Zobrazeno 1 - 10
of 59
pro vyhledávání: '"Michael A. Patane"'
Autor:
Bharat Lagu, Eric L. Bell, Effie Tozzo, Nirbhay Kumar Tiwari, Andrew Basinski, Arthur F. Kluge, Matthew M. Goddeeris, Ramesh S. Senaiar, Narasimha Rao Krishnamurthy, Ross Fredenburg, Sunil Kumar Panigrahi, Michael A. Patane, Mahaboobi Jaleel, Taisuke Takahashi, Peter Dwyer
Publikováno v:
ACS Medicinal Chemistry Letters. 9:935-940
The X-ray structure of the previously reported PPARδ modulator 1 bound to the ligand binding domain (LBD) revealed that the amide moiety in 1 exists in the thermodynamically disfavored cis-amide orientation. Isosteric replacement of the cis-amide wi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::0663921ac4e0f062d40544f2aece30db
https://doi.org/10.1021/acsmedchemlett.8b00287
https://doi.org/10.1021/acsmedchemlett.8b00287
Autor:
Ross Fredenburg, Matthew M. Goddeeris, Shekar Chellur, Ramesh S. Senaiar, Bharat Lagu, Mahaboobi Jaleel, Michael A. Patane, Nirbhay Kumar Tiwari, D. Ravi Krishna Babu, Arthur F. Kluge, Taisuke Takahashi, Effie Tozzo
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:533-536
Compound 1 regulates significantly fewer genes than the PPARδ modulator, GW501516. Both compounds are efficacious in a thermal injury model of muscle regeneration. The restricted gene profile of 1 relative to GW501516 suggests that 1 may be pharmaco
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::80494cd1dc0ce8e0d6d599fa2dca230c
https://doi.org/10.1016/j.bmcl.2017.11.006
https://doi.org/10.1016/j.bmcl.2017.11.006
Autor:
David L. McElligott, Albert Lai, Alexandre Nesterov, Robert A. Mantei, T. Matthew Hansen, Peter de Vries, Arthur F. Kluge, Ronen Marmorstein, Michael R. Michaelides, Hong Liu, Kesicki Edward A, Kannan R. Karukurichi, J. William Langston, John H. Van Drie, Loren M. Lasko, Carmen Hertel, Michael A. Patane, Kenneth D. Bromberg, Ce Wang, Philip A. Cole, Roberto M. Risi
Publikováno v:
ACS Medicinal Chemistry Letters
p300 and its paralog CBP can acetylate histones and other proteins and have been implicated in a number of diseases characterized by aberrant gene activation, such as cancer. A novel, highly selective, orally bioavailable histone acetyltransferase (H
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ea72017a0bf311573c69bf7322aa291f
https://doi.org/10.1021/acsmedchemlett.7b00395
https://doi.org/10.1021/acsmedchemlett.7b00395
Autor:
Loren M. Lasko, Clarissa G. Jakob, Rohinton P. Edalji, Wei Qiu, Debra Montgomery, Enrico L. Digiammarino, T. Matt Hansen, Roberto M. Risi, Robin Frey, Vlasios Manaves, Bailin Shaw, Mikkel Algire, Paul Hessler, Lloyd T. Lam, Tamar Uziel, Emily Faivre, Debra Ferguson, Fritz G. Buchanan, Ruth L. Martin, Maricel Torrent, Gary G. Chiang, Kannan Karukurichi, J. William Langston, Brian T. Weinert, Chunaram Choudhary, Peter de Vries, Arthur F. Kluge, Michael A. Patane, John H. Van Drie, Ce Wang, David McElligott, Ed Kesicki, Ronen Marmorstein, Chaohong Sun, Philip A. Cole, Saul H. Rosenberg, Michael R. Michaelides, Albert Lai, Kenneth D. Bromberg
Publikováno v:
Nature. 550:128-132
The dynamic and reversible acetylation of proteins, catalysed by histone acetyltransferases (HATs) and histone deacetylases (HDACs), is a major epigenetic regulatory mechanism of gene transcription and is associated with multiple diseases. Histone de
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1fcdc4d0d1efd86b44451095a833f08b
https://doi.org/10.1038/nature24028
https://doi.org/10.1038/nature24028
Autor:
Raveendra Bhat, Arthur F. Kluge, M. Ramakrishna, B. Mallesh, Ramesh S. Senaiar, Michael A. Patane, Bharat Lagu
Publikováno v:
Bioorganicmedicinal chemistry letters. 30(4)
One of the most commonly used strategies to reduce hERG (human ether-a-go-go) activity in the drug candidates is introduction of a carboxylic acid group. During the optimization of PPARδ modulators, some of the compounds containing a carboxylic acid
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c003dfd546435ed2170f7388ca90affb
https://pubmed.ncbi.nlm.nih.gov/31889664
https://pubmed.ncbi.nlm.nih.gov/31889664
Autor:
Mahaboobi Jaleel, Matthew M. Goddeeris, Ramesh S. Senaiar, Peter Dwyer, Eric L. Bell, Sunil Kumar Panigrahi, Ross Fredenburg, Bharat Lagu, Narasimha Rao Krishnamurthy, Andrew Basinski, Michael A. Patane, Nirbhay Kumar Tiwari, Taisuke Takahashi, Effie Tozzo, Arthur F. Kluge
[Image: see text] The X-ray structure of the previously reported PPARδ modulator 1 bound to the ligand binding domain (LBD) revealed that the amide moiety in 1 exists in the thermodynamically disfavored cis-amide orientation. Isosteric replacement o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6579f783424d3bdf0cdce8fc284c2809
https://europepmc.org/articles/PMC6580794/
https://europepmc.org/articles/PMC6580794/
Autor:
Nicolas Bruneau-Latour, Gerald W. Shipps, Chantal Grand-Maître, Martin Dery, Vibha Oza, Michael A. Luther, Lea Constantineau-Forget, Stephane Ciblat, Michael A. Patane, Jedd Levine, Edith Bellavance, Matthew J. Kostura, Alan B. Cooper, Arshad Siddiqui
Publikováno v:
Bioorganicmedicinal chemistry letters. 28(5)
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::027ff0f55fdb19838d200a517fc88271
https://pubmed.ncbi.nlm.nih.gov/28844391
https://pubmed.ncbi.nlm.nih.gov/28844391
Autor:
Sunil Kumar Panigrahi, Effie Tozzo, Narasimha Rao Krishnamurthy, Taisuke Takahashi, Mahaboobi Jaleel, Nirbhay Kumar Tiwari, Bharat Lagu, Michael A. Patane, Ramesh S. Senaiar, Ross Fredenburg, Arthur F. Kluge
Publikováno v:
Bioorganicmedicinal chemistry letters. 27(23)
Optimization of benzamide PPARδ modulator 1 led to (E)-6-(2-((4-(furan-2-yl)-N-methylbenzamido)methyl)phenoxy)-4-methylhex-4-enoic acid (18), a potent selective PPARδ modulator with significantly improved exposure in multiple species following oral
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2f57037ac6e56607083a4697cf927ed4
https://pubmed.ncbi.nlm.nih.gov/29103972
https://pubmed.ncbi.nlm.nih.gov/29103972
Autor:
Arshad Siddiqui, Chantal Grand-Maître, Alan B. Cooper, Martin Dery, Edith Bellavance, Stephane Ciblat, Michael A. Luther, Matthew J. Kostura, Nicolas Bruneau-Latour, Vibha Oza, Michael A. Patane, Gerald W. Shipps, Lea Constantineau-Forget, Jedd Levine
Publikováno v:
Bioorganicmedicinal chemistry letters. 27(18)
A class of substituted 1-thiazol-2-yl-N-3-methyl-1H-pyrozole-5-carboxylic acid derivatives was found to have potent anti-proliferative activity against a broad range of tumor cell lines. A compound from this class (14) was profiled across a broad pan
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a1299a7a6b92309cde33ee679c02518d
https://pubmed.ncbi.nlm.nih.gov/29433931
https://pubmed.ncbi.nlm.nih.gov/29433931
Autor:
JoAnne Dzink-Fox, Jason T. Brewer, Esther K. Schmitt, Karl Dean, Matthew J. LaMarche, Stacey Tiamfook, Gabe Gamber, Zachary Robinson, Jennifer A. Leeds, Michael A. Patane, Deborah Palestrant, Colin Osborne, Franco Lombardo, Akash K. Jain, David McKenney, Jian Ding, Lewis Whitehead, Philipp Krastel, Elin M. Rann, Travis Stams, Donghui Yu, Ryan Kerrigan, Georg Neckermann, Kwangho Lee
Publikováno v:
Journal of medicinal chemistry. 59(14)
Synthetic studies of the antimicrobial secondary metabolite thiomuracin A (1) provided access to analogues in the Northern region (C2–C10). Selective hydrolysis of the C10 amide of lead compound 2 and subsequent derivatization led to novel carbon-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::86e6e2e5b9088dc74bc09de581c51bc2
https://pubmed.ncbi.nlm.nih.gov/27355833
https://pubmed.ncbi.nlm.nih.gov/27355833