Zobrazeno 1 - 10
of 17
pro vyhledávání: '"Lance Goulet"'
Autor:
Jian Zhao, Shimiao Wang, Sun Hee Kim, Sangdon Han, Elizabeth Rico-Bautista, Emmanuel Sturchler, Julie Nguyen, Hannah Tan, Christine Staley, Ana Karin Kusnetzow, Stephen F. Betz, Michael Johns, Lance Goulet, Rosa Luo, Melissa Fowler, Jon Athanacio, Stacy Markison, R. Scott Struthers, Yunfei Zhu
Publikováno v:
Bioorganicmedicinal chemistry letters. 71
SST5 receptor activation potently inhibits insulin secretion from pancreatic β-cells, and an orally available nonpeptide selective SST5 agonist may be used to effectively manage the blood glucose levels of congenital HI patients to avoid severe hypo
Autor:
Andiliy G. Lai, Katherine Nguyen, Gretchen Bain, Lance Goulet, Imelda Calderon, Fei Huang, Deidre A. MacKenna, Kristen E. Shannon, Janice Darlington, Patricia Prodanovich, John H. Hutchinson, David Lonergan, Angelina M. Santini, Gina L. Ma, Jilly F. Evans, Taylor Lasof, Martin W. Rowbottom, Christopher D. King
Publikováno v:
Journal of Medicinal Chemistry. 60:4403-4423
LOXL2 catalyzes the oxidative deamination of ε-amines of lysine and hydroxylysine residues within collagen and elastin, generating reactive aldehydes (allysine). Condensation with other allysines or lysines drives the formation of inter- and intramo
Autor:
Lance Goulet, Robert Lafyatis, Katharine E. Black, Leaya George, Andrew M. Tager, Gretchen Bain, Clemens K. Probst, Flavia V. Castelino, Veronica A. Pace
Publikováno v:
Arthritis & Rheumatology. 68:2964-2974
Objective We previously implicated the lipid mediator lysophosphatidic acid (LPA) as having a role in dermal fibrosis in systemic sclerosis (SSc). The aim of this study was to identify the role of the LPA-producing enzyme autotaxin (ATX), and to conn
Autor:
Adam J. Stein, Ranjinder S. Sidhu, Lance Goulet, Jilly F. Evans, Jeffrey M. Schaub, Dave Lonergan, Janice Darlington, Gretchen Bain, Nina M. P. Stelzer, Imelda Calderon, Angelina M. Santini, John H. Hutchinson, Pat Prodanovich
Publikováno v:
Molecular Pharmacology. 88:982-992
Autotaxin (ATX) is a secreted enzyme that hydrolyzes lysophosphatidylcholine to lysophosphatidic acid (LPA). LPA is a bioactive phospholipid that regulates diverse biological processes, including cell proliferation, migration, and survival/apoptosis,
Autor:
Zhongzhou Shen, Evan Smith, Weiwei Tan, Melissa O'Gorman, Gregory S. Walker, Shinji Yamazaki, Deepak Dalvie, Bill J. Smith, Lance Goulet, Gabriella Bedarida, Helen Y. Zou, Theodore R. Johnson, James G. Christensen, Akintunde Bello, Leslie Nguyen
Publikováno v:
Xenobiotica. 45:45-59
1. Crizotinib (XALKORI®), an oral inhibitor of anaplastic lymphoma kinase (ALK) and mesenchymal-epithelial transition factor kinase (c-Met), is currently approved for the treatment of patients with non-small cell lung cancer that is ALK-positive. 2.
Autor:
Dean Stamos, Michael Liu, Beth Fleck, Lance Goulet, Weichao Chen, Harmon J. Zuccola, Phillip W. Snyder, Dao Tran, Peggy Chiang, James Reynolds, Azin Nezami, Samuel Sperry, Khisal Ahmed Alvi, Alcacio Timothy, Lisa Woody, William Kargo, Amy Turnbull, Timothy Neubert, Justin T. Ernst
Publikováno v:
Journal of Medicinal Chemistry. 57:3382-3400
A structure-based drug design strategy was used to optimize a novel benzolactam series of HSP90α/β inhibitors to achieve >1000-fold selectivity versus the HSP90 endoplasmic reticulum and mitochondrial isoforms (GRP94 and TRAP1, respectively). Selec
Autor:
Lance Goulet, Fei Huang, Patricia Prodanovich, Dave Lonergan, Gretchen Bain, Janice Darlington, Andiliy G. Lai, Angelina M. Santini, Kristen E. Shannon, Gina L. Ma, Christopher D. King, Jilly F. Evans, Imelda Calderon, Adam J. Stein, John H. Hutchinson
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 360(1)
Autotaxin (ATX) is a secreted glycoprotein that converts lysophosphatidylcholine (LPC) to the bioactive phospholipid lysophosphatidic acid (LPA) and is the major enzyme generating circulating LPA. Inhibition of LPA signaling has profound antifibrotic
Autor:
Simon Bailey, Cheng Hengmiao, Marlena Walls, Matthew A. Marx, Kevin K.-C. Liu, Jacqui Elizabeth Hoffman, Zhengyu Liu, Jinjiang Zhu, Lisa Guo, John Li, Lance Goulet, Peter A. Wells, Chunze Li, Ying Jiang, Daniel R. Knighton, Min-Jean Yin, Ted William Johnson, Michael Zientek, Sangita M. Baxi, Theodore O. Johnson
Publikováno v:
ACS Medicinal Chemistry Letters. 4:91-97
PI3K, AKT, and mTOR are key kinases from PI3K signaling pathway being extensively pursued to treat a variety of cancers in oncology. To search for a structurally differentiated back-up candidate to PF-04691502, which is currently in phase I/II clinic
Autor:
Angus N. R. Nedderman, Dennis A. Smith, Cho-Ming Loi, Lance Goulet, Hai-Zhi Bu, Susan Hurst, R. Scott Obach, Evan Smith, Ping Kang, Deepak Dalvie, Chandra Prakash
Publikováno v:
Chemical Research in Toxicology. 22:357-368
An early understanding of key metabolites of drugs is crucial in drug discovery and development. As a result, several in vitro models typically derived from liver are frequently used to study drug metabolism. It is presumed that these in vitro system
Autor:
Flavia V, Castelino, Gretchen, Bain, Veronica A, Pace, Katharine E, Black, Leaya, George, Clemens K, Probst, Lance, Goulet, Robert, Lafyatis, Andrew M, Tager
Publikováno v:
Arthritisrheumatology (Hoboken, N.J.). 68(12)
We previously implicated the lipid mediator lysophosphatidic acid (LPA) as having a role in dermal fibrosis in systemic sclerosis (SSc). The aim of this study was to identify the role of the LPA-producing enzyme autotaxin (ATX), and to connect the AT