Detail of "6699-20-3"

Reference

Structure of mammalian protein geranylgeranyltransferase type-I

Structure of mammalian protein geranylgeranyltransferase type-I. Taylor, Jeffrey S.; Reid, T. Scott; Terry, Kimberly L.; Casey, Patrick J.; Beese, Lorena S. (Department of Biochemistry, Duke Univ. Medical Center, Durham, NC 27710, USA). EMBO Journal, 22(22), 5963-5974 (English) 2003 Oxford University Press. CODEN: EMJODG. ISSN: 0261-4189. DOCUMENT TYPE: Journal CA Section: 7 (Enzymes) Section cross-reference(s): 75 Protein geranylgeranyltransferase type-I (GGTase-I), one of two CaaX prenyltransferases, is an essential enzyme in eukaryotes. GGTase-I catalyzes C-terminal lipidation of >100 proteins, including many GTP- binding regulatory proteins. We present the first structural information for mammalian GGTase-I, including a series of substrate and product complexes that delineate the path of the chem. reaction. These structures reveal that all protein prenyltransferases share a common reaction mechanism and identify specific residues that play a dominant role in detg. prenyl group specificity. 651740-20-4 and 6699-20-3 which are cas registry numbers of substances are two of reagents here. This hypothesis was confirmed by converting farnesyltransferase (15-C prenyl substrate) into GGTase-I (20-C prenyl substrate) with a single point mutation. GGTase-I discriminates against farnesyl diphosphate (FPP) at the product turnover step through the inability of a 15-C FPP to displace the 20-C prenyl-peptide product. Understanding these key features of specificity is expected to contribute to optimization of anti-cancer and anti-parasite drugs. .

Stable analogs of geranylgeranyl diphosphate possessing improved geranylgeranyl versus farnesyl protein transferase inhibitory selectivity

Stable analogs of geranylgeranyl diphosphate possessing improved geranylgeranyl versus farnesyl protein transferase inhibitory selectivity. Minutolo, Filippo; Bertini, Simone; Betti, Laura; Danesi, Romano; Gervasi, Gianbattista; Giannaccini, Gino; Papi, Chiara; Placanica, Giorgio; Barontini, Silvia; Rapposelli, Simona; Macchia, Marco ( Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Pisa 56126, Italy). Bioorganic & Medicinal Chemistry Letters, 13(24), 4405-4408 (English) 2003 Elsevier Science B.V. CODEN: BMCLE8. 120877-66-9 and 6699-20-3 are cas registry numbers of chemicals which are used as reagents here. ISSN: 0960-894X. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 30 Phosphonoacetamido(oxy) groups have proven to be good mimics of the diphosphate portion in geranylgeranyl protein transferase I (GGTase I) inhibitors. The introduction of small alkyl groups (Me, Et) into the diphosphate mimic moiety caused a further decrease in collateral farnesyl protein transferase (FTase) inhibitory activity, thereby improving GGTase I over FTase selectivity. .