Zobrazeno 1 - 10
of 26
pro vyhledávání: '"Timothy B. Durham"'
Autor:
Kacey J. Prentice, Stacy G. Wendell, Ying Liu, Judith A. Eversley, Sonia R. Salvatore, Haneesha Mohan, Sydney L. Brandt, Andrew C. Adams, X. Serena Wang, David Wei, Garret A. FitzGerald, Timothy B. Durham, Craig D. Hammond, Kyle W. Sloop, Carsten Skarke, Francisco J. Schopfer, Michael B. Wheeler
Publikováno v:
EBioMedicine, Vol 27, Iss C, Pp 200-213 (2018)
Prescription ω-3 fatty acid ethyl ester supplements are commonly used for the treatment of hypertriglyceridemia. However, the metabolic profile and effect of the metabolites formed by these treatments remain unknown. Here we utilized unbiased metabo
Externí odkaz:
https://doaj.org/article/8859af43754d46f59999fc8b6184ede4
Autor:
Rongjun He, Jifeng Wang, Zhi-Hong Yu, Julie S. Moyers, M. Dodson Michael, Timothy B. Durham, Jeff W. Cramer, Yuewei Qian, Amy Lin, Li Wu, Nicholas Noinaj, David G. Barrett, Zhong-Yin Zhang
Publikováno v:
J Med Chem
Protein tyrosine phosphatases constitute an important class of drug targets, whose potential has been limited by the paucity of drug-like small molecule inhibitors. We recently described a class of active site-directed, moderately selective and poten
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0c61119301642263decda2d2789be67b
https://doi.org/10.1021/acs.jmedchem.2c01143
https://doi.org/10.1021/acs.jmedchem.2c01143
Autor:
Harold B. Brooks, Shuang Luo, Timothy I. Meier, Kwame Frimpong, Timothy B. Durham, Matthew Lee, Kevin Robert Fales, Kenneth Jeff Thrasher, Philip W. Iversen, Robert T. Foreman, Yu-Hua Hui, Charles D. Spencer, Sandaruwan Geeganage, Kenneth D. Roth, Alicia Torrado, Yong Wang, Chong Si, Jefferson R. Mc Cowan, Stefan Jon Thibodeaux, Zhipei Wu, Timothy Alan Shepherd, James Lee Toth, Tao Wang, Yue-Wei Qian, Robert Dean Dally, Njoroge F George, Susan A. Konicek
Publikováno v:
Scientific Reports, Vol 8, Iss 1, Pp 1-12 (2018)
Scientific Reports
Scientific Reports
AICARFT is a folate dependent catalytic site within the ATIC gene, part of the purine biosynthetic pathway, a pathway frequently upregulated in cancers. LSN3213128 is a potent (16 nM) anti-folate inhibitor of AICARFT and selective relative to TS, SHM
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8239c8bd258656146d4e890853c7f73a
http://link.springer.com/article/10.1038/s41598-018-33453-4
http://link.springer.com/article/10.1038/s41598-018-33453-4
Autor:
David W. Wei, Francisco J. Schopfer, Michael B. Wheeler, Kacey J. Prentice, Stacy G. Wendell, Sydney L. Brandt, X. Serena Wang, Timothy B. Durham, Haneesha Mohan, Carsten Skarke, Ying Liu, Garret A. FitzGerald, Andrew C. Adams, Kyle W. Sloop, Craig D. Hammond, Sonia R. Salvatore, Judith A. Eversley
Publikováno v:
EBioMedicine
EBioMedicine, Vol 27, Iss C, Pp 200-213 (2018)
EBioMedicine, Vol 27, Iss C, Pp 200-213 (2018)
Prescription ω-3 fatty acid ethyl ester supplements are commonly used for the treatment of hypertriglyceridemia. However, the metabolic profile and effect of the metabolites formed by these treatments remain unknown. Here we utilized unbiased metabo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d69c5df5ad4be939071a4f9a6852c058
https://doi.org/10.1016/j.ebiom.2017.12.019
https://doi.org/10.1016/j.ebiom.2017.12.019
Autor:
José Francisco Soriano, Javier Agejas, Rosario Gonzalez, Ramón Rodríguez, Timothy B. Durham, Howard Barff Broughton, Juan F. Espinosa, Paloma Vidal, Ana B. Bueno, Robert Dean Dally, Hsiu-Chiung Yang, Alicia Marcos, David E. Timm, Gema Sanz, James R. McCarthy, Patric James Hahn
Publikováno v:
Journal of Medicinal Chemistry. 60:9807-9820
NMR conformational analysis of a hydroxyethylamine peptide isostere developed as an aspartic protease inhibitor shows that it is a flexible architecture. Cyclization to form pyrrolidines, piperidines, or morpholines results in a preorganization of th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d3c3ae5f96ab4869e6ec456bade5b1dc
https://doi.org/10.1021/acs.jmedchem.7b01304
https://doi.org/10.1021/acs.jmedchem.7b01304
Autor:
Alicia Torrado, Shane Atwell, Timothy B. Durham, Njoroge F George, Timothy I. Meier, Brandon J. Margolis, Stefan Jon Thibodeaux, Yu-Hua Hui, Robert Dean Dally, Kevin Robert Fales, Kenneth Jeff Thrasher, James Lee Toth, Jing Wang, Kwame Frimpong, Susan A. Konicek, Yong Wang, Chong Si, Kenneth D. Roth, Matthew Lee, Zhipei Wu, Jefferson R. Mc Cowan, Timothy Alan Shepherd, Sandaruwan Geeganage, Harold B. Brooks
Publikováno v:
Journal of Medicinal Chemistry. 60:9599-9616
A hallmark of cancer is unbridled proliferation that can result in increased demand for de novo synthesis of purine and pyrimidine bases required for DNA and RNA biosynthesis. These synthetic pathways are frequently upregulated in cancer and involve
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b243bbece7ad1a8ca057dbf632832ff1
https://doi.org/10.1021/acs.jmedchem.7b01046
https://doi.org/10.1021/acs.jmedchem.7b01046
Autor:
Kannan Thirunavukkarasu, Mark Chambers, Daniel R. Mudra, Michael Robert Wiley, Craig A. Swearingen, Lisa A. Adams, Timothy B. Durham, Jothirajah Marimuthu, C. Lin, James Lee Toth, Chin Liu
Publikováno v:
Journal of Medicinal Chemistry. 60:5933-5939
Aggrecanase-1 and -2 (ADAMTS-4 and ADAMTS-5) are zinc metalloproteases involved in the degradation of aggrecan in cartilage. Inhibitors could provide a means of altering the progression of osteoarthritis. We report the identification of 7 which had g
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2b1aa6bde3d0801758aea530059c1a40
https://doi.org/10.1021/acs.jmedchem.7b00650
https://doi.org/10.1021/acs.jmedchem.7b00650
Autor:
Kannan Thirunavukkarasu, Mark Chambers, Daniel R. Mudra, Craig A. Swearingen, Lisa A. Adams, Jennifer M. Weller, P.G. Mitchell, Timothy B. Durham, Chin Liu, C. Lin, James Lee Toth, Michael Robert Wiley, Jothirajah Marimuthu
Publikováno v:
Journal of Medicinal Chemistry. 59:5810-5822
The development of reliable relationships between in vivo target engagement, pharmacodynamic activity, and efficacy in chronic disease models is beneficial for enabling hypothesis-driven drug discovery and facilitating the development of patient-focu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f252c22eeb38a66a724a46f915a1a225
https://doi.org/10.1021/acs.jmedchem.6b00398
https://doi.org/10.1021/acs.jmedchem.6b00398
Autor:
Timothy B. Durham, Jeffrey T. Dixon, James Lee Toth, Angela M. Siesky, Michael E. Christe, Valentine J. Klimkowski, Nathan A. Calvert, John F. Schindler, Dana Sindelar, Kyle W. Sloop, M. Dodson Michael, Jesline T. Alexander-Chacko, Julia X.C. Cao, Ginger Y. Wu, James E. McGee, Rachel N. Cavitt, Stefan Jon Thibodeaux, Sherry Y. Guo, Yong Wang, Michael J. Coghlan, Vladislav V. Kiselyov
Publikováno v:
Journal of Biological Chemistry. 290:20044-20059
Insulin-degrading enzyme (IDE, insulysin) is the best characterized catabolic enzyme implicated in proteolysis of insulin. Recently, a peptide inhibitor of IDE has been shown to affect levels of insulin, amylin, and glucagon in vivo. However, IDE(-/-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3b79e6dcdb0455d21e4b543d83d06c40
https://doi.org/10.1074/jbc.m115.638205
https://doi.org/10.1074/jbc.m115.638205
Autor:
Jerome F. Baker, Kelly L. Dauer, Nicholas J. Karney, Mary C. O’Sullivan, Hannah E. Valdes, Andrew C. Forrestel, Cyrus J. Bacchi, Timothy B. Durham
Publikováno v:
Bioorganic & Medicinal Chemistry. 23:996-1010
Trypanothione reductase (TR) is an enzyme critical to the maintenance of the thiol redox balance in trypanosomatids, including the genera Trypanosoma and Leishmania that are parasites responsible for several serious diseases. Analogs of clomipramine
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b0a69750efbe3e13dc873c07606d81f7
https://doi.org/10.1016/j.bmc.2015.01.018
https://doi.org/10.1016/j.bmc.2015.01.018