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Table 3 The response of CRPC-associated AR mutations to anti-androgen treatments

From: Functional analysis of androgen receptor mutations that confer anti-androgen resistance identified in circulating cell-free DNA from prostate cancer patients

AR mutants

Agonist response to treatment

Hydroxyflutamide

Bicalutamide

Enzalutamide

ARN509

L702H

Partial

Partial

No

No

V716M

Partial

Partial

No

No

V731M

Partial

Partial

No

No

W742L

Partial

Yes

No

No

W742C

Partial

Yes

No

No

H875Y

Yes

Partial

Partial

Partial

H875Q

Partial

Partial

No

No

F877L

Partial

No

Partial

partial

T878A

Partial

Yes

Partial

partial

T878S

Partial

Yes

Partial

partial

D880E

Partial

Partial

No

No

L882I

Partial

Partial

No

No

S889G

Yes

Yes

No

No

D891H

Yes

Yes

No

No

E894K

Partial

Partial

No

No

M896V

Partial

Yes

No

No

M896T

Partial

Yes

No

No

E898G

Partial

No

No

No

T919S

Partial

Partial

No

No

H875Q/T919S

Partial

Partial

No

No

T878A/S889G

Yes

Yes

Partial

Partial

T878A/D891H

Yes

Yes

Partial

No

F877L/ T878A

No

Yes

Yes

Yes

H875Y/T878A

Yes

Yes

Partial

Partial

  1. Results presented in Additional file 4: Table S2 are summarized here. We considered as partial agonist a drug that inhibited a mutant at low concentrations and stimulated its activity at high concentrations