Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Summer E. Young"'
Publikováno v:
PLoS ONE, Vol 8, Iss 6, p e65528 (2013)
Protease activated receptor-4 (PAR4) is one of the thrombin receptors on human platelets and is a potential target for the management of thrombotic disorders. We sought to develop potent, selective, and novel PAR4 antagonists to test the role of PAR4
Externí odkaz:
https://doaj.org/article/f1fe95d2121446d78f56e84568d803ff
Autor:
Summer E. Young, Shaun R. Stauffer, Kayla J. Temple, Craig W. Lindsley, Wandong Wen, Matthew T. Duvernay, Jae G. Maeng, Anna L. Blobaum, Wenjun Wu, Heidi E. Hamm
Publikováno v:
Journal of Medicinal Chemistry. 59:7690-7695
Here, we describe the development of a series of highly selective PAR4 antagonists with nanomolar potency and selectivity versus PAR1, derived from the indole-based 3. Of these, 9j (PAR4 IC50 = 445 nM, PAR1 response IC50 > 30 µM) and 10h (PAR4 IC50
Autor:
Charles W. Locuson, Summer E. Young, Julie L. Engers, Wenjun Wu, Kellie D. Nance, Wandong Wen, Bruce J. Melancon, J. Scott Daniels, Matthew T. Duvernay, Michael L. Schulte, Michael R. Wood, Shaun R. Stauffer, Craig W. Lindsley, Heidi E. Hamm
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:4708-4713
Herein we report the discovery and SAR of an indole-based protease activated receptor-4 (PAR-4) antagonist scaffold derived from a similarity search of the Vanderbilt HTS collection, leading to MLPCN probe ML354 (VU0099704). Using a novel PAC-1 fluor
Publikováno v:
Molecular Pharmacology. 83:781-792
With the recent interest of protease-activated receptors (PAR) 1 and PAR4 as possible targets for the treatment of thrombotic disorders, we compared the efficacy of protease-activated receptor (PAR)1 and PAR4 in the generation of procoagulant phenoty
Publikováno v:
Chemical Research in Toxicology. 19:463-468
The C2'-oxidized abasic lesion (C2-AP) is produced in DNA that is subjected to oxidative stress. C2-AP is incised by phosphodiesterases, but is not a substrate for endonuclease III even though a Schiff base is formed (Greenberg, M. M., et al. (2004)
Publikováno v:
PLoS ONE, Vol 8, Iss 6, p e65528 (2013)
PLoS ONE
PLoS ONE
Protease activated receptor-4 (PAR4) is one of the thrombin receptors on human platelets and is a potential target for the management of thrombotic disorders. We sought to develop potent, selective, and novel PAR4 antagonists to test the role of PAR4
Autor:
Summer E. Young, Heidi E. Hamm, Nancy Colowick, Olivier Boutaud, W. James Hudson, John A. Oates, Michael Holinstat
Publikováno v:
The FASEB Journal. 23
Publikováno v:
Blood. 118:1135-1135
Abstract 1135 Protease activated receptor (PAR) stimulation induces procoagulant phenotypes on platelets leading to thrombin generation; however, the efficacy of PAR1 versus PAR4 in the presentation of coagulation cofactors and assembly of coagulatio