General Information of the Drug (ID: M6APDG03325)
Name
AZD-1152-HQPA
Synonyms
Barasertib
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Status
Phase 1
Structure
Formula
C26H30FN7O3
InChI
1S/C26H30FN7O3/c1-2-34(10-11-35)9-4-12-37-21-7-8-22-23(16-21)28-17-29-26(22)31-24-14-20(32-33-24)15-25(36)30-19-6-3-5-18(27)13-19/h3,5-8,13-14,16-17,35H,2,4,9-12,15H2,1H3,(H,30,36)(H2,28,29,31,32,33)
InChIKey
QYZOGCMHVIGURT-UHFFFAOYSA-N
PubChem CID
16007391
TTD Drug ID
D0Q7RE
VARIDT Drug ID
DR01712
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.
Aurora kinase B (AURKB)
RNA demethylase ALKBH5 (ALKBH5)
In total 1 mechanisms lead to this potential drug response
Response Summary Aurora kinase B (AURKB) is a therapeutic target for AZD-1152-HQPA. The RNA demethylase ALKBH5 (ALKBH5) has potential in affecting the response of AZD-1152-HQPA through regulating the expression of Aurora kinase B (AURKB). [1], [2]
Breast cancer resistance protein (ABCG2)
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Breast cancer resistance protein (ABCG2) is a therapeutic target for AZD-1152-HQPA. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of AZD-1152-HQPA through regulating the expression of Breast cancer resistance protein (ABCG2). [3], [4]
References
Ref 1 ALKBH5 promotes the proliferation of renal cell carcinoma by regulating AURKB expression in an m(6)A-dependent manner. Ann Transl Med. 2020 May;8(10):646. doi: 10.21037/atm-20-3079.
Ref 2 Clinical pipeline report, company report or official report of Cyclacel.
Ref 3 METTL3 promotes adriamycin resistance in MCF-7 breast cancer cells by accelerating pri-microRNA-221-3p maturation in a m6A-dependent manner. Exp Mol Med. 2021 Jan;53(1):91-102. doi: 10.1038/s12276-020-00510-w. Epub 2021 Jan 8.
Ref 4 P-glycoprotein and breast cancer resistance protein in acute myeloid leukaemia cells treated with the aurora-B kinase inhibitor barasertib-hQPA. BMC Cancer. 2011 Jun 16;11:254.