m6A-centered Drug Response Information

General Information of the Drug (ID: M6APDG00318)
Name
PHA-739358
Synonyms
Danusertib; PHA 739358; Danusertib, PHA-739358; (R)-N-(5-(2-methoxy-2-phenylacetyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)-4-(4-methylpiperazin-1-yl)benzamide; 5-Amido-pyrrolopyrazole 9d
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Status
Phase 2
Structure
Formula
C26H30N6O3
InChI
1S/C26H30N6O3/c1-30-12-14-31(15-13-30)20-10-8-19(9-11-20)25(33)27-24-21-16-32(17-22(21)28-29-24)26(34)23(35-2)18-6-4-3-5-7-18/h3-11,23H,12-17H2,1-2H3,(H2,27,28,29,33)/t23-/m1/s1
InChIKey
XKFTZKGMDDZMJI-HSZRJFAPSA-N
PubChem CID
11442891
TTD Drug ID
D02RJY
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 2 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Aurora kinase B (AURKB) is a therapeutic target for PHA-739358. The RNA demethylase ALKBH5 (ALKBH5) has potential in affecting the response of PHA-739358 through regulating the expression of Aurora kinase B (AURKB). [1], [2]
Aurora kinase B (AURKB) is a therapeutic target for PHA-739358. The RNA demethylase ALKBH5 (ALKBH5) has potential in affecting the response of PHA-739358 through regulating the expression of Aurora kinase B (AURKB). [1], [3]
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 A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
Ref 3 A phase I dose escalation study with anti-CD44v6 bivatuzumab mertansine in patients with incurable squamous cell carcinoma of the head and neck or esophagus. Clin Cancer Res. 2006 Oct 15;12(20 Pt 1):6064-72. doi: 10.1158/1078-0432.CCR-06-0910.