Zobrazeno 1 - 10
of 18
pro vyhledávání: '"David J. Maloney"'
Autor:
Matthew D. Hall, David J. Maloney, Amy Wang, Jeffrey W. Strovel, Makoto Yoshioka, Daniel J. Urban, Xin Xu, Shyh-Ming Yang, Pranav Shah, Ajit Jadhav, Steven Fletcher, Xin Hu
Publikováno v:
Bioorg Med Chem Lett
A new series of quinazoline-based analogs as potent bromodomain-containing protein 4 (BRD4) inhibitors is described. The structure-activity relationships on 2- and 4-position of quinazoline ring, and the substitution at 6-position that mimic the acet
Autor:
Paul M Will, Wenwei Huang, Stephan Meister, Dorjbal Dorjsuren, Anton Simeonov, Bryan T. Mott, Andrew T Girvin, Pranav Shah, David A. Fidock, Daniel C. Talley, Benjamin A Sigmon, Richard T. Eastman, Xin Xu, Sachel Mok, Leila S. Ross, Tomas Yeo, Daniel J. Jansen, Robert F. Campbell, Alexey V. Zakharov, Richard J. Sciotti, Carleen Klumpp-Thomas, Yevgeniya Antonova-Koch, Norman C. Waters, Juan J. Marugan, Norma Roncal, Elizabeth A. Winzeler, David J. Maloney, Kathryn J. Wicht, Ajit Jadhav, Hongmao Sun
Publikováno v:
Scientific Reports
Scientific Reports, Vol 11, Iss 1, Pp 1-16 (2021)
Scientific Reports, Vol 11, Iss 1, Pp 1-16 (2021)
The spread of Plasmodium falciparum parasites resistant to most first-line antimalarials creates an imperative to enrich the drug discovery pipeline, preferably with curative compounds that can also act prophylactically. We report a phenotypic quanti
Autor:
Ryan M. Anderson, Gaurav Chopra, Chanelle Benjamin, Jonathan Fine, Jerry L. Nadler, Raghavendra G. Mirmira, Abass M. Conteh, Sarah A. Tersey, David J. Maloney, Marimar Hernandez-Perez, Jennifer B. Nelson, Kara S. Benninger, Amelia K. Linnemann
Publikováno v:
Diabetes
Islet β-cell dysfunction and aggressive macrophage activity are early features in the pathogenesis of type 1 diabetes (T1D). 12/15-Lipoxygenase (12/15-LOX) is induced in β-cells and macrophages during T1D and produces proinflammatory lipids and lip
Autor:
Rachel Schiller, Jacob T. Bush, G Scozzafava, James Wickens, Ganesha Rai, Bryan T. Mott, Akane Kawamura, Anthony Tumber, Clarisse Lejeune, Mun Chiang Chan, Tzu-Lan Yeh, James S. O. McCullagh, Hwanho Choi, David J. Maloney, Christopher J. Schofield
Publikováno v:
ChemMedChem
Chemmedchem
Chemmedchem
The 2-oxoglutarate (2OG)-dependent Jumonji C domain (JmjC) family is the largest family of histone lysine demethylases. There is interest in developing small-molecule probes that modulate JmjC activity to investigate their biological roles. 5-Carboxy
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1052dfdee934f6f0cda848f1ab26d89f
https://ora.ox.ac.uk/objects/uuid:cc2a3734-4a5d-4aa5-b621-f371f424091f
https://ora.ox.ac.uk/objects/uuid:cc2a3734-4a5d-4aa5-b621-f371f424091f
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:
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:
Bioorganic & Medicinal Chemistry. 16:4331-4340
Bioassay-guided fractionation of extracts prepared from Couepia polyandra and Edgeworthia gardneri resulted in the isolation of the DNA polymerase beta (pol beta) inhibitors oleanolic acid (1), edgeworin (2), betulinic acid (3), and stigmasterol (4).
Publikováno v:
Bioorganic & Medicinal Chemistry. 15:5018-5034
Inappropriate activity of p90 ribosomal S6 kinase (RSK) has been implicated in various human cancers as well as other pathologies. We previously reported the isolation, characterization, and synthesis of the natural product kaempferol 3-O-(3'',4''-di
Influence of rhamnose substituents on the potency of SL0101, an inhibitor of the Ser/Thr kinase, RSK
Autor:
David J. Maloney, Jeffrey A. Smith, David E. Clark, Sidney M. Hecht, Yaming Xu, Deborah A. Lannigan
Publikováno v:
Bioorganic & Medicinal Chemistry. 14:6034-6042
We have previously reported the isolation of kaempferol 3-O-(3'',4''-di-O-acetyl-alpha-l-rhamnopyranoside) from Forsteronia refracta [Xu, Y.-M.; Smith, J. A.; Lannigan, D. A.; Hecht, S. M. Biorg. Med. Chem.2006, 14, 3974-3977.]. This flavonoid glycos
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