Zobrazeno 1 - 10
of 23
pro vyhledávání: '"David B. Belanger"'
Autor:
Yves A. Millet, Jeffrey Meisner, Jie Tan, Adarsh Jose, Eric Humphries, Kelsey J. Miller, Charlie Bayne, Megan McComb, Michael Giuggio, Camille M. Konopnicki, David B. Belanger, Lingyao Li, Han Yuan, Madeline Rosini, Hoa Luong, Jared Martin, Zhengzheng Pan, C. Ronald Kahn, Johan E.T. van Hylckama Vlieg
BackgroundIncreasing evidence indicates that an altered gut microbiome participates in the development of cardiometabolic syndrome and associated risk factors, such as insulin resistance, dyslipidemia, and obesity, and that targeting the gut microbio
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::993eed8e5e811a71998422c0f115fd65
https://doi.org/10.1101/2022.04.04.487010
https://doi.org/10.1101/2022.04.04.487010
Autor:
Christopher M. Adams, Catherine Solovay, Muneto Mogi, Byron Li, Doug Bevan, Mitsunori Kato, Jonathan E. Grob, Erik Meredith, David B. Belanger, Powers James J, Philippe Bolduc, Louis Yang, Nan Ji, Michael Paul Capparelli, Donglei Liu, Christopher Towler, Ganesh Prasanna, Matthew H. Daniels, Takeru Ehara, Rebecca C. Stacy, Luciana Ferrara
Publikováno v:
Journal of Medicinal Chemistry. 61:2552-2570
Soluble guanylate cyclase (sGC), the endogenous receptor for nitric oxide (NO), has been implicated in several diseases associated with oxidative stress. In a pathological oxidative environment, the heme group of sGC can be oxidized becoming unrespon
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0c16c37de994217e68708053a88c17a0
https://doi.org/10.1021/acs.jmedchem.8b00007
https://doi.org/10.1021/acs.jmedchem.8b00007
Autor:
Anna Vulpetti, Upendra A. Argikar, Stefanie Flohr, Aengus Mac Sweeney, Melissa Prentiss, Edwige Lorthiois, Karen Anderson, David B. Belanger, Sha-Mei Liao, Nan Ji, Christopher M. Adams, Frederic Cumin, Andrea De Erkenez, Nathalie Gradoux, Muneto Mogi, Donglei Liu, Maura Crowley, Keith Jendza, Debby Long, Nello Mainolfi, Catherine Solovay, Ann Brown, Laura R. La Bonte, Rajeshri Ganesh Karki, Omar Delgado, Powers James J, Bruce D Jaffee, Christine F. Gelin
Publikováno v:
Journal of medicinal chemistry. 62(9)
Complement factor D (FD), a highly specific S1 serine protease, plays a central role in the amplification of the alternative complement pathway (AP) of the innate immune system. Dysregulation of AP activity predisposes individuals to diverse disorder
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::da588cee5e7843ba124041bcbf4f4b5e
https://pubmed.ncbi.nlm.nih.gov/30995036
https://pubmed.ncbi.nlm.nih.gov/30995036
Autor:
Ning Sui, Alan Hruza, Yushi Xiao, Ming Liu, Angela D. Kerekes, David B. Belanger, Andrea Basso, Matthew Paul Rainka, Tao Yu, Li-Kang Zhang, Jayaram R. Tagat, Lianzhu Liang, Matthew Ernst Voss, Yonglian Zhang, Doll Ronald J, Sara Esposite, Daniel Prelusky, Diane Rindgen
Publikováno v:
Bioorganicmedicinal chemistry letters. 28(8)
Imidazo-[1, 2-a]pyrazine 1 is a potent inhibitor of Aurora A and B kinase in vitro and is effective in in vivo tumor models, but has poor oral bioavailbility and is unsuitable for oral dosing. We describe herein our effort to improve oral exposure in
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9b6ebb786db353a9acedd5aacec90bd7
https://pubmed.ncbi.nlm.nih.gov/29545102
https://pubmed.ncbi.nlm.nih.gov/29545102
Autor:
Mike Fleming, David B. Belanger, Kimberly Gray, Matthew P. Rainka, Andrea D. Basso, M. Arshad Siddiqui, Matthew Ernst Voss, Johannes H. Voigt, Alan Hruza, Lisa H. Peterson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:3544-3549
The structure–activity relationships of new Aurora A/B kinase inhibitors derived from the previously identified kinase inhibitor 12 are described. Introduction of acetic acid amides onto the pyrazole of compound 12 was postulated to influence Auror
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8de034d96517afc96aac15977909ba4e
https://doi.org/10.1016/j.bmcl.2012.03.051
https://doi.org/10.1016/j.bmcl.2012.03.051
Autor:
Yan Wang, Patrick J. Curran, Jack B. Bracken, Gerald W. Shipps, M. Arshad Siddiqui, Hua Miao, David B. Belanger, Hongbo Zeng, Michael Malkowski
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:5870-5875
A series of substituted imidazo[1,2-a]pyrazin-8-amines were discovered as novel breast tumor kinase (Brk)/protein tyrosine kinase 6 (PTK6) inhibitors. Tool compounds with low-nanomolar Brk inhibition activity, high selectivity towards other kinases a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c602c45bbeb7b8ec30580b6a5d7bc119
https://doi.org/10.1016/j.bmcl.2011.07.101
https://doi.org/10.1016/j.bmcl.2011.07.101
Autor:
Jing Sun, Corey O. Strickland, John P. Caldwell, Kristin E. Rosner, Pauline C. Ting, Bandarpalle B. Shankar, Shiying Chen, David B. Belanger, Gerald W. Shipps, Vinay Girijavallabhan, Guowei Zhou, Brian J. Lavey, Dansu Li, Razia Rizvi, Peter Orth, Neng-Yang Shih, M. Arshad Siddiqui, Zhaoning Zhu, Wensheng Yu, Zhuyan Guo, Zhidan Liu, Maria David, John J. Piwinski, Daniel Lundell, Henry M. Vaccaro, Joe F. Lee, Jim Spitler, Vincent S. Madison, Xiaoda Niu, Chaoyang Dai, Mckittrick Brian A, Joseph A. Kozlowski, Janeta Popovici-Muller, Rob Mazzola
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:4812-4815
The syntheses and structure-activity relationships of the tartrate-based TACE inhibitors are discussed. The optimization of both the prime and non-prime sites led to compounds with picomolar activity. Several analogs demonstrated good rat pharmacokin
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::78b8670bf1029b4ff13b82406eff8483
https://doi.org/10.1016/j.bmcl.2010.06.104
https://doi.org/10.1016/j.bmcl.2010.06.104
Autor:
Neng-Yang Shih, David B. Belanger, Jennifer Jones, Mengwei Hu, Yushi Xiao, Patrick J. Curran, Andrea D. Basso, Elizabeth Smith, Angela Kerekes, Samad Ponery, Winifred W. Prosise, Lata Ramanathan, Jayaram R. Tagat, Johannes H. Voigt, Tao Yu, Yonglian Zhang, Doll Ronald J, Sara Esposite, M. Arshad Siddiqui, Lianzhu Liang, Ming Liu, Amit K. Mandal, Suining Lee, Seema Tevar, Kimberly Gray, Alan Hruza
Publikováno v:
ACS Medicinal Chemistry Letters. 1:214-218
The imidazo-[1,2-a]-pyrazine (1) is a dual inhibitor of Aurora kinases A and B with modest cell potency (IC50 = 250 nM) and low solubility (5 μM). Lead optimization guided by the binding mode led to the acyclic amino alcohol 12k (SCH 1473759), which
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bdb38c49ba025b07a5cfa2162b25788f
https://doi.org/10.1021/ml100063w
https://doi.org/10.1021/ml100063w
Publikováno v:
Synthesis. 2000:1009-1019
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::24989e21a7a6b35bd22726cfd83b921f
https://doi.org/10.1055/s-2000-6301
https://doi.org/10.1055/s-2000-6301
Publikováno v:
Tetrahedron Letters. 39:7637-7640
Heat alone has been found sufficient to promote intramolecular Pauson-Khand cyclizations catalyzed by high purity Co 2 (CO) 8 . The existence of a very narrow thermal window (e.g., 60 °C – 70 °C) for the attainment of efficient catalysis is a not
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::fbb467811fb9cf55b4071656b8fbacaf
https://doi.org/10.1016/s0040-4039(98)01693-1
https://doi.org/10.1016/s0040-4039(98)01693-1