Structural basis for binding and selectivity of antimalarial and anticancer ethylenediamine inhibitors to protein farnesyltransferase

Autor: Wesley C. Van Voorhis, Michael A. Hast, Said M. Sebti, Michael H. Gelb, Lorena S. Beese, Erin E. Pusateri, Christopher G. Cummings, Michelle A. Blaskovich, Kasey Rivas, Andrew D. Hamilton, Steven Fletcher

Publikováno v: Chemistrybiology. 16(2)

SummaryProtein farnesyltransferase (FTase) catalyzes an essential posttranslational lipid modification of more than 60 proteins involved in intracellular signal transduction networks. FTase inhibitors have emerged as a significant target for developm

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::90e531cceff87f28e0a0a9f6030117fc
https://pubmed.ncbi.nlm.nih.gov/19246009

Synthesis and evaluation of potent, highly-selective, 3-aryl-piperazinone inhibitors of protein geranylgeranyltransferase-I

Autor: Hairuo Peng, Said M. Sebti, Michelle A. Blaskovich, Andrew D. Hamilton, Erin E. Pusateri, Van Thai, Cynthia Bucher, Dora Carrico

Publikováno v: Organic & Biomolecular Chemistry. 4:1768

A series of compounds based on the carboxyl-terminal CAAL sequence of PGGTase-I substrates was designed and synthesized. Using piperazin-2-one as a semi-rigid scaffold, we have introduced critical pharmacophores in a well-defined arrangement to mimic

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7145889c74c82d1111d721ec6d05f3e5
https://doi.org/10.1039/b517572k

Identification of broad-spectrum antiviral compounds and assessment of the druggability of their target for efficacy against respiratory syncytial virus (RSV).

Autor: Bonavia A; Novartis Institutes for Biomedical Research, Inc., 250 Massachusetts Avenue, Cambridge, MA 02139, USA., Franti M, Pusateri Keaney E, Kuhen K, Seepersaud M, Radetich B, Shao J, Honda A, Dewhurst J, Balabanis K, Monroe J, Wolff K, Osborne C, Lanieri L, Hoffmaster K, Amin J, Markovits J, Broome M, Skuba E, Cornella-Taracido I, Joberty G, Bouwmeester T, Hamann L, Tallarico JA, Tommasi R, Compton T, Bushell SM

Publikováno v: Proceedings of the National Academy of Sciences of the United States of America [Proc Natl Acad Sci U S A] 2011 Apr 26; Vol. 108 (17), pp. 6739-44. Date of Electronic Publication: 2011 Apr 18.