m6A-centered Drug Response Information

General Information of the Drug (ID: M6APDG02362)
Name
PD-0183812
Synonyms
PETCVZZPKYJZAU-UHFFFAOYSA-N; PD183812; AC1NS8PJ; CHEMBL139653; SCHEMBL5268115; BDBM6280; PD 0183812; N8 Pyrido[2,3-d]pyrimidin-7-one deriv 72; 8-{bicyclo[221]heptan-2-yl}-2-({4-[4-(3-hydroxypropyl)piperidin-1-yl]phenyl}amino)-7H,8H-pyrido[2,3-d]pyrimidin-7-one; 8-(3-bicyclo[221]heptanyl)-2-[4-[4-(3-hydroxypropyl)piperidin-1-yl]anilino]pyrido[2,3-d]pyrimidin-7-one; PD0183813
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Status
Terminated
Structure
Formula
C28H35N5O2
InChI
1S/C28H35N5O2/c34-15-1-2-19-11-13-32(14-12-19)24-8-6-23(7-9-24)30-28-29-18-22-5-10-26(35)33(27(22)31-28)25-17-20-3-4-21(25)16-20/h5-10,18-21,25,34H,1-4,11-17H2,(H,29,30,31)
InChIKey
PETCVZZPKYJZAU-UHFFFAOYSA-N
PubChem CID
5330258
TTD Drug ID
D0Z0KD
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.
Cyclin A2 (CCNA2)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Cyclin A2 (CCNA2) is a therapeutic target for PD-0183812. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of PD-0183812 through regulating the expression of Cyclin A2 (CCNA2). [1], [2]
YTH domain-containing family protein 2 (YTHDF2)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Cyclin A2 (CCNA2) is a therapeutic target for PD-0183812. The YTH domain-containing family protein 2 (YTHDF2) has potential in affecting the response of PD-0183812 through regulating the expression of Cyclin A2 (CCNA2). [1], [2]
Cyclin-dependent kinase 2 (CDK2)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Cyclin-dependent kinase 2 (CDK2) is a therapeutic target for PD-0183812. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of PD-0183812 through regulating the expression of Cyclin-dependent kinase 2 (CDK2). [1], [3]
YTH domain-containing family protein 1 (YTHDF1)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Cyclin-dependent kinase 2 (CDK2) is a therapeutic target for PD-0183812. The YTH domain-containing family protein 1 (YTHDF1) has potential in affecting the response of PD-0183812 through regulating the expression of Cyclin-dependent kinase 2 (CDK2). [3], [4]
YTH domain-containing family protein 2 (YTHDF2)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Cyclin-dependent kinase 2 (CDK2) is a therapeutic target for PD-0183812. The YTH domain-containing family protein 2 (YTHDF2) has potential in affecting the response of PD-0183812 through regulating the expression of Cyclin-dependent kinase 2 (CDK2). [1], [3]
Cyclin-dependent kinase 4 (CDK4)
Insulin-like growth factor 2 mRNA-binding protein 1 (IGF2BP1)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Cyclin-dependent kinase 4 (CDK4) is a therapeutic target for PD-0183812. The Insulin-like growth factor 2 mRNA-binding protein 1 (IGF2BP1) has potential in affecting the response of PD-0183812 through regulating the expression of Cyclin-dependent kinase 4 (CDK4). [5], [6]
Protein virilizer homolog (VIRMA)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Cyclin-dependent kinase 4 (CDK4) is a therapeutic target for PD-0183812. The Protein virilizer homolog (VIRMA) has potential in affecting the response of PD-0183812 through regulating the expression of Cyclin-dependent kinase 4 (CDK4). [5], [6]
YTH domain-containing family protein 1 (YTHDF1)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Cyclin-dependent kinase 4 (CDK4) is a therapeutic target for PD-0183812. The YTH domain-containing family protein 1 (YTHDF1) has potential in affecting the response of PD-0183812 through regulating the expression of Cyclin-dependent kinase 4 (CDK4). [4], [6]
Cyclin-dependent kinase 6 (CDK6)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Cyclin-dependent kinase 6 (CDK6) is a therapeutic target for PD-0183812. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of PD-0183812 through regulating the expression of Cyclin-dependent kinase 6 (CDK6). [3], [7]
Fibroblast growth factor receptor 4 (FGFR4)
Methyltransferase-like 14 (METTL14)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary Fibroblast growth factor receptor 4 (FGFR4) is a therapeutic target for PD-0183812. The Methyltransferase-like 14 (METTL14) has potential in affecting the response of PD-0183812 through regulating the expression of Fibroblast growth factor receptor 4 (FGFR4). [8], [9]
G1/S-specific cyclin-E1 (CCNE1)
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
 Regulator Info 
Response Summary G1/S-specific cyclin-E1 (CCNE1) is a therapeutic target for PD-0183812. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of PD-0183812 through regulating the expression of G1/S-specific cyclin-E1 (CCNE1). [10], [11]
References
Ref 1 FTO regulates adipogenesis by controlling cell cycle progression via m(6)A-YTHDF2 dependent mechanism. Biochim Biophys Acta Mol Cell Biol Lipids. 2018 Oct;1863(10):1323-1330. doi: 10.1016/j.bbalip.2018.08.008. Epub 2018 Aug 13.
Ref 2 Clinical pipeline report, company report or official report of Alnylam Pharmaceuticals.
Ref 3 What are next generation innovative therapeutic targets? Clues from genetic, structural, physicochemical, and systems profiles of successful targets. J Pharmacol Exp Ther. 2009 Jul;330(1):304-15. doi: 10.1124/jpet.108.149955. Epub 2009 Apr 8.
Ref 4 YTHDF1 links hypoxia adaptation and non-small cell lung cancer progression. Nat Commun. 2019 Oct 25;10(1):4892. doi: 10.1038/s41467-019-12801-6.
Ref 5 Identification of pathology-specific regulators of m(6)A RNA modification to optimize lung cancer management in the context of predictive, preventive, and personalized medicine. EPMA J. 2020 Jul 29;11(3):485-504. doi: 10.1007/s13167-020-00220-3. eCollection 2020 Sep.
Ref 6 Liposarcoma: molecular genetics and therapeutics. Sarcoma. 2011;2011:483154. doi: 10.1155/2011/483154. Epub 2010 Dec 27.
Ref 7 FTO promotes tumour proliferation in bladder cancer via the FTO/miR-576/CDK6 axis in an m6A-dependent manner. Cell Death Discov. 2021 Nov 1;7(1):329. doi: 10.1038/s41420-021-00724-5.
Ref 8 N6-methyladenosine regulated FGFR4 attenuates ferroptotic cell death in recalcitrant HER2-positive breast cancer. Nat Commun. 2022 May 13;13(1):2672. doi: 10.1038/s41467-022-30217-7.
Ref 9 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 10 Methyltransferase like 3 promotes colorectal cancer proliferation by stabilizing CCNE1 mRNA in an m6A-dependent manner. J Cell Mol Med. 2020 Mar;24(6):3521-3533. doi: 10.1111/jcmm.15042. Epub 2020 Feb 10.
Ref 11 US patent application no. 6,271,030, Antisense inhibition of C/EBP beta expression.