Výsledky vyhledávání - "Dawn M. George"

Akademický článek

Prodrugs for colon-restricted delivery: Design, synthesis, and in vivo evaluation of colony stimulating factor 1 receptor (CSF1R) inhibitors.

Autor: Dawn M George, Raymond J Huntley, Kevin Cusack, David B Duignan, Michael Hoemann, Jacqueline Loud, Regina Mario, Terry Melim, Kelly Mullen, Gagandeep Somal, Lu Wang, Jeremy J Edmunds

Publikováno v: PLoS ONE, Vol 13, Iss 9, p e0203567 (2018)

The ability to restrict low molecular weight compounds to the gastrointestinal (GI) tract may enable an enhanced therapeutic index for molecular targets known to be associated with systemic toxicity. Using a triazolopyrazine CSF1R inhibitor scaffold,

Externí odkaz: https://doaj.org/article/f9e4d7a1ef864cb18c1b355c36fdb091

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Prodrugs for colon-restricted delivery: Design, synthesis, and in vivo evaluation of colony stimulating factor 1 receptor (CSF1R) inhibitors

Autor: Kevin P. Cusack, David B. Duignan, Jacqueline Loud, Michael Z. Hoemann, Lu Wang, Kelly D. Mullen, Regina Mario, Jeremy J. Edmunds, Dawn M. George, Gagandeep Somal, Raymond Huntley, Terry Melim

Publikováno v: PLoS ONE, Vol 13, Iss 9, p e0203567 (2018)
PLoS ONE

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fb4342c0d0784cf989301c8a18f47c3a
http://europepmc.org/articles/PMC6128612?pdf=render

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Structure activity optimization of 6H-pyrrolo[2,3-e][1,2,4]triazolo[4,3-a]pyrazines as Jak1 kinase inhibitors

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 25:4399-4404

Previous work investigating tricyclic pyrrolopyrazines as kinase cores led to the discovery that 1-cyclohexyl-6H-pyrrolo[2,3-e][1,2,4]triazolo[4,3-a]pyrazine (12) had Jak inhibitory activity. Herein we describe our initial efforts to develop orally b

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8d4901230904cbadeac613bde22f9aa3
https://doi.org/10.1016/j.bmcl.2015.09.020

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Discovery of thieno[2,3-c]pyridines as potent COT inhibitors

Autor: Jose-Andres Salmeron, Kevin P. Cusack, Dawn M. George, Thomas D. Gordon, Michael Friedman, Bernd Janssen, Agnieszka Bischoff, Claude Barberis, Woller Kevin R, Yong Jia, Neil Wishart, Shannon R. Fix-Stenzel, Richard W. Dixon, Christopher Quinn, Maria A. Argiriadi, Zhengtian Yu, Anca Clabbers, Hamish Allen, Maria D Moskey

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 18:4952-4955

Evaluation of hit chemotypes from high throughput screening identified a novel series of 2,4-disubstituted thieno[2,3-c]pyridines as COT kinase inhibitors. Structural modifications exploring SAR at the 2- and 4-positions resulting in inhibitors with

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dbf9f19003a922c321db0fa9412b49ff
https://doi.org/10.1016/j.bmcl.2008.08.037

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Optimized protein kinase Cθ (PKCθ) inhibitors reveal only modest anti-inflammatory efficacy in a rodent model of arthritis

Autor: Pratima Bansal-Pakala, David B. Duignan, QingYu Lang, Lian Rundell, Eric C. Breinlinger, Jianfei Wang, Scott W. Mittelstadt, Yang Zhang, Annette Schwartz, Jiakang Sun, Maria A. Argiriadi, P. Honore, Jeremy J. Edmunds, Dawn M. George

Publikováno v: Journal of medicinal chemistry. 58(1)

We previously demonstrated that selective inhibition of protein kinase Cθ (PKCθ) with triazinone 1 resulted in dose-dependent reduction of paw swelling in a mouse model of arthritis.1,2 However, a high concentration was required for efficacy, thus

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2cb3afcba5aae2b6746c954032c8e149
https://pubmed.ncbi.nlm.nih.gov/25254961

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Discovery of selective and orally bioavailable protein kinase Cθ (PKCθ) inhibitors from a fragment hit

Autor: Lian Rundell, Dominique Potin, Martine Barth, Yang Zhang, Jianfei Wang, Pratima Bansal-Pakala, Michael Friedman, Maria A. Argiriadi, QingYu Lang, David B. Duignan, Eric C. Breinlinger, Scott W. Mittelstadt, Jeremy J. Edmunds, Dawn M. George, P. Honore

Publikováno v: Journal of medicinal chemistry. 58(1)

Protein kinase Cθ (PKCθ) regulates a key step in the activation of T cells. On the basis of its mechanism of action, inhibition of this kinase is hypothesized to serve as an effective therapy for autoimmune diseases such as rheumatoid arthritis (RA

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::acc66c8e424479ef51abc03dde2fafe3
https://pubmed.ncbi.nlm.nih.gov/25000588

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Identification of a selective thieno[2,3-c]pyridine inhibitor of COT kinase and TNF-alpha production

Publikováno v: Bioorganicmedicinal chemistry letters. 19(6)

COT (Tpl2 in mice) is a serine/threonine MAP3 kinase that regulates production of TNF-alpha and other pro-inflammatory cytokines such as IL-1beta via the ERK/MAP kinase pathway. As TNF-alpha and IL-1beta are clinically validated targets for therapeut

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::50f181a4a20bde9e1eb2381df4be8001
https://pubmed.ncbi.nlm.nih.gov/19217782

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