Zobrazeno 1 - 5
of 5
pro vyhledávání: '"James Pribish"'
Autor:
Mark Munson, James Pribish, Lim Sungtaek, Maniar Sachin, Bradford H. Hirth, Robert H. Barker, Jiang John Z, Yong Mi Choi-Sledeski, Sukanthini Thurairatnam, Kwon Yon Musick, Elina Makino, John E. Macor
Publikováno v:
ACS Med Chem Lett
[Image: see text] Metachromatic leukodystrophy (MLD) is a rare, genetic lysosomal storage disorder caused by the deficiency of arylsulfatase A enzyme, which results in the accumulation of sulfatide in the lysosomes of the tissues of central and perip
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ee0e9cd71be8f13535f7151488851852
https://europepmc.org/articles/PMC7549271/
https://europepmc.org/articles/PMC7549271/
Autor:
Sachin Maniar, Anlai Wang, James Pribish, Shih-Min A. Huang, Andrew Hebert, Mikhail Levit, Jinyu Liu, Claude Barberis, Luke Fire, Elina Tserlin, Paul Erdman, Vinod F. Patel, Mark Czekaj, Joseph D. Batchelor, Frank Sun
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 30:127625
N-substituted azaindoles were discovered as potent pan-PIM inhibitors. Lead optimization, guided by structure and focused on physico-chemical properties allowed us to solve inherent hERG and permeability liabilities, and provided compound 27, which s
Discovery of N-substituted 7-azaindoles as Pan-PIM kinases inhibitors - Lead optimization - Part III
Autor:
Andrew Hebert, Paul Erdman, Maniar Sachin, Anlai Wang, Alexandre Gross, Elina Tserlin, Claude Barberis, Vinod F. Patel, Jiang John Z, Mark Czekaj, Mikhail Levit, James Pribish, Frank Sun, Matthieu Barrague, Luke Fire, Shih-Min A. Huang
Publikováno v:
Bioorganicmedicinal chemistry letters. 29(3)
N-substituted azaindoles were discovered as promising pan-PIM inhibitors. Lead optimization is described en route toward the identification of a clinical candidate. Modulation of physico-chemical properties allowed to solve inherent hERG and permeabi
Autor:
James Pribish, Claude Barberis, Liduo Shen, Mark Czekaj, Neil Moorcroft, Mikhail Levit, Elina Tserlin, Anlai Wang, Andrew Hebert, Sandra Moreno-Mazza, Matthieu Barrague, Tahir Majid, Joseph D. Batchelor, Paul Erdman, Alexandre Gross
Publikováno v:
Bioorganicmedicinal chemistry letters. 27(20)
N-Substituted azaindoles have been discovered as pan-PIM kinase inhibitors. Initial SAR, early ADME and PK/PD data of a series of compounds is described and led to the identification of promising pan-PIM inhibitors which validated our interest in the
Autor:
Keith Sides, James Pribish, Magali Mathieu, Sam Rebello, Gregory H. Merriman, Henry W. Pauls, Guyan Liang, Xin Chen, Julian Levell, Jennifer Cairns, Isabelle Morize, Brian Whitely, Joseph T. Tsay, Aldous Suzanne C, Sébastien Maignan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:1049-1054
A solid phase combinatorial library was designed based on X-ray structures and in-silico models to explore an inducible S4+ pocket, which is formed by a simple side-chain rotation of Tyr95. This inducible S4+ pocket is unique to β-tryptase and does