Target General Infomation
Target ID
T76396
Former ID
TTDR00229
Target Name
Geranylgeranyltransferase I
Gene Name
CDC43
Synonyms
GGTase-I-beta; PGGT; RAS proteins geranylgeranyltransferase beta subunit; Type I protein geranyl-geranyltransferase beta subunit; CDC43
Target Type
Clinical Trial
Disease Lymphoma [ICD9: 202.8, 208.9; ICD10: C81-C86]
Function
Catalyzes the transfer of a geranyl-geranyl moietyfrom geranyl-geranyl pyrophosphate to proteins having the C-terminal sequence Cys-Ile-Ile-Leu or Cys-Val-Leu-Leu. Acts, among other substrates, on Rho1 and Rho2 and CDC42 proteins. Participates in a RAS-like C-terminal modification of proteins involved in nuclear division and bud growth. It is involved in bud positioning and cell polarity.
BioChemical Class
Alkyl aryl transferase
UniProt ID
EC Number
EC 2.5.1.59
Sequence
MCQATNGPSRVVTKKHRKFFERHLQLLPSSHQGHDVNRMAIIFYSISGLSIFDVNVSAKY
GDHLGWMRKHYIKTVLDDTENTVISGFVGSLVMNIPHATTINLPNTLFALLSMIMLRDYE
YFETILDKRSLARFVSKCQRPDRGSFVSCLDYKTNCGSSVDSDDLRFCYIAVAILYICGC
RSKEDFDEYIDTEKLLGYIMSQQCYNGAFGAHNEPHSGYTSCALSTLALLSSLEKLSDKF
KEDTITWLLHRQVSSHGCMKFESELNASYDQSDDGGFQGRENKFADTCYAFWCLNSLHLL
TKDWKMLCQTELVTNYLLDRTQKTLTGGFSKNDEEDADLYHSCLGSAALALIEGKFNGEL
CIPQEIFNDFSKRCCF
Drugs and Mode of Action
Drug(s) L-778123 Drug Info Phase 1 Lymphoma [521452], [527183]
GGTI-298 Drug Info Terminated Discovery agent [546421]
Inhibitor GGTI-298 Drug Info [538058]
J-109,390 Drug Info [534950]
L-269,289 Drug Info [534950]
Modulator L-778123 Drug Info
References
Ref 521452ClinicalTrials.gov (NCT00003430) L-778,123 in Treating Patients With Recurrent or Refractory Solid Tumors. U.S. National Institutes of Health.
Ref 527183A phase I trial of the dual farnesyltransferase and geranylgeranyltransferase inhibitor L-778,123 and radiotherapy for locally advanced pancreatic cancer. Clin Cancer Res. 2004 Aug 15;10(16):5447-54.
Ref 546421Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008012)
Ref 534950Geranylgeranyltransferase I of Candida albicans: null mutants or enzyme inhibitors produce unexpected phenotypes. J Bacteriol. 2000 Feb;182(3):704-13.
Ref 538058The geranylgeranyltransferase-I inhibitor GGTI-298 arrests human tumor cells in G0/G1 and induces p21(WAF1/CIP1/SDI1) in a p53-independent manner. J Biol Chem. 1997 Oct 24;272(43):27224-9.
Ref 1587926URL: https://www.ebi.ac.uk/chembl/ The ChEMBL database in 2017

If you find any error in data or bug in web service, please kindly report it to Dr. Wang and Dr. Li.