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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