Resistance mutation info of target

Target General Information
Target ID T11211
Target Name Androgen receptor (AR) Target Info
Gene Name AR
Species Homo sapiens
Uniprot ID ANDR_HUMAN
Sequence MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQ
QQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQ
SALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSAD
LKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELC
KAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAG
KSTEDTAEYSPFKGGYTKGLEGESLGCSGSAAAGSSGTLELPSTLSLYKSGALDEAAAYQ
SRDYYNFPLALAGPPPPPPPPHPHARIKLENPLDYGSAWAAAAAQCRYGDLASLHGAGAA
GPGSGSPSAAASSSWHTLFTAEEGQLYGPCGGGGGGGGGGGGGGGGGGGGGGGEAGAVAP
YGYTRPPQGLAGQESDFTAPDVWYPGGMVSRVPYPSPTCVKSEMGPWMDSYSGPYGDMRL
ETARDHVLPIDYYFPPQKTCLICGDEASGCHYGALTCGSCKVFFKRAAEGKQKYLCASRN
DCTIDKFRRKNCPSCRLRKCYEAGMTLGARKLKKLGNLKLQEEGEASSTTSPTEETTQKL
TVSHIEGYECQPIFLNVLEAIEPGVVCAGHDNNQPDSFAALLSSLNELGERQLVHVVKWA
KALPGFRNLHVDDQMAVIQYSWMGLMVFAMGWRSFTNVNSRMLYFAPDLVFNEYRMHKSR
MYSQCVRMRHLSQEFGWLQITPQEFLCMKALLLFSIIPVDGLKNQKFFDELRMNYIKELD
RIIACKRKNPTSCSRRFYQLTKLLDSVQPIARELHQFTFDLLIKSHMVSVDFPEMMAEII
SVQVPKILSGKVKPIYFHTQ [Homo sapiens]
Drug Resistance Mutation and Corresponding Drugs
Ref 536361Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20.
Ref 539888(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: 2863).
Ref 538297FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 075298.
Ref 541984(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: 6943).
Ref 527863Selective blockade of androgenic steroid synthesis by novel lyase inhibitors as a therapeutic strategy for treating metastatic prostate cancer. BJU Int. 2005 Dec;96(9):1241-6.
Ref 5317832011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
Ref 541843(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: 6745).
Ref 524719ClinicalTrials.gov (NCT02116582) A Study to Evaluate Enzalutamide After Abiraterone in Metastatic Castration-Resistant Prostate Cancer. U.S. National Institutes of Health.
Ref 541894(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: 6812).
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 529385Phase II study of the pure non-steroidal antiandrogen nilutamide in prostatic cancer. Italian Prostatic Cancer Project (PONCAP). Eur J Cancer. 1991;27(9):1100-4.
Ref 524437ClinicalTrials.gov (NCT01946204) A Study of ARN-509 in Men With Non-Metastatic Castration-Resistant Prostate Cancer. U.S. National Institutes of Health.
Ref 1572605The ChEMBL database in 2017.
Mutation Info Missense: F876L
Drugs
Drug Name Enzalutamide Drug Info [1559230]
Targeted Disease Prostate Cancer
Drug Name Antiandrogens Drug Info [556070]
Targeted Disease Prostate Cancer
Mutation Info Missense: F877L
Drugs
Drug Name Enzalutamide Drug Info [555952], [556050]
Targeted Disease Prostate Cancer
Drug Name Arn-509 Drug Info [555952]
Targeted Disease Prostate Cancer
Mutation Info Missense: L702H
Drugs
Drug Name Abiraterone Drug Info [556089]
Targeted Disease Prostate Cancer
Mutation Prevalence 3 out of 59 patients
Mutation Info Missense: Q641*
Drugs
Drug Name Flutamide Drug Info [555528]
Targeted Disease Prostate Cancer
Mutation Info Missense: T878A
Drugs
Drug Name Enzalutamide Drug Info [556050], [556134]
Targeted Disease Prostate Cancer
Mutation Prevalence 2 out of 62 patients
Drug Name Abiraterone Drug Info [556089]
Targeted Disease Prostate Cancer
Mutation Prevalence 4 out of 59 patients
Drug Name Flutamide Drug Info [555520], [555528], [555862]
Targeted Disease Prostate Cancer
Drug Name Androgen Drug Info [556050]
Targeted Disease Prostate Cancer
Mutation Prevalence 2 out of 62 patients
Mutation Info Missense: T878S
Drugs
Drug Name Flutamide Drug Info [556165]
Targeted Disease Prostate Cancer
Mutation Prevalence 1 out of 4 patients
Drug Name Abiraterone Drug Info [556089]
Targeted Disease Prostate Cancer
Mutation Info Missense: V716M
Drugs
Drug Name Flutamide Drug Info [555704]
Targeted Disease Prostate Cancer
Mutation Prevalence 3 out of 28 patients
Drug Name Androgen Drug Info [556178]
Targeted Disease Prostate Cancer
Mutation Info Missense: W741C
Drugs
Drug Name Bicalutamide Drug Info [556056]
Targeted Disease Prostate Cancer
Mutation Info Missense: W741L
Drugs
Drug Name Bicalutamide Drug Info [556056]
Targeted Disease Prostate Cancer
Reference
Ref 555520Androgen receptor mutations in androgen-independent prostate cancer: Cancer and Leukemia Group B Study 9663. J Clin Oncol. 2003 Jul 15;21(14):2673-8.
Ref 555528Constitutive activation of the androgen receptor by a point mutation in the hinge region: a new mechanism for androgen-independent growth in prostate cancer. Int J Cancer. 2004 Jan 1;108(1):152-7.
Ref 555704Treatment-dependent androgen receptor mutations in prostate cancer exploit multiple mechanisms to evade therapy. Cancer Res. 2009 May 15;69(10):4434-42. doi: 10.1158/0008-5472.CAN-08-3605. Epub 2009 Apr 14.
Ref 555862A mutation in the ligand binding domain of the androgen receptor of human LNCaP cells affects steroid binding characteristics and response to anti-androgens. Biochem Biophys Res Commun. 1990 Dec 14;173(2):534-40.
Ref 555952A clinically relevant androgen receptor mutation confers resistance to second-generation antiandrogens enzalutamide and ARN-509. Cancer Discov. 2013 Sep;3(9):1020-9. doi: 10.1158/2159-8290.CD-13-0226. Epub 2013 Jun 18.
Ref 556050Androgen Receptor Gene Aberrations in Circulating Cell-Free DNA: Biomarkers of Therapeutic Resistance in Castration-Resistant Prostate Cancer. Clin Cancer Res. 2015 May 15;21(10):2315-24. doi: 10.1158/1078-0432.CCR-14-2666. Epub 2015 Feb 23.
Ref 556056Progress in antiandrogen design targeting hormone binding pocket to circumvent mutation based resistance. Front Pharmacol. 2015 Mar 24;6:57. doi: 10.3389/fphar.2015.00057. eCollection 2015.
Ref 556070Discovery of ODM-201, a new-generation androgen receptor inhibitor targeting resistance mechanisms to androgen signaling-directed prostate cancer therapies. Sci Rep. 2015 Jul 3;5:12007. doi: 10.1038/srep12007.
Ref 556089Plasma AR and abiraterone-resistant prostate cancer. Sci Transl Med. 2015 Nov 4;7(312):312re10. doi: 10.1126/scitranslmed.aac9511.
Ref 556134Integrated Analysis of Multiple Biomarkers from Circulating Tumor Cells Enabled by Exclusion-Based Analyte Isolation. Clin Cancer Res. 2016 Jul 11. doi: 10.1158/1078-0432.CCR-16-1021. [Epub ahead of print]
Ref 556165Mutation of the androgen-receptor gene in metastatic androgen-independent prostate cancer. N Engl J Med. 1995 May 25;332(21):1393-8.
Ref 556178Mutant androgen receptor detected in an advanced-stage prostatic carcinoma is activated by adrenal androgens and progesterone. Mol Endocrinol. 1993 Dec;7(12):1541-50.
Ref 1559230An F876L mutation in androgen receptor confers genetic and phenotypic resistance to MDV3100 (enzalutamide).Cancer Discov.2013 Sep;3(9):1030-43.

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