TTD Target ID: TTDR00786

Target Information
Name	G1/S-specific cyclin E1
Type of target	Research target
Synonyms	Cyclin E
	G1/S-specific cyclin E
Disease	Hepatocellular carcinoma    [1]
Pathway	Cell cycle
	Pathways in cancer
	Prostate cancer
	Small cell lung cancer
	p53 signaling pathway
UniProt ID	P24864
PDB Structure	1W98.
Function	Essential for the control of the cell cycle at the g1/s (start) transition.
Sequence	MPRERRERDAKERDTMKEDGGAEFSARSRKRKANVTVFLQDPDEEMAKIDRTARDQCGSQ PWDNNAVCADPCSLIPTPDKEDDDRVYPNSTCKPRIIAPSRGSPLPVLSWANREEVWKIM LNKEKTYLRDQHFLEQHPLLQPKMRAILLDWLMEVCEVYKLHRETFYLAQDFFDRYMATQ ENVVKTLLQLIGISSLFIAAKLEEIYPPKLHQFAYVTDGACSGDEILTMELMIMKALKWR LSPLTIVSWLNVYMQVAYLNDLHEVLLPQYPQQIFIQIAELLDLCVLDVDCLEFPYGILA ASALYHFSSSELMQKVSGYQWCDIENCVKWMVPFAMVIRETGSSKLKHFRGVADEDAHNI QTHRDSLDLLDKARAKKAMLSEQNRASPLPSGLLTPPQSGKKQSSGPEMA
Target Validation	Click to Find Target Validation Information.
Inhibitor	(2'Z,3'E)-5-Chloro-5'-chloro-indirubin-3'-oxime		[2]
	(2'Z,3'E)-5-Chloro-5'-fluoro-indirubin-3'-oxime		[2]
	(2'Z,3'E)-5-Chloro-5'-hydroxy-indirubin-3'-oxime		[2]
	(2'Z,3'E)-5-Chloro-5'-methyl-indirubin-3'-oxime		[2]
	(2'Z,3'E)-5-Fluoro-5'-chloro-indirubin-3'-oxime		[2]
	(2'Z,3'E)-5-Fluoro-5'-fluoro-indirubin-3'-oxime		[2]
	(2'Z,3'E)-5-Fluoro-5'-hydroxy-indirubin-3'-oxime		[2]
	(2'Z,3'E)-5-Fluoro-5'-methoxy-indirubin-3'-oxime		[2]
	(2'Z,3'E)-5-Fluoro-5'-methyl-indirubin-3'-oxime		[2]
	(2'Z,3'E)-5-Nitro-5'-chloro-indirubin-3'-oxime		[2]
	(2'Z,3'E)-5-Nitro-5'-fluoro-indirubin-3'-oxime		[2]
	(2'Z,3'E)-5-Nitro-5'-hydroxy-indirubin-3'-oxime		[2]
	(2'Z,3'E)-5-Nitro-5'-methoxy-indirubin-3'-oxime		[2]
	(2'Z,3'E)-5-Nitro-5'-methyl-indirubin-3'-oxime		[2]
	2- (		[3]
	3,4-di- (4-methoxyphenyl)-1H-pyrrole-2,5-dione		[4]
	3,4-diphenyl-1H-pyrrole-2,5-dione		[4]
	3- (		[3]
	3- (4-methoxyphenyl)-4-phenyl-1H-pyrrole-2,5-dione		[4]
	3- (indole-3-yl)-4-phenyl-1H-pyrrole-2,5-dione		[4]
	4- (7-Butyl-5H-pyrrolo[2,3-b]pyrazin-6-yl)-phenol		[5]
	4-[ (3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol		[3]
	5-nitroindirubin-3'-oxime		[2]
	BMS-536924		[6]
	PD-0183812		[7]
Cross References	3D Structure Related Literature On-Line Medical Dictionary
Ref 1	Use of RNA interference to target cyclin E-overexpressing hepatocellular carcinoma. Cancer Res. 2003 Jul 1;63(13):3593-7. To Reference
Ref 2	J Med Chem. 2010 May 13;53(9):3696-706.5,5'-substituted indirubin-3'-oxime derivatives as potent cyclin-dependent kinase inhibitors with anticancer activity. To Reference
Ref 3	J Med Chem. 2006 Nov 2;49(22):6500-9.4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. To Reference
Ref 4	J Med Chem. 2006 Feb 23;49(4):1271-81.Design, synthesis, and biological evaluation of 3,4-diarylmaleimides as angiogenesis inhibitors. To Reference
Ref 5	J Med Chem. 2003 Jan 16;46(2):222-36.Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects. To Reference
Ref 6	J Med Chem. 2005 Sep 8;48(18):5639-43.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 antitumor activity. To Reference
Ref 7	J Med Chem. 2000 Nov 30;43(24):4606-16.Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases. To Reference

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Professor in Department of Pharmacy
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