Target Information

Target General Infomation
Target ID
T36056
Former ID
TTDR01070
Target Name
Geranylgeranyl transferase type I beta subunit
Gene Name
PGGT1B
Synonyms
GGTase-I-beta; Type I protein geranyl-geranyltransferase beta subunit; PGGT1B
Target Type
Discontinued
Disease Cancer [ICD9: 140-229; ICD10: C00-C96]
Function
Catalyzes the transfer of a geranyl-geranyl moiety from geranyl-geranyl pyrophosphate to a cysteine at the fourth position from the c-terminus of proteins having the c-terminal sequence cys-aliphatic-aliphatic-x. Acts on the rac1, rac2, rap1a and rap1b.
BioChemical Class
Alkyl aryl transferase
Target Validation
T36056
UniProt ID
P53609
EC Number
EC 2.5.1.59
Sequence
MAATEDERLAGSGEGERLDFLRDRHVRFFQRCLQVLPERYSSLETSRLTIAFFALSGLDM
LDSLDVVNKDDIIEWIYSLQVLPTEDRSNLNRCGFRGSSYLGIPFNPSKAPGTAHPYDSG
HIAMTYTGLSCLVILGDDLSRVNKEACLAGLRALQLEDGSFCAVPEGSENDMRFVYCASC
ICYMLNNWSGMDMKKAITYIRRSMSYDNGLAQGAGLESHGGSTFCGIASLCLMGKLEEVF
SEKELNRIKRWCIMRQQNGYHGRPNKPVDTCYSFWVGATLKLLKIFQYTNFEKNRNYILS
TQDRLVGGFAKWPDSHPDALHAYFGICGLSLMEESGICKVHPALNVSTRTSERLLDLHQS
WKTKDSKQCSENVHIST
Drugs and Mode of Action
Drug(s) L-745631 Drug Info Terminated Cancer [546335]
Inhibitor A-313326 Drug Info [527321]
L-745631 Drug Info [534466]
PD-83176 Drug Info [534307]
References
Ref 546335Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007537)
Ref 527321Bioorg Med Chem Lett. 2005 Jan 3;15(1):153-8.Design and synthesis of o-trifluoromethylbiphenyl substituted 2-amino-nicotinonitriles as inhibitors of farnesyltransferase.
Ref 534307J Med Chem. 1997 Jan 17;40(2):192-200.Structure-activity relationships of cysteine-lacking pentapeptide derivatives that inhibit ras farnesyltransferase.
Ref 534466J Med Chem. 1997 Sep 12;40(19):2971-90.Ras farnesyltransferase: a new therapeutic target.

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