Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T76396
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| Former ID |
TTDR00229
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| Target Name |
Geranylgeranyltransferase I
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| Gene Name |
CDC43
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| Synonyms |
GGTase-I-beta; PGGT; RAS proteins geranylgeranyltransferase beta subunit; Type I protein geranyl-geranyltransferase beta subunit; CDC43
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| Target Type |
Clinical Trial
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| 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.
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| BioChemical Class |
Alkyl aryl transferase
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| UniProt ID | |||||
| EC Number |
EC 2.5.1.59
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| Sequence |
MCQATNGPSRVVTKKHRKFFERHLQLLPSSHQGHDVNRMAIIFYSISGLSIFDVNVSAKY
GDHLGWMRKHYIKTVLDDTENTVISGFVGSLVMNIPHATTINLPNTLFALLSMIMLRDYE YFETILDKRSLARFVSKCQRPDRGSFVSCLDYKTNCGSSVDSDDLRFCYIAVAILYICGC RSKEDFDEYIDTEKLLGYIMSQQCYNGAFGAHNEPHSGYTSCALSTLALLSSLEKLSDKF KEDTITWLLHRQVSSHGCMKFESELNASYDQSDDGGFQGRENKFADTCYAFWCLNSLHLL TKDWKMLCQTELVTNYLLDRTQKTLTGGFSKNDEEDADLYHSCLGSAALALIEGKFNGEL CIPQEIFNDFSKRCCF |
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| Drugs and Mode of Action | |||||
| Drug(s) | L-778123 | Drug Info | Phase 1 | Lymphoma | [1], [2] |
| GGTI-298 | Drug Info | Terminated | Discovery agent | [3] | |
| Inhibitor | GGTI-298 | Drug Info | [4] | ||
| J-109,390 | Drug Info | [5] | |||
| L-269,289 | Drug Info | [5] | |||
| Modulator | L-778123 | Drug Info | |||
| References | |||||
| REF 1 | ClinicalTrials.gov (NCT00003430) L-778,123 in Treating Patients With Recurrent or Refractory Solid Tumors. U.S. National Institutes of Health. | ||||
| REF 2 | A 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 3 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008012) | ||||
| REF 4 | The 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 5 | Geranylgeranyltransferase I of Candida albicans: null mutants or enzyme inhibitors produce unexpected phenotypes. J Bacteriol. 2000 Feb;182(3):704-13. | ||||
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