: apolipoprotein M, heme-binding protein 2 and folate receptor α." Doctoral thesis, 2008. http://hdl.handle.net/11562/337640.

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In questo lavoro di tesi ci si è occupati dell’espressione, della purificazione e della cristallizzazione di tre proteine umane (l’apolipoproteina M, il recettore del folato α e la proteina SOUL) con lo scopo finale di determinarne la struttura tridimensionale mediante analisi di diffrazione di raggi X. L’apolipoproteina M umana è stata espressa utilizzando il lievito metilotrofico P. pastoris. La proteina ricombinante così ottenuta è stata purificata tramite cromatografia a scambio ionico, isoelettrofocalizzazione preparativa, gel filtrazione e cromatografia ad interazione idrofobica. Per ottenere una proteina più omogenea è stato espresso e purificato anche il mutante Asn135Gln, privo del sito di glicosilazione. Le prove di cristallizzazione hanno dato esito positivo con la proteina mutata, anche se i cristalli fino ad ora ottenuti non sono idonei per gli esperimenti di diffrazione di raggi X. L’espressione eterologa del recettore del folato umano ha dato parecchi problemi, nonostante siano stati provati diversi sistemi di espressione (P. pastoris, baculovirus e N. benthamiana). Solo una piccola quantità di proteina ricombinante è stata ottenuta (da P. pastoris) e purificata (mediante cromatografia a scambio ionico e gel filtrazione). Nessuna delle condizioni di cristallizzazione testata ha avuto successo, probabilmente a causa della bassa concentrazione della proteina utilizzata in tali prove. La proteina SOUL (heme-binding protein 2) è stata espressa in E. coli e purificata tramite cromatografia di affinità, sfruttando la coda di sei istidine aggiunta all’estremità C-terminale della proteina. La SOUL ricombinante è stata cristallizzata sia come apopoteina sia come oloproteina (complesso SOUL/emina). Gli studi preliminari di diffrazione di raggi X mostrano la presenza di sei molecole nella cella unitaria. Non è stata inoltre rilevata alcuna significativa differenza tra la forma apo- e la forma olo-. Ulteriori studi suggeriscono che l’emina non sia legata alla proteina, poiché il picco corrispondente al ferro non è stato trovato nello spettro di fluorescenza ai raggi X ottenuto dai cristalli. Al momento sono in corso i tentativi di risolverne la struttura tridimensionale per mezzo di sostituzione isomorfa multipla, multiwavelength anomalous diffraction e sostituzione molecolare.
This thesis work was aimed at the expression, purification and crystallization of three human proteins (apolipoprotein M, folate receptor α and SOUL protein) in order to determine their three-dimensional structure by means of X-ray protein crystallography. Human apolipoprotein M was expressed using the methylotrophic yeast P. pastoris. The recombinant protein was purified by ion-exchange chromatography, preparative isoelectric focusing, gel filtration, and Lipidex-1000 chromatography. In order to obtain a more homogeneous protein, the non-glycosylated mutant (Asn135Gln) was also expressed and purified. The crystallization trials gave some positive results with mutated apoM, although the crystals are still not suitable for X-ray diffraction experiments. The heterologous expression of the human FR-a was troublesome, and although different expression systems (P. pastoris, baculovirus, and N. benthamiana) were tested, only a low amount of recombinant protein was obtained (from P. pastoris) and purified (by ion-exchange chromatography and gel filtration). However non of the crystallization conditions tested was successful, probably due to the low protein concentration. Human SOUL (heme-binding protein 2) was expressed in E. coli and purified by immobilized metal ion affinity chromatography, using the hexa-histidine tag added to the C-terminus of the protein. The recombinant SOUL was crystallized both as apoprotein and as a complex in the presence of hemin. The preliminary X-ray diffraction analysis shows the presence of six molecules in the unit cell, and no significant differences between the apoand the holoprotein were found. Further studies suggest that hemin is not bound to the protein, since the Fe peak could not be found in the X-ray fluorescence spectrum of the crystals. Attempts to solve the three-dimensional structure by means of multiple isomorphous replacement, multiwavelength anomalous diffraction and molecular replacement are still in progress.
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Book chapters on the topic "Folate receptor α"

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Ng, Chau H. M., and Ann L. Jackman. "Potential for α-Folate Receptor-Targeted Treatment for Ovarian Cancer." In Emerging Therapeutic Targets in Ovarian Cancer, 245–58. New York, NY: Springer New York, 2010. http://dx.doi.org/10.1007/978-1-4419-7216-3_12.

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Mishra, Brahmeshwar, and Sathish Thokala. "Multifunctional Nanocarrier Systems for Effective Delivery of Drugs in Cancer Treatment." In Multifunctional Nanocarriers for Contemporary Healthcare Applications, 301–27. IGI Global, 2018. http://dx.doi.org/10.4018/978-1-5225-4781-5.ch011.

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The drug delivery to the cancer sites, with maintained effective drug concentration for longer duration, using low dose of drug, with minimum side effects is the prime concern of formulation scientist today. In the recent times, the nanocarrier systems are not only being utilized for achieving targeted, sustained and controlled release of drug to the disease site, but also are used in imaging of diseases. An attempt has been made through this chapter to give a brief outline about the cancer and elaborate details on the various multifunctional nanocarriers researched till date for effective delivery of drugs in cancer treatment. Further, functionalization and surface modification of nanocarrier with various ligands like folate, transferrin, TPGS (d-α- Tocopheryl Polyethylene Glycol 1000 Succinate), trastuzumab and hyaluronic acid etc., that have specific receptor in the proximity of disease site have been explained along with pros and cons of such carrier systems.
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Conference papers on the topic "Folate receptor α"

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O'Shannessy, Daniel J., Elizabeth B. Somers, Yao-Shi Fu, Robert Smale, Robert P. Thiel, and Nicholas C. Nicolaides. "Abstract 2516: Immunohistochemical characterization of a novel, highly sensitive monoclonal antibody to folate receptor α." In Proceedings: AACR 103rd Annual Meeting 2012‐‐ Mar 31‐Apr 4, 2012; Chicago, IL. American Association for Cancer Research, 2012. http://dx.doi.org/10.1158/1538-7445.am2012-2516.

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Yazaki, Shu, Yohei Chiba, Yuki Kojima, Hiroshi Yoshida, Shigemasa Takamizawa, Rui Kitadai, Ayumi Saito, et al. "2022-RA-629-ESGO Association of folate receptor α expression and tumor immune microenvironment in patients with cervical cancer." In ESGO 2022 Congress. BMJ Publishing Group Ltd, 2022. http://dx.doi.org/10.1136/ijgc-2022-esgo.39.

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Ng, Chau HM, Melanie Valenti, Ruth Ruddle, Florence Raynaud, Davinder S. Theti, Fraser Mitchell, and Ann L. Jackman. "Abstract 2544: Preclinical pharmacodynamics (PD) of ONX 0801, a folate receptor-α (FRα) and tumor-targeted thymidylate synthase (TS) inhibitor." In Proceedings: AACR 102nd Annual Meeting 2011‐‐ Apr 2‐6, 2011; Orlando, FL. American Association for Cancer Research, 2011. http://dx.doi.org/10.1158/1538-7445.am2011-2544.

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Ab, Olga, Laura M. Bartle, Xiuxia Sun, Rui Wu, Holly A. Johnson, Kathleen R. Whiteman, Alyssa LaBelle, and Victor S. Goldmacher. "Abstract 667: IMGN853, a folate receptor (FR) α-targeting antibody-drug conjugate (ADC), is highly effective against xenograft models with clinically relevant levels of receptor expression." In Proceedings: AACR Annual Meeting 2014; April 5-9, 2014; San Diego, CA. American Association for Cancer Research, 2014. http://dx.doi.org/10.1158/1538-7445.am2014-667.

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Fittall, Matthew W., Anthony Cheung, Gyula M. Petranyi, Diana Rodriguez-Dominguez, Heather J. Bax, Panagiotis Karagiannis, Kristina M. Ilieva, Andrew Tutt, and Sophia N. Karagiannis. "Abstract A090: Exploring folate receptor α immunotherapy of breast carcinomas: Human monocytic cell-mediated killing triggered by IgG1 and IgE antibodies." In Abstracts: CRI-CIMT-EATI-AACR Inaugural International Cancer Immunotherapy Conference: Translating Science into Survival; September 16-19, 2015; New York, NY. American Association for Cancer Research, 2016. http://dx.doi.org/10.1158/2326-6074.cricimteatiaacr15-a090.

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Qiu, Qifeng, Rui Wu, Leanne Lanieri, Erin Maloney, Anna Skaletskaya, Shan Jin, Lintao Wang, et al. "Abstract 71: Bystander activity andin vivoefficacy of a folate receptor α (FRα)-targeting antibody-drug conjugate with a novel peptide linker." In Proceedings: AACR Annual Meeting 2017; April 1-5, 2017; Washington, DC. American Association for Cancer Research, 2017. http://dx.doi.org/10.1158/1538-7445.am2017-71.

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Lu, Yingjuan, Theresa P. Johnson, Leroy W. Wheeler, Alex M. Lloyd, Vicky A. Cross, Elaine M. Westrick, Nikki L. Parker, and Christopher P. Leamon. "Abstract 3670: Treatment of epithelial ovarian cancer with folate receptor (α/β) targeted chemotherapy is enhanced by CTLA-4 blockade: Learning from animal models." In Proceedings: AACR Annual Meeting 2017; April 1-5, 2017; Washington, DC. American Association for Cancer Research, 2017. http://dx.doi.org/10.1158/1538-7445.am2017-3670.

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Cherian, Christina, Lei Wang, Adrianne Wallace, Steven Orr, Zhanjun Hou, Aleem Gangjee, and Larry H. Matherly. "Abstract 2706: Tumor-targeting with novel pyridyl 6-substituted pyrrolo[2,3-d]pyrimidine antifolates via cellular uptake by folate receptor (FR) α and the proton-coupled folate transporter (PCFT) and inhibition ofde novopurine nucleotide biosynthesis." In Proceedings: AACR Annual Meeting 2014; April 5-9, 2014; San Diego, CA. American Association for Cancer Research, 2014. http://dx.doi.org/10.1158/1538-7445.am2014-2706.

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Thirlway, Jenny, Adam Lodge, Andria Pelava, Daniel J. Williamson, Davide Carta, Majid Al Nakeeb, Justyna Mysliwy, Paul J. M. Jackson, David E. Thurston, and Robert J. Lutz. "Abstract C023: IKS01, a next generation antibody drug conjugate, shows target-dependent efficacy in a platinum-resistant tumor model with low levels of folate receptor α expression." In Abstracts: AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics; October 26-30, 2019; Boston, MA. American Association for Cancer Research, 2019. http://dx.doi.org/10.1158/1535-7163.targ-19-c023.

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Matherly, Larry H., Xin Zhang, Adrianne Wallace, Zhanjun Hou, Christina George, Xilin Zhou, and Aleem Gangjee. "Abstract 4481: Tumor-targeting with novel 6-substituted thienoyl[2,3-d]pyrimidine antifolates via cellular uptake by folate receptor α, and inhibition of de novopurine nucleotide biosynthesis." In Proceedings: AACR 106th Annual Meeting 2015; April 18-22, 2015; Philadelphia, PA. American Association for Cancer Research, 2015. http://dx.doi.org/10.1158/1538-7445.am2015-4481.

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