Christopher J Dinsmore
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Explore the profile of Christopher J Dinsmore including associated specialties, affiliations and a list of published articles.
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Articles
24
Citations
453
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0
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Recent Articles
1.
Josue Ruiz E, Pinto-Fernandez A, Turnbull A, Lan L, Charlton T, Scott H, et al.
Elife
. 2021 Oct;
10.
PMID: 34636321
Lung squamous cell carcinoma (LSCC) is a considerable global health burden, with an incidence of over 600,000 cases per year. Treatment options are limited, and patient's 5-year survival rate is...
2.
Caravella J, Lin J, Diebold R, Campbell A, Ericsson A, Gustafson G, et al.
J Med Chem
. 2020 Jan;
63(4):1612-1623.
PMID: 31971798
Inhibition of mutant IDH1 is being evaluated clinically as a treatment option for oncology. Here we describe the structure-based design and optimization of quinoline lead compounds to identify , a...
3.
Evans D, Dinsmore C, Watson P, Wood M, Richardson T, Trotter B, et al.
Angew Chem Int Ed Engl
. 2018 May;
37(19):2704-2708.
PMID: 29711602
Controlling the elements of planar and axial chirality are the principal challenges in the synthesis of the aglycon of vancomycin. Vancomycin is the prototypical member of the glycopeptide family of...
4.
Siu T, Brubaker J, Fuller P, Torres L, Zeng H, Close J, et al.
J Med Chem
. 2017 Nov;
60(23):9676-9690.
PMID: 29156136
The discovery of a potent selective low dose Janus kinase 1 (JAK1) inhibitor suitable for clinical evaluation is described. As part of an overall goal to minimize dose, we pursued...
5.
Turnbull A, Ioannidis S, Krajewski W, Pinto-Fernandez A, Heride C, Martin A, et al.
Nature
. 2017 Oct;
550(7677):481-486.
PMID: 29045389
Ubiquitination controls the stability of most cellular proteins, and its deregulation contributes to human diseases including cancer. Deubiquitinases remove ubiquitin from proteins, and their inhibition can induce the degradation of...
6.
Wolkenberg S, Nolt M, Bilodeau M, Trotter B, Manley P, Kett N, et al.
Bioorg Med Chem Lett
. 2017 Jan;
27(4):1062-1069.
PMID: 28131713
Selective inhibition of Kv1.5, which underlies the ultra-rapid delayed rectifier current, I, has been pursued as a treatment for atrial fibrillation. Here we describe the discovery of MK-1832, a Kv1.5...
7.
Simov V, Deshmukh S, Dinsmore C, Elwood F, Fernandez R, Garcia Y, et al.
Bioorg Med Chem Lett
. 2016 Mar;
26(7):1803-8.
PMID: 26927423
The mammalian Janus Kinases (JAK1, JAK2, JAK3 and TYK2) are intracellular, non-receptor tyrosine kinases whose activities have been associated in the literature and the clinic with a variety of hyperproliferative...
8.
Siu T, Kumarasinghe S, Altman M, Katcher M, Northrup A, White C, et al.
Bioorg Med Chem Lett
. 2014 Mar;
24(6):1466-71.
PMID: 24582987
This communication discusses the discovery of novel reverse tricyclic pyridones as inhibitors of Janus kinase 2 (JAK2). By using a kinase cross screening approach coupled with molecular modeling, a unique...
9.
Northrup A, Katcher M, Altman M, Chenard M, Daniels M, Deshmukh S, et al.
J Med Chem
. 2013 Feb;
56(6):2294-310.
PMID: 23379595
This report documents the first example of a specific inhibitor of protein kinases with preferential binding to the activated kinase conformation: 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one 11r (MK-8033), a dual c-Met/Ron inhibitor under investigation...
10.
Lim J, Taoka B, Otte R, Spencer K, Dinsmore C, Altman M, et al.
J Med Chem
. 2011 Sep;
54(20):7334-49.
PMID: 21942426
The JAK-STAT pathway mediates signaling by cytokines, which control survival, proliferation, and differentiation of a variety of cells. In recent years, a single point mutation (V617F) in the tyrosine kinase...