Výsledky vyhledávání - "Richard Soll"

Discovery and Structural Characterization of Small Molecule Binders of the Human CTLH E3 Ligase Subunit GID4

Publikováno v: Journal of Medicinal Chemistry. 65:12725-12746

Targeted protein degradation (TPD) strategies exploit bivalent small molecules to bridge substrate proteins to an E3 ubiquitin ligase to induce substrate degradation. Few E3s have been explored as degradation effectors due to a dearth of E3-binding s

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9e9bd44e2ad315c9a8487c6d1e86a88a
https://doi.org/10.1021/acs.jmedchem.2c00509

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Deep learning enables rapid identification of potent DDR1 kinase inhibitors

Publikováno v: Nature Biotechnology. 37:1038-1040

We have developed a deep generative model, generative tensorial reinforcement learning (GENTRL), for de novo small-molecule design. GENTRL optimizes synthetic feasibility, novelty, and biological activity. We used GENTRL to discover potent inhibitors

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::57935a11c69db73ee57db030f1e4ba3b
https://doi.org/10.1038/s41587-019-0224-x

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Development of a New Structural Class of Broadly Acting HCV Non‐Nucleoside Inhibitors Leading to the Discovery of MK‐8876

Autor: Richard Soll, Peng Li, Jin Wu, Peter T. Meinke, David B. Olsen, Anandan Palani, Ajay Ummat, Wei Chang, Nigel J. Liverton, M. Katharine Holloway, Xuanjia Peng, Casey C. Mccomas, Jie Wu, Charles A. Lesburg, Nicolas Zorn, Steven W. Ludmerer

Publikováno v: ChemMedChem. 12:1436-1448

Studies directed at developing a broadly acting non-nucleoside inhibitor of HCV NS5B led to the discovery of a novel structural class of 5-aryl benzofurans that simultaneously interact with both the palm I and palm II binding regions. An initial cand

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::10b371b4c60faeab68df38952d1991a2
https://doi.org/10.1002/cmdc.201700228

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Design, Synthesis, and Evaluation of Prodrugs of Ertapenem

Autor: Richard Soll, Sheo B. Singh, Peter T. Meinke, Wanying Sun, Lovji D. Cama, Li Wang, Deborah A. Nicoll-Griffith, Michael J. Hafey, Hongshi Yu, Takao Suzuki, Hao Wu, Diane Rindgen, Basheng Zhang, David B. Olsen, Nengxue Wang, Bradley Prudence K, Chongmin Ji

Publikováno v: ACS Medicinal Chemistry Letters. 4:715-719

Carbapenems are intravenous lifesaving hospital antibiotics. Once patients leave the hospital, they are sent home with antibiotics other than carbapenems since they cannot be administered orally due to lack of oral absorption primarily because of ver

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::94296f59abf183723a6a4c18232ff8f9
https://doi.org/10.1021/ml400092n

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Alternative core development around the tetracyclic indole class of HCV NS5A inhibitors

Publikováno v: Bioorganicmedicinal chemistry letters. 26(20)

Herein, we describe our research efforts to develop unique cores in molecules which function as HCV nonstructural protein 5A (NS5A) inhibitors. In particular, various fused tetracyclic cores were identified which showed genotype and mutant activities

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3c44dc14e3baf5b21019c48ab0792245
https://pubmed.ncbi.nlm.nih.gov/27634194

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Design and synthesis of polyethylene glycol-modified biphenylsulfonyl-thiophene-carboxamidine inhibitors of the complement component C1s

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 22:5303-5307

Complement C1s protease inhibitors have potential utility in the treatment of diseases associated with activation of the classical complement pathway such as humorally mediated graft rejection, ischemia-reperfusion injury (IRI), vascular leak syndrom

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::44891a19d07c75d5617cf44b0ba3e337
https://doi.org/10.1016/j.bmcl.2012.06.030

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Aerosolized Phosphoinositide 3-Kinase γ/δ Inhibitor TG100-115 [3-[2,4-Diamino-6-(3-hydroxyphenyl)pteridin-7-yl]phenol] as a Therapeutic Candidate for Asthma and Chronic Obstructive Pulmonary Disease

Autor: Dellamary Luis A, Glenn Noronha, John A. Doukas, Lisa Eide, Karin Stebbins, Lisette M. Acevedo, Wolfgang Wrasidlo, David A. Cheresh, Elena Dneprovskaia, Richard Soll, Adrienne Racanelli-Layton, Michael D. Martin

Publikováno v: Journal of Pharmacology and Experimental Therapeutics. 328:758-765

Phosphatidylinositol 3-kinases (PI3Ks) are key elements in the signaling cascades that lie downstream of many cellular receptors. In particular, PI3K delta and gamma isoforms contribute to inflammatory cell recruitment and subsequent activation. For

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::706df9f9b0e25d1201d46d3c4905ff35
https://doi.org/10.1124/jpet.108.144311

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Topical administration of a multi-targeted kinase inhibitor suppresses choroidal neovascularization and retinal edema

Autor: Jon Cao, Naoyasu Umeda, Shu Kachi, Katsutoshi Yokoi, Dellamary Luis A, Betty Tam, John Doukas, Adrienne Racanelli-Layton, Michael D. Martin, Hideo Akiyama, Zoe Chen, Sankaranarayana Pillai Mahesh, Peter A. Campochiaro, Glenn Noronha, Richard Soll, John Hood

Publikováno v: Journal of Cellular Physiology. 216:29-37

Age-related macular degeneration, diabetic retinopathy, and retinal vein occlusions are complicated by neovascularization and macular edema. Multi-targeted kinase inhibitors that inhibit select growth factor receptor tyrosine kinases and/or component

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c41fe9c637c4fbadbc0bab0c4a181cb3
https://doi.org/10.1002/jcp.21426

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Cyclic Conversion of the Novel Src Kinase Inhibitor [7-(2,6-Dichloro-phenyl)-5-methyl-benzo[1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-amine (TG100435) and Its N-Oxide Metabolite by Flavin-Containing Monoxygenases and Cytochrome P450 Reductase

Autor: Ahmed A Kousba, Shiyin Yee, Michael Martin, Richard Soll

Publikováno v: Drug Metabolism and Disposition. 35:2242-2251

[7-(2,6-Dichloro-phenyl)-5-methyl-benzo[1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-amine (TG100435) is a novel multi-targeted Src family kinase inhibitor with demonstrated anticancer activity in preclinical species. Potent kinase inhib

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::d6bc1dfd24324742b024735098dc3325
https://doi.org/10.1124/dmd.107.017384

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