Zobrazeno 1 - 10 of 40 pro vyhledávání: '"David S. Huang"'
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Akademický článek
Structural basis for species-selective targeting of Hsp90 in a pathogenic fungus
Autor: Luke Whitesell, Nicole Robbins, David S. Huang, Catherine A. McLellan, Tanvi Shekhar-Guturja, Emmanuelle V. LeBlanc, Catherine S. Nation, Raymond Hui, Ashley Hutchinson, Cathy Collins, Sharanya Chatterjee, Richard Trilles, Jinglin L. Xie, Damian J. Krysan, Susan Lindquist, John A. Porco, Utpal Tatu, Lauren E. Brown, Juan Pizarro, Leah E. Cowen
Publikováno v: Nature Communications, Vol 10, Iss 1, Pp 1-17 (2019)
The chaperone Hsp90 is a potential target for the development of drugs against fungal pathogens. Here the authors determine the structure of the Hsp90 nucleotide-binding domain from Candida albicans, which they use to design an inhibitor and demonstr
Externí odkaz: https://doaj.org/article/c204109fbee74209af84981ef754b8a6
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2
Identification of the Metabolic Profile of the α-Tubulin-Binding Natural Product (−)–Pironetin
Autor: Gunda I. Georg, Henry L. Wong, Sara K. Coulup, David S. Huang
Publikováno v: Journal of Medicinal Chemistry. 62:1684-1689
Pironetin, the only crystallographically confirmed natural product to target α-tubulin, displays potent cytotoxic activity against sensitive and resistant A2780 ovarian cancer cell lines but is only marginally active in vivo. We now report that piro
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ed6dfd45e73c9e892b2d1c6547d56bf9
https://doi.org/10.1021/acs.jmedchem.8b01774
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3
Cytotoxicity of phenylpironetin analogs and the metabolic fate of pironetin and phenylpironetin
Autor: Md Abdullah Al Noman, David S. Huang, Sara K. Coulup, Shameem Sultana Syeda, null Henry, L. Wong, Gunda I. Georg
Publikováno v: Bioorganic Chemistry. 125:105915
To improve pironetin's metabolic stability we prepared four analogs by replacing its C12-14 segment with an aryl group. The antiproliferative activity of phenyl analog 4 was reduced two-fold and dihydroxy-4-fluorophenyl analog 5 was slightly more eff
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c03aedfe2fc0a80bd5e7823723c1cd24
https://doi.org/10.1016/j.bioorg.2022.105915
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5
Synthesis and Cytotoxicity Evaluation of C4‐ and C5‐Modified Analogues of the α,β‐Unsaturated Lactone of Pironetin
Autor: Henry L. Wong, Gunda I. Georg, David S. Huang
Publikováno v: Chemmedchem
Pironetin is a natural product with potent antiproliferative activity that forms a covalent adduct with α‐tubulin via conjugate addition into the natural product's α,β‐unsaturated lactone. Although pironetin's α,β‐unsaturated lactone is in
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9b18bea5f2f051756cf8d4ede73244c5
http://europepmc.org/articles/PMC5413833
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6
Design and synthesis of fungal-selective resorcylate aminopyrazole Hsp90 inhibitors
Autor: Leah E. Cowen, Luke Whitesell, Lauren E. Brown, Tanvi Shekhar-Guturja, Emmanuelle V. LeBlanc, Juan C. Pizarro, Nicole Robbins, Damian J. Krysan, David S. Huang
Publikováno v: J Med Chem
The molecular chaperone Hsp90, essential in all eukaryotes, plays a multifaceted role in promoting survival, virulence, and drug resistance across diverse pathogenic fungal species. The chaperone is also critically important, however, to the pathogen
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::563736a5ed4e9072ba00f6494461a988
https://europepmc.org/articles/PMC7069776/
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7
Structural basis for species-selective targeting of Hsp90 in a pathogenic fungus
Autor: Nicole Robbins, Damian J. Krysan, Catherine A. McLellan, David S. Huang, Catherine S. Nation, Tanvi Shekhar-Guturja, Emmanuelle V. LeBlanc, Luke Whitesell, Ashley Hutchinson, Cathy Collins, John A. Porco, Raymond Hui, Leah E. Cowen, Richard Trilles, Utpal Tatu, Jinglin L. Xie, Lauren E. Brown, Juan C. Pizarro, Sharanya Chatterjee, Susan Lindquist
Publikováno v: Nature Communications, Vol 10, Iss 1, Pp 1-17 (2019)
Nature Communications
New strategies are needed to counter the escalating threat posed by drug-resistant fungi. The molecular chaperone Hsp90 affords a promising target because it supports survival, virulence and drug-resistance across diverse pathogens. Inhibitors of hum
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fd06c64a48751b5a45513a82976781a8
https://igi.indrastra.com/items/show/195861
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8
Synthesis and evaluation of C2 functionalized analogs of the α-tubulin-binding natural product pironetin
Autor: David S. Huang, Henry L. Wong, Gunda I. Georg
Publikováno v: Bioorganicmedicinal chemistry letters. 28(16)
Pironetin is an α-tubulin-binding natural product with potent antiproliferative activity against several cancer cell lines that inhibits cell division by forming a covalent adduct with α-tubulin via a Michael addition into the natural product’s
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b25acb33a086f262c8f4d3401b656f75
https://pubmed.ncbi.nlm.nih.gov/29138028
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10
Novel Bisaryl Substituted Thiazoles and Oxazoles as Highly Potent and Selective Peroxisome Proliferator-Activated Receptor δ Agonists
Autor: Tracy A. Spalding, Enrique Saez, Yongping Xie, Andrea Gerken, Robert Epple, Vân T. B. Nguyêñ-Trân, Xing Wang, Donald S. Karanewsky, Cara Cuc Ngo, David S. Huang, Christopher Cow, Ross Russo, John Wityak, Tove Tuntland, H. Martin Seidel, Shin-Shay Tian, Mihai Azimioara, Maya Iskandar
Publikováno v: Journal of Medicinal Chemistry. 53:77-105
The discovery, synthesis, and optimization of compound 1 from a high-throughput screening hit to highly potent and selective peroxisome proliferator-activated receptor delta (PPARdelta) agonists are reported. The synthesis and structure-activity rela
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::489777559d3d46598f5c54e284a36080
https://doi.org/10.1021/jm9007399
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