General Information of the Drug (ID: M6APDG03390)
Name
GSK2849466
Status
Discontinued in Phase 1
TTD Drug ID
D03SHP
Target Gene(s) and Their Upstream m6A Regulator, Together with the Effect of Target Gene(s) in Drug Response
The target genes involved in drug-target interaction (such as drug-metabolizing enzymes, drug transporters and therapeutic targets) and drug-mediated cell death signaling (including modulating DNA damage and repair capacity, escaping from drug-induced apoptosis, autophagy, cellular metabolic reprogramming, oncogenic bypass signaling, cell microenvironment, cell stemness, etc.) could be regulated by m6A regulator(s) and affected their corresponding drug response. You can browse detailed information on drug-related target gene(s) mediated by m6A regulators.
Androgen receptor (AR)
ETS-related transcription factor Elf-3 (ELF3)
In total 1 mechanisms lead to this potential drug response
Response Summary Androgen receptor (AR) is a therapeutic target for GSK2849466. The ETS-related transcription factor Elf-3 (ELF3) has potential in affecting the response of GSK2849466 through regulating the expression of Androgen receptor (AR). [1], [2]
References
Ref 1 ELF3 is a repressor of androgen receptor action in prostate cancer cells. Oncogene. 2014 Feb 13;33(7):862-71. doi: 10.1038/onc.2013.15. Epub 2013 Feb 25.
Ref 2 Androgen antagonistic effect of estramustine phosphate (EMP) metabolites on wild-type and mutated androgen receptor. Biochem Pharmacol. 1998 May 1;55(9):1427-33. doi: 10.1016/s0006-2952(97)00657-6.