Zobrazeno 1 - 10
of 22
pro vyhledávání: '"Jay A. Markwalder"'
Autor:
Jay A. Markwalder, Aaron J. Balog, David K. Williams, Susheel J. Nara, Ratnakar Reddy, Saumya Roy, Yadagiri Kanyaboina, Xin Li, Kathy Johnston, Yi Fan, Hal Lewis, Frank Marsilio, Chunhong Yan, David Critton, John A. Newitt, Sarah C. Traeger, Dauh-Rurng Wu, Maria N. Jure-Kunkel, Lata Jayaraman, Tai-An Lin, Michael W. Sinz, John T. Hunt, Steven P. Seitz
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::64f0da67b51d6c7282c418d8dbb98887
https://doi.org/10.2139/ssrn.4348735
https://doi.org/10.2139/ssrn.4348735
Autor:
M. Jure-Kunkel, Jay A. Markwalder, Weifang Shan, Bin Chen, Steven P. Seitz, Andrew Nation, John T. Hunt, Lauren Haque, Gregory D. Vite, Jennifer Donnell, David K. Williams, Kelly L. Covello, Aaron Balog, Hart Amy C, Sunil Kumar Mandal, Libing Chen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:732-736
A novel series of o-phenylenediamine-based inhibitors of indoleamine 2,3-dioxygenase (IDO) has been identified. IDO is a heme-containing enzyme, overexpressed in the tumor microenvironment of many cancers, which can contribute to the suppression of t
Autor:
Steven P. Seitz, John T. Hunt, Kelly L. Covello, Lisa Elkin, Gregory D. Vite, Yuval Blat, Jay A. Markwalder, Jonathan G. Pabalan, Maria Jure-Kunkel
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:582-585
The discovery of a series of structurally-novel biaryl urea IDO inhibitors is described. Optimization of a micromolar hit through iterative cycles of synthesis and screening in an assay measuring IDO-mediated intracellular conversion of tryptophan to
Publikováno v:
International Journal of Peptide and Protein Research. 38:314-323
The solution structure of a gramicidin S (GS) analog containing a beta-turn mimic [BTD4-5, Lys2.2']GS has been compared to that of native GS. The linear [BTD4-5, Lys2.2']GS was synthesized by solid phase methodology and the cyclized peptide was analy
Autor:
Heshani de Silva, Jay A. Markwalder, Hong Xiao, Tai-An Lin, Qi Guo, Donald G. Jackson, Chen-Yi Hung, Petra Ross-Macdonald, Steven P. Seitz, Judith Wardwell-Swanson, Liqi He, Charles Tilford, Ricardo M. Attar, Becky Penhallow
Publikováno v:
Molecular Cancer Therapeutics. 7:3490-3498
In developing inhibitors of the LIM kinases, the initial lead molecules combined potent target inhibition with potent cytotoxic activity. However, as subsequent compounds were evaluated, the cytotoxic activity separated from inhibition of LIM kinases
Autor:
Steven P. Seitz, Sarah Cox, Pieter F. W. Stouten, Michael D. Boisclair, Stephen L. Brenner, Jay A. Markwalder, Karen A. Rossi, Leonardo Brizuela, Chong-Hwan Chang
Publikováno v:
Journal of Computer-Aided Molecular Design. 19:111-122
Cyclin-dependent kinases (CDKs) play a key role in regulating the cell cycle. The cyclins, their activating agents, and endogenous CDK inhibitors are frequently mutated in human cancers, making CDKs interesting targets for cancer chemotherapy. Our ai
Autor:
Angela Smallwood, Jodi K. Muckelbauer, Sarah Cox, C. Anne Higley, Steven P. Seitz, Eddy W. Yue, George L. Trainor, Dimeo Susan, Haiying Chen, Robert H. Grafstrom, Pamela A. Benfield, Jay A. Markwalder, Catherine R. Burton, Chong Hwan Chang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:343-346
New indeno[1,2-c]pyrazol-4-one cyclin dependent kinase inhibitors have been disclosed. The most promising compounds are nanomolar enzyme inhibitors with excellent activity against tumor cells. The most advanced compound retains cell culture activity
Autor:
Maria D.F.S. Barbosa, Siqi Lin, Christopher A. Teleha, Andrew S. Thompson, Vasudha Garlapati, Jay A. Markwalder, George L. Trainor, Joseph A. DeVito, Charles Liu, David L. Pompliano, Michael G. Kurilla, Jonathan A. Mills
Publikováno v:
Antimicrobial Agents and Chemotherapy. 46:3549-3554
Escherichia coli under-expressing lepB was utilized to test cellular inhibition of signal peptidase I (SPase). For the construction of a lepB regulatable strain, the E. coli lepB gene was cloned into pBAD, with expression dependent on l -arabinose. T
Autor:
Abdul E Mutlib, Jay A. Markwalder, David D. Christ, Beverly C. Cordova, Ronald M. Klabe, Steven P. Seitz
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:619-622
Studies on the biotransformation of the clinically important non-nucleoside reverse transcriptase inhibitor efavirenz have shown that oxidation and secondary conjugation are important components of the processing of this molecule in vivo. We have syn
Autor:
Jay A. Markwalder, Senliang Pan, Jeffrey W. Corbett, Beverly C. Cordova, James D. Rodgers, Sena Garber, Susan Erickson-Viitanen, Ronald M. Klabe
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:211-214
A series of unique 3,3a-dihydropyrano[4,3,2-de]quinazolin-2(1H)-ones and a 2a,5-dihydro-2H-thieno[4,3,2-de]quinazoline-4(3H)-thione were found to be HIV-1 non-nucleoside reverse transcriptase inhibitors. One of these compounds, as the racemate, posse