Target Information

Target General Infomation
Target ID
T83386
Former ID
TTDI01918
Target Name
Folate receptor alpha
Gene Name
FOLR1
Synonyms
Adult folatebinding protein; FBP; FRalpha; Folate receptor 1; Folate receptor, adult; KB cells FBP; Ovarian tumorassociated antigen MOv18; FOLR1
Target Type
Successful
Disease Acute malaria [ICD9: 84; ICD10: B50-B54]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Ovarian cancer [ICD9: 183; ICD10: C56]
Platinum-resistant ovarian cancer [ICD9: 140-229, 183; ICD10: C56]
Renal cancer [ICD9: 140-229, 189; ICD10: C64]
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48]
Function
Binds to folate and reduced folic acid derivatives and mediates delivery of 5-methyltetrahydrofolate and folate analogs into the interior of cells. Has high affinity for folate and folic acid analogs at neutral pH. Exposure to slightly acidic pHafter receptor endocytosis triggers a conformation change that strongly reduces its affinity for folates and mediates their release. Required for normal embryonic development and normal cell proliferation.
BioChemical Class
Folate receptor
UniProt ID
P15328
Sequence
MAQRMTTQLLLLLVWVAVVGEAQTRIAWARTELLNVCMNAKHHKEKPGPEDKLHEQCRPW
RKNACCSTNTSQEAHKDVSYLYRFNWNHCGEMAPACKRHFIQDTCLYECSPNLGPWIQQV
DQSWRKERVLNVPLCKEDCEQWWEDCRTSYTCKSNWHKGWNWTSGFNKCAVGAACQPFHF
YFPTPTVLCNEIWTHSYKVSNYSRGSGRCIQMWFDPAQGNPNEEVARFYAAAMSGAGPWA
AWPFLLSLALMLLWLLS
Drugs and Mode of Action
Drug(s) Pyrimethamine Drug Info Approved Acute malaria [468031], [536773]
EC20 Drug Info Phase 3 Ovarian cancer [547956]
Farletuzumab Drug Info Phase 3 Ovarian cancer [548173]
MK-8109 Drug Info Phase 3 Platinum-resistant ovarian cancer [549855]
EC-145 Drug Info Phase 2 Solid tumours [522073]
EC-17 Drug Info Phase 2 Renal cancer [523759]
BMS-753493 Drug Info Phase 1/2 Cancer [522150], [539707]
Talotrexin Drug Info Phase 1/2 Solid tumours [521643]
EC0489 Drug Info Phase 1 Solid tumours [522597]
IMGN-853 Drug Info Phase 1 Solid tumours [523926]
Modulator BMS-753493 Drug Info [533020]
EC-145 Drug Info [544306]
EC-17 Drug Info [530365]
EC0489 Drug Info [550438]
EC20 Drug Info [550882]
Farletuzumab Drug Info
MK-8109 Drug Info [544488]
Pyrimethamine Drug Info [556264]
Inhibitor IMGN-853 Drug Info [530499]
Antagonist Talotrexin Drug Info [544163]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Endocytosis
Reactome COPII (Coat Protein 2) Mediated Vesicle Transport
Cargo concentration in the ER
WikiPathways Folate Metabolism
References
Ref 468031(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4800).
Ref 521643ClinicalTrials.gov (NCT00112060) A Study to Assess the Safety and Preliminary Efficacy of PT-523 in Patients With Advanced Non-Small Cell Lung Cancer (NSCLC). U.S. National Institutes of Health.
Ref 522073ClinicalTrials.gov (NCT00507741) Study of Vintafolide (MK-8109, EC145) in Participants With Advanced Ovarian and Endometrial Cancers (MK-8109-007, EC-FV-02). U.S. National Institutes of Health.
Ref 522150ClinicalTrials.gov (NCT00550017) A Phase 1/2 Study of Epofolate (BMS-753493) in Subjects With Advanced Cancer (Schedule 2). U.S. National Institutes of Health.
Ref 522597ClinicalTrials.gov (NCT00852189) Study of EC0489 for the Treatment of Refractory or Metastatic Tumors. U.S. National Institutes of Health.
Ref 523759ClinicalTrials.gov (NCT01511055) Intra-op Detection of Occult Ovarian Carcinoma Using a Folate-Alpha Receptor Specific Fluorescent Ligand. U.S. National Institutes of Health.
Ref 523926ClinicalTrials.gov (NCT01609556) First-in-Human Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of IMGN853 in Adults With Ovarian Cancer and Other FOLR1-Positive Solid Tumors. U.S. National Institutes of Health.
Ref 536773How many modes of action should an antibiotic have? Curr Opin Pharmacol. 2008 Oct;8(5):564-73. Epub 2008 Jul 30.
Ref 539707(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2641).
Ref 547956Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020691)
Ref 548173Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022740)
Ref 549855Clinical pipeline report, company report or official report of Endocyte.
Ref 530365Responsiveness of the Effective Consumer Scale (EC-17). J Rheumatol. 2009 Sep;36(9):2087-91.
Ref 530499Tumor delivery and in vivo processing of disulfide-linked and thioether-linked antibody-maytansinoid conjugates. Bioconjug Chem. 2010 Jan;21(1):84-92.
Ref 533020A phase I pharmacokinetic and safety analysis of epothilone folate (BMS-753493), a folate receptor targeted chemotherapeutic agent in humans with advanced solid tumors. Invest New Drugs. 2015 Apr;33(2):321-31.
Ref 544163Cancer chemotherapy: targeting folic acid synthesis. Cancer Manag Res. 2010; 2: 293-301.
Ref 544306Significance of Folate Receptor alpha and Thymidylate Synthase Protein Expression in Patients with Non-Small Cell Lung Cancer treated with Pemetrexed. J Thorac Oncol. 2013 January; 8(1): 19-30.
Ref 544488A current review of folate receptor alpha as a potential tumor target in non-small-cell lung cancer. Drug Des Devel Ther. 2015; 9: 4989-4996.
Ref 550438National Cancer Institute Drug Dictionary (drug id 638649).
Ref 550882EP patent application no. 2822386, Folate receptor alpha binding ligands.
Ref 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.

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