Search results for "Geranylgeranyl Transferase"
showing 3 items of 3 documents
Identification of the Privileged Position in the Imidazo[1,2-a]pyridine Ring of Phosphonocarboxylates for Development of Rab Geranylgeranyl Transfera…
2017
Members of the Rab GTPase family are master regulators of vesicle trafficking. When disregulated, they are associated with a number of pathological states. The inhibition of RGGT, an enzyme responsible for post-translational geranylgeranylation of Rab GTPases represents one way to control the activity of these proteins. Because the number of molecules modulating RGGT is limited, we combined molecular modeling with biological assays to ascertain how modifications of phosphonocarboxylates, the first reported RGGT inhibitors, rationally improve understanding of their structure-activity relationship. We have identified the privileged position in the core scaffold of the imidazo[1,2-a]pyridine r…
RAS proteins and control of the cell cycle inSaccharomyces cerevisiae
1995
Genes related to the mammalian H-, K-, and N-ras oncogenes were identified in S. cerevisiae by DNA hybridization techniques (for reviews, see Tamanoi, 1988; Gibbs and Marshall, 1989; Broach and Deschenes, 1990). According to the rules of yeast genetics (dominant genes are indicated by three capital letters followed by a number), the yeast genes were denominated RAS1 and RAS2 (collectively referred to as RAS). The corresponding RAS1 and RAS2 proteins were 309 and 322 amino acids long, respectively. The sequence similarity between the human and yeast proteins was very high, reaching 90% identity at the level of the N-terminal 80 amino acids. As a consequence, perfect sequence conservation was…
Identification of the privileged position in the imidazo[1,2-a]pyridine ring of phosphonocarboxylates for development of Rab geranylgeranyl transfera…
2017
Members of the Rab GTPase family are master regulators of vesicle trafficking. When disregulated, they are associated with a number of pathological states. The inhibition of RGGT, an enzyme responsible for post-translational geranylgeranylation of Rab GTPases represents one way to control the activity of these proteins. Because the number of molecules modulating RGGT is limited, we combined molecular modeling with biological assays to ascertain how modifications of phosphonocarboxylates, the first reported RGGT inhibitors, rationally improve understanding of their structure–activity relationship. We have identified the privileged position in the core scaffold of the imidazo[1,2-a]pyridine r…