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Dive into the research topics where James Pribish is active.

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Featured researches published by James Pribish.


Bioorganic & Medicinal Chemistry Letters | 2012

Structure-based library design and the discovery of a potent and selective mast cell β-tryptase inhibitor as an oral therapeutic agent

Guyan Liang; Suzanne Aldous; Gregory H. Merriman; Julian Levell; James Pribish; Jennifer Cairns; Xin Chen; Sébastien Maignan; Magali Mathieu; Joseph Tsay; Keith Sides; Sam Rebello; Brian Whitely; Isabelle Morize; Henry W. Pauls

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 not exist for other trypsin-like serine proteases of interest. Therefore, inhibitors utilizing this pocket have inherent advantages for being selective against other proteases in the same family. A member of this library was found to be a potent and selective β-tryptase inhibitor with a suitable pharmacokinetic profile for further clinical evaluation.


Archive | 2001

Arylmethylamine derivatives for use as tryptase inhibitors

Peter Charles Astles; Paul Robert Eastwood; Olivier Houille; Julian Levell; Heinz W. Pauls; Mark Czekaj; Guyan Liang; Yong Gong; James Pribish; Kent Neuenschwander


Bioorganic & Medicinal Chemistry Letters | 2005

Design, synthesis, and biological activity of potent and selective inhibitors of mast cell tryptase

Corey R. Hopkins; Mark Czekaj; Steven S. Kaye; Zhongli Gao; James Pribish; Henry W. Pauls; Guyan Liang; Keith Sides; Dona Cramer; Jennifer Cairns; Yongyi Luo; Heng Keang Lim; Roy J. Vaz; Sam Rebello; Sebastian Maignan; Alain Dupuy; Magali Mathieu; Julian Levell


Bioorganic & Medicinal Chemistry | 2005

Structure based design of 4-(3-aminomethylphenyl)piperidinyl-1-amides: novel, potent, selective, and orally bioavailable inhibitors of βII tryptase

Julian Levell; Peter Charles Astles; Paul Robert Eastwood; Jennifer Cairns; Olivier Houille; Suzanne Aldous; Gregory H. Merriman; Brian Whiteley; James Pribish; Mark Czekaj; Guyan Liang; Sébastien Maignan; Jean-Pierre Guilloteau; Alain Dupuy; Jane Davidson; Trevor K.P. Harrison; Andrew David Morley; Simon Watson; Garry Fenton; Clive McCarthy; Joseph Romano; Rose Mappilakunnel Mathew; Darren Engers; Michael Gardyan; Keith Sides; Jennifer Kwong; Joseph Tsay; Sam Rebello; Liduo Shen; Jie Wang


Journal of Medicinal Chemistry | 1967

4-aza-steroids

James Pribish; Cynthia A. Gates; Philip M. Weintraub


Archive | 2008

Pyrimidine hydrazide compounds as PGDS inhibitors

Suzanne Aldous; Michael W Fennie; John Z. Jiang; Stanly John; Lan Mu; Brian Pedgrift; James Pribish; Barbara Rauckman; Jeffrey S. Sabol; Grzegorz T Stoklosa; Sukanthini Thurairatnam; Christopher Loren Vandeusen


Bioorganic & Medicinal Chemistry Letters | 2004

Design of bivalent ligands using hydrogen bond linkers: synthesis and evaluation of inhibitors for human β-tryptase

Roy J. Vaz; Zhongli Gao; James Pribish; Xin Chen; Julian Levell; Larry Davis; Eva Albert; Maurice Brollo; Antonio Ugolini; Dona Cramer; Jennifer Cairns; Keith Sides; Feng Liu; Jennifer Kwong; Jiesheng Kang; Sam Rebello; Michael Elliot; Heng-Keang Lim; Vinolia Chellaraj; Robert W. Singleton; Yi Li


Archive | 1997

17-beta-cyclopropyl (amino/oxy 4-aza steroids as active inhibitors of testosterone 5-alpha-reductase and C17-20-lyase

James Pribish; Cynthia A. Gates; Philipp M Weintraub


Archive | 2008

COMPUESTO DE PIRMIDINA

Brian Pedgrift; Suzanne Aldous; Michael W Fennie; John Z. Jiang; Stanly John; Lan Mu; James Pribish; Barbara Rauckman; Jeffrey S. Sabol; Grzegorz T Stoklosa; Sukanthini Thrurairatnam; Christopher Loren Vandeusen


Archive | 2008

Composés d'hydrazide de pyrimidine en tant qu'inhibiteurs de pgds

Suzanne Aldous; Michael W Fennie; John Z. Jiang; Stanly John; Lan Mu; Brian Pedgrift; James Pribish; Barbara Rauckman; Jeffrey S. Sabol; Grzegorz T Stoklosa; Sukanthini Thurairatnam; Christopher Loren Vandeusen

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