Zobrazeno 1 - 10
of 12
pro vyhledávání: '"Mike Fiorino"'
Autor:
Kent Miner, Katja Labitzke, Benxian Liu, Paul Wang, Kathryn Henckels, Kevin Gaida, Robin Elliott, Jian Jeffrey Chen, Longbin Liu, Anh Leith, Esther Trueblood, Kelly Hensley, Xing-Zhong Xia, Oliver Homann, Brian Bennett, Mike Fiorino, John Whoriskey, Gang Yu, Sabine Escobar, Min Wong, Teresa L. Born, Alison Budelsky, Mike Comeau, Dirk Smith, Jonathan Phillips, James A. Johnston, Joseph G. McGivern, Kerstin Weikl, David Powers, Karl Kunzelmann, Deanna Mohn, Andreas Hochheimer, John K. Sullivan
Publikováno v:
Frontiers in Pharmacology, Vol 10 (2019)
There is an unmet need in severe asthma where approximately 40% of patients exhibit poor β-agonist responsiveness, suffer daily symptoms and show frequent exacerbations. Antagonists of the Ca2+-activated Cl− channel, TMEM16A, offers a new mechanis
Externí odkaz:
https://doaj.org/article/41d8cbf66f0741758aee1902a2f9ab21
Autor:
John A. Davis, Yu Zhang, James B. Rottman, Fergus R. Byrne, Jeannette Bigler, Alison L. Budelsky, Carole L. Smith, Antony Symons, Mike Fiorino, William A. Brown, Erin Stevens, Joseph R. Maxwell, Jennifer E. Towne
Publikováno v:
Immunity. 43(4):739-750
SummaryInterleukin-23 (IL-23) and IL-17 are cytokines currently being targeted in clinical trials. Although inhibition of both of these cytokines is effective for treating psoriasis, IL-12 and IL-23 p40 inhibition attenuates Crohn’s disease, wherea
Autor:
Andrew Tasker, Andrea Itano, Anu Gore, Paul E. Harrington, Mike Frohn, Victor J. Cee, Michele McElvain, Min Wong, Mike Fiorino, Alexander J. Pickrell, Kelvin K. C. Sham, Han Xu, Brian A. Lanman, Anthony B. Reed, Yang Xu, Susana C. Neira, Scot Middleton, Henry Morrison
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:1779-1783
Replacement of the azetidine carboxylate of an S1P1 agonist development candidate, AMG 369, with a range of acyclic head-groups led to the identification of a novel, S1P3-sparing S1P1 agonist, (−)-2-amino-4-(3-fluoro-4-(5-(1-phenylcyclopropyl)thiaz
Autor:
Kelvin K. C. Sham, Lewis D. Pennington, Paul E. Harrington, Matthew R. Lee, Michele McElvain, Xuxia Zhang, Heather A. Arnett, Min Wong, Alexander J. Pickrell, Anthony B. Reed, Henry Morrison, Victor J. Cee, Mike Fiorino, Christopher H. Fotsch, Michael J. Frohn, Yang Xu, Michael Croghan, Han Xu, Brian A. Lanman, Andrew Tasker, Michelle Horner
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:527-531
We reveal how a N-scan SAR strategy (systematic substitution of each CH group with a N atom) was employed for quinolinone-based S1P(1) agonist 5 to modulate physicochemical properties and optimize in vitro and in vivo activity. The diaza-analog 17 di
Autor:
Michael Croghan, Andrew Tasker, Matthew R. Lee, Xuxia Zhang, Heather A. Arnett, Victor J. Cee, Anthony B. Reed, Kelvin K. C. Sham, Michele McElvain, Henry Morrison, Alexander J. Pickrell, Lewis D. Pennington, Mike Frohn, Yang Xu, Paul E. Harrington, Min Wong, Han Xu, Brian A. Lanman, Mike Fiorino, Christopher H. Fotsch
Publikováno v:
ACS Medicinal Chemistry Letters. 3:74-78
The optimization of a series of S1P1 agonists with limited activity against S1P3 is reported. A polar headgroup was used to improve the physicochemical and pharmacokinetic parameters of lead quinolinone 6. When dosed orally at 1 and 3 mg/kg, the azah
Autor:
Min Wong, Heather A. Arnett, Michael Croghan, Michele McElvain, Yang Xu, Xuxia Zhang, Matthew R. Lee, Lewis D. Pennington, Paul E. Harrington, Henry Morrison, Victor J. Cee, Anthony B. Reed, Michael J. Frohn, Alexander J. Pickrell, Mike Fiorino, Kelvin K. C. Sham, Han Xu, Brian A. Lanman, Christopher H. Fotsch, Michelle Horner
Publikováno v:
ACS Medicinal Chemistry Letters. 2:752-757
The sphingosine-1-phosphate-1 receptor (S1P1) and its endogenous ligand sphingosine-1-phosphate (S1P) cooperatively regulate lymphocyte trafficking from the lymphatic system. Herein, we disclose 4-methoxy-N-[2-(trifluoromethyl)biphenyl-4-ylcarbamoyl]
Autor:
Min Wong, Yang Xu, Scot Middleton, Matthew R. Lee, Anu Gore, Mike Fiorino, Alex Pickrell, Kristine M. Muller, Andrea Itano, Mike Frohn, Heather A. Arnett, Janet Buys, Michelle Horner, Dalia Rivenzon-Segal, Jennifer E. Golden, Victor J. Cee, Hugo M. Vargas, Roland Burli, Susana C. Neira, Michael Schrag, Han Xu, Brian A. Lanman, Michele McElvain, Xuxia Zhang, Jerry Siu
Publikováno v:
ACS Medicinal Chemistry Letters. 2:107-112
The optimization of a series of thiazolopyridine S1P1 agonists with limited activity at the S1P3 receptor is reported. These efforts resulted in the discovery of 1-(3-fluoro-4-(5-(1-phenylcyclopropyl)thiazolo-[5,4-b]pyridin-2-yl)benzyl)azetidine-3-ca
Autor:
Yang Xu, Mike Fiorino, Elizabeth Tominey, Min Wong, Lisa Sherman, Victor J. Cee, Roland Burli, Brad Henkle, Han Xu, Jerry Siu, Keith Kelley, Matt Adlam, Michele McElvain
Publikováno v:
Journal of biomolecular screening. 18(9)
Surrogate readouts of G-protein-coupled receptor signaling pathways using highly engineered systems are often employed in the drug discovery process. However, accumulating data have demonstrated the importance of selecting relevant biological activit
Autor:
Mike, Frohn, Victor J, Cee, Brian A, Lanman, Alexander J, Pickrell, Jennifer, Golden, Dalia, Rivenzon-Segal, Scot, Middleton, Mike, Fiorino, Han, Xu, Michael, Schrag, Yang, Xu, Michele, McElvain, Kristine, Muller, Jerry, Siu, Roland, Bürli
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(1)
An SAR campaign designed to increase polarity in the 'tail' region of benzothiazole 1 resulted in two series of structurally novel 5-and 6-substituted S1P(1) agonists. Structural optimization for potency ultimately delivered carboxamide (+)-11f, whic
Autor:
Michelle Horner, Kristine M. Muller, Xuxia Zhang, Xiang Yu, Nili Schutz, Jerry Siu, Dalia Rivenzon-Segal, Roland Burli, Zhang Zhaoda, Susana C. Neira, Hugo M. Vargas, Alexander J. Pickrell, Jennifer E. Golden, Yang Xu, Victor J. Cee, Michael Schrag, Scot Middleton, Jian Lin, Yael Marantz, Andrea Itano, Mercedes Lobera, Han Xu, Brian A. Lanman, Michele McElvain, Janet Buys, Anu Gore, Srinivasa R Cheruku, Anurag Sharadendu, Mike Fiorino, Mike Frohn
Optimization of a benzofuranyl S1P1 agonist lead compound (3) led to the discovery of 1-(3-fluoro-4-(5-(2-fluorobenzyl)benzo[d]thiazol-2-yl)benzyl)azetidine-3-carboxylic acid (14), a potent S1P1 agonist with minimal activity at S1P3. Dosed orally at
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4114b66ba763963fd644e7ff1f508317
https://europepmc.org/articles/PMC4018108/
https://europepmc.org/articles/PMC4018108/