Výsledky vyhledávání - "Stephen L Gwaltney"

Abstract 4964: SW-682: A novel TEAD inhibitor for the treatment of cancers bearing mutations in the Hippo signaling pathway

Autor: Lei Chen, Paula Milani de Marval, Kendall Powell, Mark Johnson, Greg Falls, Brian Lawhorn, Aurélie Candi, Amuri Kilonda, Bart Vanderhoydonck, Arnaud Marchand, Matthias Versele, Georg Halder, Stephen L. Gwaltney, Adeela Kamal

Publikováno v: Cancer Research. 83:4964-4964

Many cancers harbor mutations in the Hippo pathway that lead to constitutive activation of the transcriptional co-activators YAP/TAZ that then bind the transcription factor TEAD and drive aberrant transcription of target genes involved in cell prolif

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::ff72fff7f3b3f1feb5934f47b68973aa
https://doi.org/10.1158/1538-7445.am2023-4964

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Abstract 3945: Novel antagonists of TEAD palmitoylation inhibit the growth of Hippo-altered cancers in preclinical models

Autor: Adeela Kamal, Aurélie Candi, Matthias Versele, Bart Vanderhoydonck, Arnaud Marchand, Ron de Jong, Thuy Hoang, Georg Halder, Patrick Chaltin, Stephen L. Gwaltney, Mike Burgess

Publikováno v: Cancer Research. 82:3945-3945

Background: The Hippo pathway is an evolutionarily conserved signaling cascade whose deregulation can promote excessive cell proliferation and tumor development. Pathway output is mediated by the YAP and TAZ transcriptional co-activators, which bind

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::6c4509ba65fd9177d8f75b5e6f63729b
https://doi.org/10.1158/1538-7445.am2022-3945

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Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators

Autor: Petro Halkowycz, Zacharia Cheruvallath, Mark Sabat, Bumsup Lee, David J. Hosfield, Andrew John Jennings, Haixia Wang, Mingnam Tang, Stephen L. Gwaltney, Yiqin Wu, Charles E. Grimshaw

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 27:2678-2682

Guided by co-crystal structural information obtained from a different series we were exploring, a scaffold morphing and SBDD approach led to the discovery of the 1,4-disubstituted indazole series as a novel class of GKAs that potently activate GK in

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7ed0d84b42b1111c1cc3b8ded9c30c17
https://doi.org/10.1016/j.bmcl.2017.04.041

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Design, synthesis and SAR of novel glucokinase activators

Autor: Stephen L. Gwaltney, Mark Sabat, Yiqin Wu, Zacharia Cheruvallath, Bumsup Lee, Prasuna Guntupalli, David J. Hosfield, Andrew John Jennings, Jun Feng, Mingnam Tang, Joanne Miura, Haixia Wang

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 23:2166-2171

Guided by co-crystal structures of compounds 15, 22 and 30, an SBDD approach led to the discovery of the 6-methyl pyridone series as a novel class of GKAs that potently activate GK in enzyme and cell assays. Anti-diabetic OGTT efficacy was demonstrat

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c80f2c14ec87914050c121438173989f
https://doi.org/10.1016/j.bmcl.2013.01.093

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Structure-based design of pyridopyrimidinediones as dipeptidyl peptidase IV inhibitors

Autor: Robert J. Skene, Stephen L. Gwaltney, Betty Lam, Lihong Shi, Jeffery A. Stafford, Zhiyuan Zhang

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 22:6628-6631

Dipeptidyl peptidase IV (DPP-4) inhibitors have been shown to enhance GLP-1 levels and thereby improve hyperglycemia in type II diabetes. From a small fragment hit, using structure-based design, we have discovered a new class of non-covalent, potent

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8eb5d4fc25b8eb4d379152b0d051e114
https://doi.org/10.1016/j.bmcl.2012.08.110

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Structure-based design and synthesis of benzimidazole derivatives as dipeptidyl peptidase IV inhibitors

Autor: Christopher L. Caster, Michael B. Wallace, Rongda Xu, Daniel B. Kassel, Jun Feng, Lihong Shi, Stephen L. Gwaltney, Zhiyuan Zhang, Robert J. Skene

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 18:2362-2367

A novel series of non-covalent, benzimidazole-based inhibitors of DPP-4 has been developed from a small fragment hit using structure-based drug design. A highly versatile synthetic route was created for the development of SAR, which led to the discov

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5af34c70552c6b3d1b8fdeaf7c4e07bc
https://doi.org/10.1016/j.bmcl.2008.02.071

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Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors

Autor: Hing L. Sham, Russell A. Judge, Akiyo Claiborne, Thomas J. Sowin, Haiying Zhang, Stephen L. Gwaltney, Nan-Horng Lin, Kent D. Stewart, Yunsong Tong, Chang Park, Saul H. Rosenberg, Peter Kovar, Zehan Chen, Wen-Zhen Gu, Robert B. Credo

Publikováno v: Bioorganic & Medicinal Chemistry. 15:2759-2767

A new class of checkpoint kinase 1 (CHK-1) inhibitors bearing a 1,4-dihydroindeno[1,2-c]pyrazole core was developed after initial hits from high throughput screening. The efficient hit-to-lead process was facilitated by X-ray crystallography and led

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7ae47e5b591d4943cf0905bb26642807
https://doi.org/10.1016/j.bmc.2007.01.012

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Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 13:1359-1362

Inhibitors of farnesyltransferase are effective against a variety of tumors in mouse models of cancer. Clinical trials to evaluate these agents in humans are ongoing. In our effort to develop new farnesyltransferase inhibitors, we have discovered a s

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bace2fe027ea17136753c78626be974f
https://doi.org/10.1016/s0960-894x(03)00095-7

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