William Westlin
Overview
Explore the profile of William Westlin including associated specialties, affiliations and a list of published articles.
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10
Citations
337
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Recent Articles
1.
Leit S, Greenwood J, Carriero S, Mondal S, Abel R, Ashwell M, et al.
J Med Chem
. 2023 Jul;
66(15):10473-10496.
PMID: 37427891
TYK2 is a key mediator of IL12, IL23, and type I interferon signaling, and these cytokines have been implicated in the pathogenesis of multiple inflammatory and autoimmune diseases such as...
2.
Leit S, Greenwood J, Mondal S, Carriero S, Dahlgren M, Harriman G, et al.
Bioorg Med Chem Lett
. 2022 Jul;
73:128891.
PMID: 35842205
TYK2 is a member of the JAK family of kinases and a key mediator of IL-12, IL-23, and type I interferon signaling. These cytokines have been implicated in the pathogenesis...
3.
TYK2 inhibition reduces type 3 immunity and modifies disease progression in murine spondyloarthritis
Gracey E, Hromadova D, Lim M, Qaiyum Z, Zeng M, Yao Y, et al.
J Clin Invest
. 2020 Mar;
130(4):1863-1878.
PMID: 32149730
Spondyloarthritis (SpA) represents a family of inflammatory diseases of the spine and peripheral joints. Ankylosing spondylitis (AS) is the prototypic form of SpA in which progressive disease can lead to...
4.
Orally active fumagillin analogues: transformations of a reactive warhead in the gastric environment
Arico-Muendel C, Blanchette H, Benjamin D, Caiazzo T, Centrella P, DeLorey J, et al.
ACS Med Chem Lett
. 2014 Jun;
4(4):381-6.
PMID: 24900682
Semisynthetic analogues of fumagillin, 1, inhibit methionine aminopeptidase-2 (MetAP2) and have entered the clinic for the treatment of cancer. An optimized fumagillin analogue, 3 (PPI-2458), was found to be orally...
5.
Walter A, Tjin Tham Sjin R, Haringsma H, Ohashi K, Sun J, Lee K, et al.
Cancer Discov
. 2013 Sep;
3(12):1404-15.
PMID: 24065731
Unlabelled: Patients with non-small cell lung cancer (NSCLC) with activating EGF receptor (EGFR) mutations initially respond to first-generation reversible EGFR tyrosine kinase inhibitors. However, clinical efficacy is limited by acquired...
6.
Nacht M, Qiao L, Sheets M, St Martin T, Labenski M, Mazdiyasni H, et al.
J Med Chem
. 2013 Jan;
56(3):712-21.
PMID: 23360348
PI3Kα has been identified as an oncogene in human tumors. By use of rational drug design, a targeted covalent inhibitor 3 (CNX-1351) was created that potently and specifically inhibits PI3Kα....
7.
Arico-Muendel C, Belanger B, Benjamin D, Blanchette H, Caiazzo T, Centrella P, et al.
Drug Metab Dispos
. 2013 Jan;
41(4):814-26.
PMID: 23355637
The natural product fumagillin exhibits potent antiproliferative and antiangiogenic properties. The semisynthetic analog PPI-2458, [(3R,4S,5S,6R)-5-methoxy-4-[(2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl]-1-oxaspiro[2.5]octan-6-yl] N-[(2R)-1-amino-3-methyl-1-oxobutan-2-yl]carbamate, demonstrates rapid inactivation of its molecular target, methionine aminopeptidase-2 (MetAP2), and good efficacy in...
8.
Arico-Muendel C, Benjamin D, Caiazzo T, Centrella P, Contonio B, Cook C, et al.
J Med Chem
. 2009 Nov;
52(24):8047-56.
PMID: 19929003
Inhibition of methionine aminopeptidase-2 (MetAP2) represents a novel approach to antiangiogenic therapy. We describe the synthesis and activity of fumagillin analogues that address the pharmacokinetic and safety liabilities of earlier...
9.
Wendt J, Wu H, Stenmark H, Boys M, Downs V, Penning T, et al.
Bioorg Med Chem Lett
. 2005 Nov;
16(4):845-9.
PMID: 16303301
We describe a series of 2,5 thiazole containing compounds, which are potent antagonists of the integrin alpha(v)beta3 and show selectivity relative to the other integrins, such as alpha(IIb)beta3 and alpha(v)beta6....
10.
Boys M, Schretzman L, Chandrakumar N, Tollefson M, Mohler S, Downs V, et al.
Bioorg Med Chem Lett
. 2005 Nov;
16(4):839-44.
PMID: 16298127
We describe a series of 1,2,4-oxadiazoles, which are potent antagonists of the integrin alpha(v)beta3 and, in addition, show selectivity relative to the other beta3 integrin alpha(IIb)beta3. In whole cells, the...