Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Shawn David Erickson"'
Autor:
Rebecca M. Reese, Desiree Amm, Justin Ly, Aleksandr Kolesnikov, Christine E. Brotherton-Pleiss, Steven Do, Daniel G. Shore, David H. Hackos, Vishal Verma, Matthew Volgraf, Lesley J. Murray, Xiaofeng Xu, Guosheng Wu, Aijun Lu, Jun Chen, Baihua Hu, Martin E. Dahl, Huifen Chen, Yuen Po-Wai, Elisia Villemure, Yamin Zhang, Joseph P. Lyssikatos, Yong Chen, Brian Safina, Lan Wang, Anthony Estrada, Wienke Lange, Shawn David Erickson, Shannon D. Shields, Suzanne Tay
Publikováno v:
Journal of medicinal chemistry. 61(8)
Transient receptor potential ankyrin 1 (TRPA1) is a non-selective cation channel expressed in sensory neurons where it functions as an irritant sensor for a plethora of electrophilic compounds and is implicated in pain, itch, and respiratory disease.
Autor:
Karin Conde-Knape, Yonglin Ren, Irina Hakimi, Paul Gillespie, Jefferson Wright Tilley, Sung-Sau So, Shawn David Erickson, Fiorenza Falcioni, Francis A. Mennona, Yimin Qian, Hamid Salari
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:4216-4220
Benzimidazole and indane are the two key fragments in our potent and selective MCH-1 receptor (MCHR1) antagonists. To identify novel linkers connecting the two fragments, we investigated diamino-cycloalkane-derived analogs and discovered highly poten
Autor:
Henrietta Dehmlow, Ulrike Obst Sander, Sherrie Lynn Pietranico-Cole, Christoph Kuratli, Olivier Gavelle, Kyungjin Kim, Caterina Bissantz, Rainer E. Martin, Hans Richter, Christoph Ullmer, Shawn David Erickson, Rubén Alvarez-Sánchez
Publikováno v:
ChemMedChem. 8:569-576
Potency with potential: 2-Phenoxy-nicotinamides were identified as potent agonists at the GPBAR1 receptor, a target in the treatment of obesity, type 2 diabetes and metabolic syndrome. Extensive structure-activity relationship studies supported by ho
Publikováno v:
Burger's Medicinal Chemistry and Drug Discovery
This chapter includes a summary of the mechanism of action, history, and ADME properties compounds selected from four classes of marketed drugs for the treatment of type 2 diabetes. These include the biguanides (metformin), α-glucosylase inhibitors,
Autor:
Rebecca Taub, David Robert Bolin, Shawn David Erickson, Charles Belunis, Stanley Wertheimer, Cristina M. Rondinone, Anish Konkar, Karin Conde-Knape
Publikováno v:
Drug Discovery Today: Therapeutic Strategies. 4:129-135
Body weight is determined by the net difference in calorie consumption and energy expenditure. The balance between triglyceride biosynthesis and breakdown processes in the body determines the amount of total fat mass in an individual. Positive energy
Autor:
Damian Arnaiz, Gary Phillips, Shawn David Erickson, Marc Whitlow, Margaret Kenrick, James J. Devlin, Gonghua Pan, Cecile Santos, William J. Guilford, Robert G. Wei, Marc Adler, Kurt W. Saionz, Bin Ye, Ron Vergona, John Parkinson, Zuchun Spring Zhao, David D. Davey, Michael Ohlmeyer, Babu Subramanyam, Vidyadhar M. Paradkar, Mark A. Polokoff, Keith A. Eagen, Michael M. Morrissey
Publikováno v:
Journal of Medicinal Chemistry. 50:1146-1157
By the screening of a combinatorial library for inhibitors of nitric oxide (NO) formation by the inducible isoform of nitric oxide synthase (iNOS) using a whole-cell assay, 2-(imidazol-1-yl)pyrimidines were identified. Compounds were found to inhibit
Autor:
Martin-Jan Smit, Jac C. H. M. Wijkmans, Rong-Qiang Liu, Jaap van der Louw, Koc-Kan Ho, Jim Inglese, Shawn David Erickson, Ming You, Ellen Son, Andrew Laird Roughton, Douglas S. Auld, G.M.T. Vogel, Christopher M. Masterson, Paolo Conti, Daming Feng, Martijn Rooseboom, Adolph Bohnstedt, Celia Kingsbury, Maria L. Webb, Steven G. Kultgen, Yajing Rong, Michael Ohlmeyer, Philippe Samama, Wim Dokter
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:2724-2728
An imidazolylpyrimidine was identified in a CXCR2 chemokine receptor antagonist screen and was optimized for potency, in vitro metabolic stability, and oral bioavailability. It was found that subtle structural modification within the series affected
Autor:
Rebecca Taub, Karin Conde-Knape, Lucy Orzechowski, Warren McComas, Chun Ma, Bruce L. Banner, Fiorenza Falcioni, Steven Gregory Mischke, Irina Hakimi, John P. Tengi, Hong Wang, Robert Francis Kester, Kyungjin Kim, Kshitij Chhabilbhai Thakkar, Francis A. Mennona, Bernard Michael Hennessy, Yimin Qian, Hamid Salari, Steven Joseph Berthel, Jefferson Wright Tilley, Shawn David Erickson
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(4)
This paper describes the lead optimization of a new series of potent, selective, orally bioavailable, brain-penetrant MCH-1 receptor antagonists. A major focus of the work was to achieve a selectivity profile appropriate for in vivo efficacy studies
Autor:
Kirk Mcmillan, Gonghua Pan, Michael M. Morrissey, Leslie J. Browne, Mark A. Polokoff, Baldwin John J, Ronald Vergona, Gary Phillips, Marc Adler, Michael Ohlmeyer, David D. Davey, John Parkinson, Cornell Mallari, Charles B. Glaser, Nolan H. Sigal, Shawn David Erickson, Keith A. Eagen, James J. Devlin, Tish A. Young, Ronald E. Dolle, Eric Blasko, Daniel Chelsky, Richard I. Feldman, Douglas S. Auld, Marc Whitlow
Publikováno v:
Proceedings of the National Academy of Sciences of the United States of America. 97(4)
Potent and selective inhibitors of inducible nitric oxide synthase (iNOS) (EC 1.14.13.39 ) were identified in an encoded combinatorial chemical library that blocked human iNOS dimerization, and thereby NO production. In a cell-based iNOS assay (A-172
Autor:
Hans Richter, Ulrike Obst Sander, Sherrie Lynn Pietranico-Cole, Caterina Bissantz, Christoph Ullmer, Shawn David Erickson, Kyungjin Kim, Rubén Alvarez-Sánchez, Christoph Kuratli, Rainer E. Martin, Olivier Gavelle, Henrietta Dehmlow
Publikováno v:
ChemMedChem. 8:533-533