Target General Information
Target ID T11211
Target Name Androgen receptor (AR)
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 and Corresponding Resistance Mutations
Mutation Info Missense: F876L
Drugs
Drug Name Enzalutamide Drug Info [4]
Targeted Disease Prostate Cancer
Drug Name Antiandrogens Drug Info [12]
Mutation Info Missense: F877L
Drugs
Drug Name Enzalutamide Drug Info [1], [2]
Targeted Disease Prostate Cancer
Drug Name Arn-509 Drug Info [1]
Targeted Disease Prostate Cancer
Mutation Info Missense: L702H
Drugs
Drug Name Abiraterone Drug Info [5]
Targeted Disease Prostate Cancer
Mutation Prevalence 3 out of 59 patients
Mutation Info Missense: Q641*
Drugs
Drug Name Flutamide Drug Info [8]
Mutation Info Missense: T878A
Drugs
Drug Name Enzalutamide Drug Info [2], [3]
Targeted Disease Prostate Cancer
Mutation Prevalence 2 out of 62 patients
Drug Name Abiraterone Drug Info [5]
Targeted Disease Prostate Cancer
Mutation Prevalence 4 out of 59 patients
Drug Name Androgen Drug Info [2]
Targeted Disease Prostate Cancer
Mutation Prevalence 2 out of 62 patients
Drug Name Flutamide Drug Info [7], [8], [9]
Mutation Info Missense: T878S
Drugs
Drug Name Abiraterone Drug Info [5]
Targeted Disease Prostate Cancer
Drug Name Flutamide Drug Info [13]
Mutation Prevalence 1 out of 4 patients
Mutation Info Missense: V716M
Drugs
Drug Name Androgen Drug Info [6]
Targeted Disease Prostate Cancer
Drug Name Flutamide Drug Info [10]
Mutation Prevalence 3 out of 28 patients
Mutation Info Missense: W741C
Drugs
Drug Name Bicalutamide Drug Info [11]
Mutation Info Missense: W741L
Drugs
Drug Name Bicalutamide Drug Info [11]
References
REF 1 A clinically relevant androgen receptor mutation confers resistance to second-generation antiandrogens enzalutamide and ARN-509. Cancer Discov. 2013 Sep;3(9):1020-9.
REF 2 Androgen 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.
REF 3 Integrated Analysis of Multiple Biomarkers from Circulating Tumor Cells Enabled by Exclusion-Based Analyte Isolation. Clin Cancer Res. 2017 Feb;23(3):746-756.
REF 4 An F876L mutation in androgen receptor confers genetic and phenotypic resistance to MDV3100 (enzalutamide).Cancer Discov.2013 Sep;3(9):1030-43.
REF 5 Plasma AR and abiraterone-resistant prostate cancer. Sci Transl Med. 2015 Nov 4;7(312):312re10.
REF 6 Mutant 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 7 Androgen 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 8 Constitutive 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 9 A 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 10 Treatment-dependent androgen receptor mutations in prostate cancer exploit multiple mechanisms to evade therapy. Cancer Res. 2009 May 15;69(10):4434-42.
REF 11 Progress in antiandrogen design targeting hormone binding pocket to circumvent mutation based resistance. Front Pharmacol. 2015 Mar 24;6:57.
REF 12 Discovery 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.
REF 13 Mutation of the androgen-receptor gene in metastatic androgen-independent prostate cancer. N Engl J Med. 1995 May 25;332(21):1393-8.

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