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Literature DB >> 25450772

Farnesyltransferase and geranylgeranyltransferase I: structures, mechanism, inhibitors and molecular modeling.

Mingyun Shen¹, Peichen Pan¹, Youyong Li², Dan Li³, Huidong Yu⁴, Tingjun Hou⁵.

Abstract

Farnesyltransferase (FTase) and geranylgeranyltransferase type I (GGTase-I) have crucial roles in the post-translational modifications of Ras proteins and, therefore, they are promising therapeutic targets for the treatment of various Ras-induced cancers and several other kinds of diseases. In this review, we provide an overview of the structures and biological functions of FTase and GGTase-I. Then, we summarize the typical inhibitors of FTase and GGTase-I, and highlight the drug candidates in clinical trials. In addition, we survey some recent advances in computer-aided drug design (CADD) and molecular modeling studies of FTase and GGTase-I.

Entities: Disease

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Year: 2014 PMID： 25450772 DOI： 10.1016/j.drudis.2014.10.002

Source DB: PubMed Journal: Drug Discov Today ISSN： 1359-6446 Impact factor: 7.851

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Cited

17 in total

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4. [Effects of geranylgeranyltransferaseⅠsilencing on the proliferation of tongue squamous cancer cells].

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Journal: Proc Natl Acad Sci U S A Date: 2017-02-21 Impact factor: 11.205

Farnesyltransferase and geranylgeranyltransferase I: structures, mechanism, inhibitors and molecular modeling.

Review 1. Targeting Metalloenzymes for Therapeutic Intervention.

2. Novel p21-Activated Kinase 4 (PAK4) Allosteric Modulators Overcome Drug Resistance and Stemness in Pancreatic Ductal Adenocarcinoma.

Review 3. All about that fat: Lipid modification of proteins in Cryptococcus neoformans.

4. [Effects of geranylgeranyltransferaseⅠsilencing on the proliferation of tongue squamous cancer cells].

Review 5. Developing effective combination therapy for pancreatic cancer: An overview.

6. Generalized myoclonic epilepsy with photosensitivity in juvenile dogs caused by a defective DIRAS family GTPase 1.

Review 7. Targeting prenylation inhibition through the mevalonate pathway.

Review 8. Regulation of Small GTPase Prenylation in the Nervous System.

9. A Farnesyltransferase Acts to Inhibit Ectopic Neurite Formation in C. elegans.

Review 10. Mechanisms of Chromosome Congression during Mitosis.