Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTCEJ4F)

• DTT Name: G1/S-specific cyclin-E1 (CCNE1)
• Synonyms: G1/S-specific cyclin E; Cyclin E; CCNE
• Gene Name: CCNE1
• DTT Type: Literature-reported target; [1]
• UniProt ID: CCNE1_HUMAN
• TTD ID: T10052
• Sequence:
  MPRERRERDAKERDTMKEDGGAEFSARSRKRKANVTVFLQDPDEEMAKIDRTARDQCGSQ
  PWDNNAVCADPCSLIPTPDKEDDDRVYPNSTCKPRIIAPSRGSPLPVLSWANREEVWKIM
  LNKEKTYLRDQHFLEQHPLLQPKMRAILLDWLMEVCEVYKLHRETFYLAQDFFDRYMATQ
  ENVVKTLLQLIGISSLFIAAKLEEIYPPKLHQFAYVTDGACSGDEILTMELMIMKALKWR
  LSPLTIVSWLNVYMQVAYLNDLHEVLLPQYPQQIFIQIAELLDLCVLDVDCLEFPYGILA
  ASALYHFSSSELMQKVSGYQWCDIENCVKWMVPFAMVIRETGSSKLKHFRGVADEDAHNI
  QTHRDSLDLLDKARAKKAMLSEQNRASPLPSGLLTPPQSGKKQSSGPEMA
• Function: Essential for the control of the cell cycle at the G1/S (start) transition.
• KEGG Pathway:
  Cell cycle (hsa04110)
  Oocyte meiosis (hsa04114)
  p53 signaling pathway (hsa04115)
  PI3K-Akt signaling pathway (hsa04151)
  Hepatitis B (hsa05161)
  Measles (hsa05162)
  Pathways in cancer (hsa05200)
  Viral carcinogenesis (hsa05203)
  MicroRNAs in cancer (hsa05206)
  Prostate cancer (hsa05215)
  Small cell lung cancer (hsa05222)
• Reactome Pathway:
  G0 and Early G1 (R-HSA-1538133)
  SCF(Skp2)-mediated degradation of p27/p21 (R-HSA-187577)
  DNA Damage/Telomere Stress Induced Senescence (R-HSA-2559586)
  Cyclin E associated events during G1/S transition (R-HSA-69202)
  G1/S-Specific Transcription (R-HSA-69205)
  p53-Dependent G1 DNA Damage Response (R-HSA-69563)
  E2F mediated regulation of DNA replication (R-HSA-113510)

Molecular Interaction Atlas (MIA) of This DTT

1 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PD-0183812	DMWYP86	Retinoblastoma	2D02.2	Terminated	[1]

24 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(2'Z,3'E)-5-Chloro-5'-chloro-indirubin-3'-oxime	DMGXRSZ	Discovery agent	N.A.	Investigative	[2]
(2'Z,3'E)-5-Chloro-5'-fluoro-indirubin-3'-oxime	DM6AUHR	Discovery agent	N.A.	Investigative	[2]
(2'Z,3'E)-5-Chloro-5'-hydroxy-indirubin-3'-oxime	DMD7WGM	Discovery agent	N.A.	Investigative	[2]
(2'Z,3'E)-5-Chloro-5'-methyl-indirubin-3'-oxime	DMZ0V6G	Discovery agent	N.A.	Investigative	[2]
(2'Z,3'E)-5-Fluoro-5'-chloro-indirubin-3'-oxime	DMO7RFL	Discovery agent	N.A.	Investigative	[2]
(2'Z,3'E)-5-Fluoro-5'-fluoro-indirubin-3'-oxime	DMJ4ABD	Discovery agent	N.A.	Investigative	[2]
(2'Z,3'E)-5-Fluoro-5'-hydroxy-indirubin-3'-oxime	DM9LQH1	Discovery agent	N.A.	Investigative	[2]
(2'Z,3'E)-5-Fluoro-5'-methoxy-indirubin-3'-oxime	DMQDH3N	Discovery agent	N.A.	Investigative	[2]
(2'Z,3'E)-5-Fluoro-5'-methyl-indirubin-3'-oxime	DMAS3JC	Discovery agent	N.A.	Investigative	[2]
(2'Z,3'E)-5-Nitro-5'-chloro-indirubin-3'-oxime	DMYLX0U	Discovery agent	N.A.	Investigative	[2]
(2'Z,3'E)-5-Nitro-5'-fluoro-indirubin-3'-oxime	DMXZ2UC	Discovery agent	N.A.	Investigative	[2]
(2'Z,3'E)-5-Nitro-5'-hydroxy-indirubin-3'-oxime	DM0S82C	Discovery agent	N.A.	Investigative	[2]
(2'Z,3'E)-5-Nitro-5'-methoxy-indirubin-3'-oxime	DMLOIUK	Discovery agent	N.A.	Investigative	[2]
(2'Z,3'E)-5-Nitro-5'-methyl-indirubin-3'-oxime	DM6BA5L	Discovery agent	N.A.	Investigative	[2]
2-((3,5-diamino-1H-pyrazol-4-yl)diazenyl)phenol	DM1BI65	Discovery agent	N.A.	Investigative	[3]
3,4-di-(4-methoxyphenyl)-1H-pyrrole-2,5-dione	DMDO175	Discovery agent	N.A.	Investigative	[4]
3,4-diphenyl-1H-pyrrole-2,5-dione	DMPK6YT	Discovery agent	N.A.	Investigative	[4]
3-((3,5-diamino-1H-pyrazol-4-yl)diazenyl)phenol	DMJZK40	Discovery agent	N.A.	Investigative	[3]
3-(4-methoxyphenyl)-4-phenyl-1H-pyrrole-2,5-dione	DMGC7RY	Discovery agent	N.A.	Investigative	[4]
3-(indole-3-yl)-4-phenyl-1H-pyrrole-2,5-dione	DM3EV9N	Discovery agent	N.A.	Investigative	[4]
4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol	DMSKJ1X	Discovery agent	N.A.	Investigative	[3]
5-nitroindirubin-3'-oxime	DM4K8N2	Discovery agent	N.A.	Investigative	[2]
aloisine A	DM5U1LN	Discovery agent	N.A.	Investigative	[5]
BMS-536924	DMXJB4N	Discovery agent	N.A.	Investigative	[6]

References

• [1] Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases. J Med Chem. 2000 Nov 30;43(24):4606-16.
• [2] 5,5'-substituted indirubin-3'-oxime derivatives as potent cyclin-dependent kinase inhibitors with anticancer activity. J Med Chem. 2010 May 13;53(9):3696-706.
• [3] 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. J Med Chem. 2006 Nov 2;49(22):6500-9.
• [4] Design, synthesis, and biological evaluation of 3,4-diarylmaleimides as angiogenesis inhibitors. J Med Chem. 2006 Feb 23;49(4):1271-81.
• [5] Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects. J Med Chem. 2003 Jan 16;46(2):222-36.
• [6] Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitum... J Med Chem. 2005 Sep 8;48(18):5639-43.