Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Paderes Genevieve Deguzman"'
Autor:
Michele Yang, Ganesh B. Bhat, Jacqui Elizabeth Hoffman, Andrea Fanjul, Stan Kupchinsky, Jacques Ermolieff, Klaus Ruprecht Dress, Cheng Hengmiao, Phuong Le, Jean Joo Matthews, Sajiv Krishnan Nair, Paul A. Rejto, T.A. Pauly, Evan Walters, Jocelyn Herrera, Christopher Ronald Smith, Martin Paul Edwards, Bridget Mccarthy Cole, Christine Loh, Cripps Stephan James, Natilie Hosea, Paderes Genevieve Deguzman
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:2897-2902
The design and development of a series of highly selective pyrrolidine carboxamide 11β-HSD1 inhibitors are described. These compounds including PF-877423 demonstrated potent in vitro activity against both human and mouse 11β-HSD1 enzymes. In an in
Autor:
Margaret L. Gregory, Eileen Valenzuela Tompkins, Karen D. Nared-Hood, Rosemary Castillo, David R. Luthin, Kenna Anderes, Vazir Haresh N, John M. May, Yufeng Hong, Mary A. Castro, Paderes Genevieve Deguzman, Mark B. Anderson, Eugenia Kraynov
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:3635-3639
A novel series of derivatives of mono- and diaminopyrimidines 1 potently displaced binding of a radiolabeled GnRH analogue to human and rat GnRH receptors. Analogues from these series competitively antagonized GnRH-stimulated increases in extracellul
Autor:
Li Haitao, Paderes Genevieve Deguzman, Brion W. Murray, Xinjun Hou, RoseAnn Ferre, Marakovits Joseph T, M. Catherine Johnson, Paul S. Humphries, Samantha Elizabeth Greasley, Eugenia Kraynov, Joseph Piraino, Dong Liming, Eleanor Dagostino, Chuangxing Guo
Publikováno v:
Bioorganicmedicinal chemistry letters. 24(17)
The design of potent Pin1 inhibitors has been challenging because its active site specifically recognizes a phospho-protein epitope. The de novo design of phosphate-based Pin1 inhibitors focusing on the phosphate recognition pocket and the successful
Correction to Highly Selective and Potent Thiophenes as PI3K Inhibitors with Oral Antitumor Activity
Autor:
Peter A. Wells, Matthew A. Marx, Qiyue Hu, Jinjiang Zhu, Marlena Walls, Graham L. Smith, Simon Bailey, Neal W. Sach, Min-Jean Yin, Qing J. Li, Paderes Genevieve Deguzman, Kevin K.-C. Liu, Chunze Li, Paul F. Richardson, Aihua Zou, Jeffrey H. Chen, Qinhua Huang, Sangita M. Baxi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::226ec5f732f92fd7798adb5241a85dd7
https://europepmc.org/articles/PMC4030792/
https://europepmc.org/articles/PMC4030792/
Autor:
Sangita M. Baxi, Marlena Walls, Paderes Genevieve Deguzman, Neal W. Sach, Kevin K.-C. Liu, Jeffrey H. Chen, Qinhua Huang, Matthew A. Marx, Aihua Zou, Min-Jean Yin, Qiyue Hu, Graham L. Smith, Simon Bailey, Qing J. Li, Jinjiang Zhu, Paul F. Richardson, Peter A. Wells, Chunze Li
Highly selective PI3K inhibitors with subnanomolar PI3Kα potency and greater than 7000-fold selectivity against mTOR kinase were discovered through structure-based drug design (SBDD). These tetra-substituted thiophenes were also demonstrated to have
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0586b273c58f27e3a33cf986e91a06d4
https://europepmc.org/articles/PMC4018126/
https://europepmc.org/articles/PMC4018126/
Autor:
Buwen Huang, Jeff Elleraas, Klaus Ruprecht Dress, Paul A. Rejto, T.A. Pauly, Paderes Genevieve Deguzman
Publikováno v:
Methods in Molecular Biology ISBN: 9781607619307
Multiproperty lead optimization that satisfies multiple biological endpoints remains a challenge in the pursuit of viable drug candidates. Optimization of a given lead compound to one having a desired set of molecular attributes often involves a leng
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d030e83b5e6cfe883b1d05029f558453
https://doi.org/10.1007/978-1-60761-931-4_10
https://doi.org/10.1007/978-1-60761-931-4_10
Autor:
Christie Lance Christopher, Mary A. Castro, Margaret L. Gregory, Rosemary Castillo, David Robert Luthin, Kenna Anderes, Ved P. Pathak, Qiang Ye, John M. May, Vazir Haresh N, Karen D. Nared-Hood, Paderes Genevieve Deguzman, Mark B. Anderson, Eugenia Kraynov
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 305(2)
Gonadotropin-releasing hormone (GnRH) receptor antagonists have potential in treating numerous hormone-dependent pathologies including cancers of the prostate, breast, and ovary, endometriosis, and fertility disorders. An unmet clinical need exists f
Autor:
Li Haitao, Eileen Valenzuela Tompkins, David R. Luthin, Vazir Haresh N, Christie Lance Christopher, Paderes Genevieve Deguzman, John M. May, Yufeng Hong, Mark B. Anderson, Mary A. Castro, Karen D. Nared-Hood, Ved P. Pathak
Publikováno v:
Bioorganicmedicinal chemistry letters. 12(23)
A novel series of non-peptide derivatives 1, 14, and 15 that bind with high affinity to the human GnRH receptors is discussed. The discovery was made from screening our in-house libraries that contained the active structure 2 along with a trace amoun