Zobrazeno 1 - 10
of 28
pro vyhledávání: '"Aravind Basavapathruni"'
Autor:
Eric Haines, Michael Burke, Rachel Catterall, Victor De Jesus, Bin Li, Joseph D. Manna, George Punkosdy, Oksana Zavidij, Sarah R. Wessel, Grace Werosta, Jill Cavanaugh, Sheila Newhouse, Aravind Basavapathruni, Lan Xu, Sergio Santillana, X. Michelle Zhang, Sabine K. Ruppel
Publikováno v:
Molecular Cancer Research. 21:PR10-PR10
Alterations in the RAS/RAF/MEK/ERK pathway are the most common drivers of oncogenesis. Although MEK is a clinically validated cancer target and several MEK inhibitors have been approved by the FDA, their clinical utility is limited to BRAFV600 mutant
Publikováno v:
Analytical Biochemistry. 645:114637
Autor:
Nigel J. Waters, Angelos Dovletoglou, Tyler B. Jensen, Scott R. Daigle, Edward J. Olhava, Brett Franklin Truitt, Aravind Basavapathruni, Carly T. Campbell, Kim Stickland, Roy M. Pollock, Bruce N. Rehlaender
Publikováno v:
Journal of Controlled Release. 220:758-765
Protein methyltransferases are emerging as promising drug targets for therapeutic intervention in human cancers. Pinometostat (EPZ-5676) is a small molecule inhibitor of the DOT1L enzyme, a histone methyltransferase that methylates lysine 79 of histo
Autor:
Edward J. Olhava, Angelos Dovletoglou, Christina J. Allain, Nigel J. Waters, Richard Chesworth, Aravind Basavapathruni, Alejandra Raimondi, Roy M. Pollock, Carly A. Therkelsen, Paul G. Pearson, Lei Jin, Victoria M. Richon, Robert A. Copeland, Mikel P. Moyer, P. Ann Boriack-Sjodin, Christine Klaus, Margaret Porter Scott, Scott R. Daigle
Publikováno v:
Biopharmaceutics & Drug Disposition. 35:237-252
(2R,3R,4S,5R)-2-(6-Amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol (EPZ-5676) is a novel DOT1L histone methyltransferase inhibitor currently in clinical
Autor:
Carly A. Therkelsen, Alejandra Raimondi, Roy M. Pollock, Margaret Porter Scott, Scott R. Daigle, Robert A. Copeland, Mikel P. Moyer, Aravind Basavapathruni, Edward J. Olhava, Christina J. Allain, Lei Jin, Christine Klaus, Richard Chesworth, Nigel J. Waters, Victoria M. Richon, P. Ann Boriack-Sjodin
Publikováno v:
Blood. 122:1017-1025
Rearrangements of the MLL gene define a genetically distinct subset of acute leukemias with poor prognosis. Current treatment options are of limited effectiveness; thus, there is a pressing need for new therapies for this disease. Genetic and small m
Autor:
Tim J. Wigle, Thomas V. Riera, Jodi Gureasko, Peter A. Leland, Robert A. Copeland, Adarsh Godbole, Margaret Porter Scott, Aravind Basavapathruni, P. Ann Boriack-Sjodin, William Hermans
Publikováno v:
Biochemistry. 55(11)
The protein methyltransferase (PMT) SETDB1 is a strong candidate oncogene in melanoma and lung carcinomas. SETDB1 methylates lysine 9 of histone 3 (H3K9), utilizing S-adenosylmethionine (SAM) as the methyl donor and its catalytic activity, has been r
Publikováno v:
Analytical Biochemistry. 416:206-210
Jump dilution analysis is commonly used to evaluate the reversibility of inhibition and to quantify the residence time of the inhibitor-enzyme complex. During hit and lead characterization, one sometimes observes apparently linear progress curves aft
Autor:
Srinivas S. Rao, Rory Coffey, Gary J. Nabel, Michael S. Seaman, Wendy W. Yeh, John R. Mascola, Peter T. Hraber, Ayush Giri, James B. Whitney, Aravind Basavapathruni, Norman L. Letvin, Bette T. Korber
Publikováno v:
Journal of Virology. 84:953-963
The evolution of envelope mutations by replicating primate immunodeficiency viruses allows these viruses to escape from the immune pressure mediated by neutralizing antibodies. Vaccine-induced anti-envelope antibody responses may accelerate and/or al
Publikováno v:
The FASEB Journal. 21:3795-3808
The HIV/AIDS pandemic has existed for >25 years. Extensive work globally has provided avenues to combat viral infection, but the disease continues to rage on in the human population and infected approximately 4 million people in 2006 alone. In this r
Autor:
Roger Hunter, Ian Hale, Karen S. Anderson, Christopher M. Bailey, Aravind Basavapathruni, Clare I. Muhanji
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:2614-2617
The synthesis of bifunctional compound 10 consisting of d4U joined at C-5 to a butynyl spacer attached to HI-236 is reported using a Sonogashira coupling as a key step. As a non-cleavable bifunctional HIV inhibitor incorporating an NRTI with an NNRTI