Zobrazeno 1 - 10
of 23
pro vyhledávání: '"David J. Maloney"'
Autor:
Adam Yasgar, David J. Maloney, Leggy A. Arnold, Ganesha Rai, Anton Simeonov, Preetpal S. Sidhu, Ajit Jadhav, Kelly A. Teske, Premchendar Nandhikonda, Belaynesh Feleke
Publikováno v:
ACS Combinatorial Science. 19:646-656
We describe the parallel synthesis of novel analogs of GW0742, a peroxisome proliferator-activated receptor δ (PPARδ) agonist. For that purpose, modified reaction conditions were applied, such as a solid-phase palladium-catalyzed Suzuki coupling. I
Autor:
Matthew D. Hall, Stephen C. Kales, John R. Shanks, Clayton B. Woodcock, Katherine Pohida, Ganesha Rai, Xin Xu, Xiaodong Cheng, Qin Chen, Bryan T. Mott, Xing Zhang, Daniel J. Jansen, David J. Maloney, Ajit Jadhav, Matthew G. Cyr, Xin Hu, Pranav Shah, John R. Horton, Xu Liu, Haian Fu, Paula M. Vertino, Mark J. Henderson, Anton Simeonov
The active sites of hundreds of human α-ketoglutarate (αKG) and Fe(II)-dependent dioxygenases are exceedingly well preserved, which challenges the design of selective inhibitors. We identified a noncatalytic cysteine (Cys481 in KDM5A) near the acti
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e1a9df54129d98fb0b1a05fc30b2f7bc
https://europepmc.org/articles/PMC6467790/
https://europepmc.org/articles/PMC6467790/
Autor:
Bryan T. Mott, Ganesha Rai, Stephen C. Kales, Kai Zhang, Daniel J. Jansen, Yuhong Fang, Xu Liu, Paula M. Vertino, John R. Shanks, David J. Maloney, Lizhen Wu, Ajit Jadhav, Xiaodong Cheng, Haian Fu, Xing Zhang, Anton Simeonov, Matthew D. Hall, Qin Yan, Katherine Pohida, Xin Hu, John R. Horton, Mark J. Henderson
Publikováno v:
Journal of medicinal chemistry. 61(7)
Isomers of chiral drugs can exhibit marked differences in biological activities. We studied the binding and inhibitory activities of 12 compounds against KDM5A. Among them are two pairs of enantiomers representing two distinct inhibitor chemotypes, n
Autor:
David J. Maloney, Anton Simeonov, Adam Yasgar, Giovanni Diaz, Edward H. Kerns, J. Brian Jameson, Diane K. Luci, Michael Holinstat, Theodore R. Holman, David A. Taylor-Fishwick, Kate Markham, Norine Kuhn, Ajit Jadhav, Netra Joshi, Steve Perry, Jennifer Yeung, Lena Schultz, Auric Kantz, Jerry L. Nadler
Publikováno v:
Journal of Medicinal Chemistry. 57:495-506
Human lipoxygenases (LOXs) are a family of iron-containing enzymes which catalyze the oxidation of polyunsaturated fatty acids to provide the corresponding bioactive hydroxyeicosatetraenoic acid (HETE) metabolites. These eicosanoid signaling molecule
Autor:
David J. Maloney, Ganesha Rai, Stephen C. Kales, John R. Shanks, Philip J. Webber, Xiaodong Cheng, Matthew D. Hall, Daniel J. Jansen, Xu Liu, Ajit Jadhav, Haian Fu, Lizhen Wu, John R. Horton, Xing Zhang, Anton Simeonov, Qin Yan, Mark J. Henderson, Joshua S.K. Bell, Margaret A. Johns, Bryan T. Mott, Paula M. Vertino, Daniel J. Urban, Molly Gale
Publikováno v:
Cell chemical biology. 23(7)
The KDM5/JARID1 family of Fe(II)- and α-ketoglutarate-dependent demethylases removes methyl groups from methylated lysine 4 of histone H3. Accumulating evidence supports a role for KDM5 family members as oncogenic drivers. We compare the in vitro in
Autor:
Michael Holinstat, David A. Taylor-Fishwick, David J. Maloney, J. Brian Jameson, Jerry L. Nadler, William Leister, Michelle Armstrong, Ganesha Rai, Theodore R. Holman, Netra Joshi, James M. Bougie, Ajit Jadhav, Lena Schultz, Steve Perry, Anton Simeonov, Victor Kenyon
Publikováno v:
Journal of Medicinal Chemistry. 54:5485-5497
We report the discovery of novel small molecule inhibitors of platelet type 12-human lipoxygenase, which display nanomolar activity against the purified enzyme, using a quantitative high throughput screen (qHTS) on a library of 153,607 compounds. The
Autor:
David J. Maloney, Craig J. Thomas, Juan J. Marugan, Bryan T. Mott, Min Shen, Tom Misteli, William Leister, James Inglese, Paul Shinn, Christopher P. Austin, Cordelle Tanega, Douglas S. Auld
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:6700-6705
A series of substituted 6-arylquinazolin-4-amines were prepared and analyzed as inhibitors of Clk4. Synthesis, structure-activity relationships and the selectivity of a potent analogue against a panel of 402 kinases are presented. Inhibition of Clk4
Publikováno v:
Angewandte Chemie International Edition. 46:7789-7792
Autor:
Sidney M. Hecht, David J. Maloney
Publikováno v:
Organic Letters. 7:4297-4300
[reaction: see text] A concise stereoselective total synthesis of a naturally occurring polymerase beta inhibitor, delta-trans-tocotrienoloic acid (2), is described. The key step in the synthesis is an acid-catalyzed cyclodehydration reaction. Additi
Autor:
Adam Yasgar, Michael D. Burkart, Thomas Daniel, Timothy L. Foley, Matias S. Attene-Ramos, William Leister, Ganesha Rai, Anton Simeonov, Nicolas M. Kosa, Ajit Jadhav, Heather L. Baker, David J. Maloney
Publikováno v:
Journal of Medicinal Chemistry
4'-Phosphopantetheinyl transferases (PPTases) catalyze a post-translational modification essential to bacterial cell viability and virulence. We present the discovery and medicinal chemistry optimization of 2-pyridinyl-N-(4-aryl)piperazine-1-carbothi