Zobrazeno 1 - 10
of 67
pro vyhledávání: '"Kenneth W Bair"'
Autor:
Weiru Wang, Kristi Elkins, Angela Oh, Yen-Ching Ho, Jiansheng Wu, Hong Li, Yang Xiao, Mandy Kwong, Mary Coons, Bobby Brillantes, Eric Cheng, Lisa Crocker, Peter S Dragovich, Deepak Sampath, Xiaozhang Zheng, Kenneth W Bair, Thomas O'Brien, Lisa D Belmont
Publikováno v:
PLoS ONE, Vol 9, Iss 10, p e109366 (2014)
Inhibiting NAD biosynthesis by blocking the function of nicotinamide phosphoribosyl transferase (NAMPT) is an attractive therapeutic strategy for targeting tumor metabolism. However, the development of drug resistance commonly limits the efficacy of
Externí odkaz:
https://doaj.org/article/bb7aac885fbb499794f3ed2668eeafc5
Autor:
Zhongguo Wang, Goss Stryker Kauffman, Stephen Hubbs, Shawn Fessler, Lili Yao, Jennifer Castro, George P. Luke, Lu Wei, Mark T. Kershaw, Matthew W. Martin, Shawn Schiller, Crystal McKinnon, Angela V. Toms, Kenneth W. Bair, David S. Millan, David R. Lancia, Deepali Gotur, Li Hongbin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 29:1001-1006
The discovery, structure-activity relationships, and optimization of a novel class of fatty acid synthase (FASN) inhibitors is reported. High throughput screening identified a series of substituted piperazines with structural features that enable int
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a8e1607021e1e0b594aba77304e55e00
https://doi.org/10.1016/j.bmcl.2019.02.012
https://doi.org/10.1016/j.bmcl.2019.02.012
Autor:
K.J. Barr, A. Ericsson, Zhongguo Wang, David R. Lancia, A. Clarke, R.B. Diebold, S. Ashwell, George P. Luke, Deepali Gotur, Wei Lu, Jian Lin, H.R. Josephine, M. Katz, D. Walker, A.M. Campbell, Goss Stryker Kauffman, L. Yao, Angela V. Toms, Caravella Justin Andrew, H. Diep, Jennifer Castro, Kenneth W. Bair, E. Fritzen, Christopher J. Dinsmore, Stephen Hubbs, Le Wang, G.R. Gustafson, Tatiana E. Shelekhin, Mark T. Kershaw
Publikováno v:
Journal of medicinal chemistry. 62(14)
Mutations at the arginine residue (R132) in isocitrate dehydrogenase 1 (IDH1) are frequently identified in various human cancers. Inhibition of mutant IDH1 (mIDH1) with small molecules has been clinically validated as a promising therapeutic treatmen
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::74eee5a37b35c08111cdd42f3f0e0830
https://pubmed.ncbi.nlm.nih.gov/31199148
https://pubmed.ncbi.nlm.nih.gov/31199148
Autor:
Bianca M. Liederer, Xiaozhang Zheng, Kenneth W. Bair, Yen-Ching Ho, Timm Baumeister, Nicholas J. Skelton, Leslie Wang, Weiru Wang, Thomas O'Brien, Lei Zhang, Jason Oeh, Yuen Po-Wai, Yongbo Liu, Peter S. Dragovich, Deepak Sampath, Yang Xiao, Xiongcai Liu, Mark Zak, Hongxing Wu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:4875-4885
Potent nicotinamide phosphoribosyltransferase (NAMPT) inhibitors containing 2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-derived ureas were identified using structure-based design techniques. The new compounds displayed improved aqueous solubilities, determ
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d07d1b7abcd81817d6ba0a072a9a0a4a
https://doi.org/10.1016/j.bmcl.2013.06.090
https://doi.org/10.1016/j.bmcl.2013.06.090
Autor:
Janet Gunzner-Toste, Maureen Caligiuri, Nicholas J. Skelton, Jian Lin, Sophie Mukadam, Weiru Wang, Paul Bauer, Kenneth W. Bair, Xiaozhang Zheng, Karl H. Clodfelter, Bianca M. Liederer, Bang Fu, Thomas O'Brien, Zhongguo Wang, Peter S. Dragovich, Jasleen K. Sodhi, Lei Zhang, Geeta Sharma, Yen-Ching Ho, Chase C. Smith, Dominic J. Reynolds, Bingsong Han, Alexandre J. Buckmelter, Timm Baumeister, Angela Oh, Guiling Zhao, Nikolai Kley, Xiaorong Liang, Yang Xiao, Yuen Po-Wai, Mark Zak
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:3531-3538
Potent, reversible inhibition of the cytochrome P450 CYP2C9 isoform was observed in a series of urea-containing nicotinamide phosphoribosyltransferase (NAMPT) inhibitors. This unwanted property was successfully removed from the described inhibitors t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::01ca604ab818ff8d825e51214466d272
https://doi.org/10.1016/j.bmcl.2013.04.040
https://doi.org/10.1016/j.bmcl.2013.04.040
Autor:
Xiongcai Liu, Yuen Po-Wai, Deepak Sampath, Thomas O'Brien, Jasleen K. Sodhi, Lei Zhang, Nicholas J. Skelton, Weiru Wang, Yen-Ching Ho, Jason Oeh, Yang Xiao, Rongbao Hua, Mark Zak, Snahel Patel, Peter S. Dragovich, Kenneth W. Bair, Bianca M. Liederer, Xiaozhang Zheng, Yunli Wang, Guiling Zhao
Publikováno v:
Journal of medicinal chemistry. 59(18)
NAMPT inhibitors may show potential as therapeutics for oncology. Throughout our NAMPT inhibitor program, we found that exposed pyridines or related heterocyclic systems in the left-hand portion of the inhibitors are necessary pharmacophores for pote
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7263ace35dab76f6417d1cb00208e78e
https://pubmed.ncbi.nlm.nih.gov/27541271
https://pubmed.ncbi.nlm.nih.gov/27541271
Autor:
Meier Hsu, Kenneth W. Bair, Arthur W. Wu, Heather Walker, Richard William Versace, Lakshmi Yeleswarapu, Dalia Cohen, Alexander W. Wood, Paul Kwon, Nancy Trogani, Remiszewski Stacy W, Larry B Perez, Lin Gao, Nagarajan Chandramouli, Peter Atadja, Lidia Sambucetti, Peter T Lassota
Publikováno v:
Cancer Research. 64:689-695
We have synthesized a histone deacetylase inhibitor, NVP-LAQ824, a cinnamic hydroxamic acid, that inhibited in vitro enzymatic activities and transcriptionally activated the p21 promoter in reporter gene assays. NVP-LAQ824 selectively inhibited growt
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e4c23af39c1e7fa71191c24a13b72384
https://doi.org/10.1158/0008-5472.can-03-2043
https://doi.org/10.1158/0008-5472.can-03-2043
Autor:
Patrick Schindler, Anthony A. Morollo, Richard William Versace, Hans Voshol, Penny E. Phillips, Hyun Kyu Song, Frederick Ray Kinder, Kenneth W. Bair, James A. DeCaprio, Sunkyu Kim, Jeanette Marjorie Wood, Sonya Zabludoff, Michael J. Eck, Harry Towbin, Dieter Mueller, Jan van Oostrum
Publikováno v:
Journal of Biological Chemistry. 278:52964-52971
LAF389 is a synthetic analogue of bengamides, a class of marine natural products that produce inhibitory effects on tumor growth in vitro and in vivo. A proteomics-based approach has been used to identify signaling pathways affected by bengamides. LA
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::dc2177d41b19ffd4f676f4359e5325d9
https://doi.org/10.1074/jbc.m309039200
https://doi.org/10.1074/jbc.m309039200
Autor:
Stacy W. Remiszewski, Lidia C. Sambucetti, Kenneth W. Bair, John Bontempo, David Cesarz, Nagarajan Chandramouli, Ru Chen, Min Cheung, Susan Cornell-Kennon, Karl Dean, George Diamantidis, Dennis France, Michael A. Green, Kobporn Lulu Howell, Rina Kashi, Paul Kwon, Peter Lassota, Mary S. Martin, Yin Mou, Lawrence B. Perez, Sushil Sharma, Troy Smith, Eric Sorensen, Francis Taplin, Nancy Trogani, Richard Versace, Heather Walker, Susan Weltchek-Engler, Alexander Wood, Arthur Wu, Peter Atadja
Publikováno v:
Journal of Medicinal Chemistry. 46:4609-4624
A series of N-hydroxy-3-phenyl-2-propenamides were prepared as novel inhibitors of human histone deacetylase (HDAC). These compounds were potent enzyme inhibitors, having IC50s < 400 nM in a partially purified enzyme assay. However, potency in cell g
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::6e0206bc14fdb324b1acbdd17eeea9cc
https://doi.org/10.1021/jm030235w
https://doi.org/10.1021/jm030235w
Publikováno v:
Journal of the American Chemical Society. 124:2148-2152
A series of alpha-substituted beta-alanine (beta) linked polyamides (DbaPyPyPy-beta*-PyPyPy) were prepared and examined. This resulted in the observation that while most substituents disrupt DNA binding, (R)-alpha-methoxy-beta-alanine (beta((R)-OMe))
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0203703fb9ad1184c90141d9a5df0992
https://doi.org/10.1021/ja0122039
https://doi.org/10.1021/ja0122039