Zobrazeno 1 - 10
of 33
pro vyhledávání: '"William Leister"'
Autor:
Christopher J. Welch, Shagawa Tomohiro, Kevin Joseph Barry, Mengling Wong, Donghong A. Gao, Iriki Takayuki, Eric T. Manning, Masami Tomita, Nobumitsu Fukushima, Timothy Lee, William Farrell, Benjamin Hritzko, Masayuki Nishimura, Larry Miller, Thomas J. Moran, Robert P. DePianta, Eric P. Seest, Lisa Schaffter, Heewon Lee, Lisa Nogle, Loanne Chung, Yingru Zhang, Katsuhiro Tanaka, Shuping Dong, Michiaki Owa, William Leister, Takeshi Bamba, Meenakshi Goel, Mirlinda Biba, Andy Sasaki, Frank Riley, James Paulson, Douglas B. Moore, Jimmy O. DaSilva, Anne Akin
Publikováno v:
Organic Process Research & Development. 24:1271-1280
Precompetitive collaborations on the development of new enabling technologies for conducting pharmaceutical research and development are becoming increasingly popular as pharmaceutical companies re...
Publikováno v:
J Agric Food Chem
Creatine transporter deficiency (CTD) is caused by a defect in the X-linked creatine transporter SLC6A8 gene leading to severe neurologic and physiologic conditions. Cyclocreatine and phosphocyclocreatine supplementation is seen as a potential treatm
Autor:
Ian S. Goldlust, Christopher A. LeClair, Paresma R. Patel, David J. Maloney, Adam Yasgar, Jonathan M. Keller, Martin J. Walsh, Christopher P. Austin, Brian D. Peyser, Paul Shinn, Rajarshi Guha, Ganesha Rai, Damien Y. Duveau, Sam Michael, Marc Ferrer, William Leister, Dongbo Liu, Wenwei Huang, Craig J. Thomas, Anton Simeonov, Bryan T. Mott, Crystal McKnight, Ryan M. Young, Matthew B. Boxer, Jian-kang Jiang, Louis M. Staudt, Lesley A. Mathews Griner, Scott E. Martin, Tim Mierzwa, Ajit Jadhav
Publikováno v:
Proceedings of the National Academy of Sciences. 111:2349-2354
The clinical development of drug combinations is typically achieved through trial-and-error or via insight gained through a detailed molecular understanding of dysregulated signaling pathways in a specific cancer type. Unbiased small-molecule combina
Autor:
Wei Zheng, Wendy Westbroek, Noel Southall, Ehud Goldin, Juan J. Marugan, Ellen Sidransky, Jae H. Choi, Samarjit Patnaik, Omid Motabar, William Leister, Arash Velayati, Wendy A. Lea
Publikováno v:
Journal of Medicinal Chemistry. 55:5734-5748
A major challenge in the field of Gaucher disease has been the development of new therapeutic strategies including molecular chaperones. All previously described chaperones of glucocerebrosidase are enzyme inhibitors, which complicates their clinical
Autor:
Lewis C. Cantley, William Leister, Kyle R. Brimacombe, Matthew G. Vander Heiden, Henrike Veith, Martin J. Walsh, Matthew B. Boxer, Min Shen, Douglas S. Auld, James M. Bougie, Thomas Daniel, Craig J. Thomas, William J. Israelsen
Publikováno v:
PMC
Compared to normal differentiated cells, cancer cells have altered metabolic regulation to support biosynthesis and the expression of the M2 isozyme of pyruvate kinase (PKM2) plays an important role in this anabolic metabolism. While the M1 isoform i
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:
Lena Schultz, William Leister, Eric K. Hoobler, Ganesha Rai, David J. Maloney, Ajit Jadhav, Anton Simeonov, Victor Kenyon, J. Brian Jameson, Theodore R. Holman, Michelle Armstrong
Publikováno v:
Journal of Medicinal Chemistry. 53:7392-7404
There are a variety of lipoxygenases in the human body (hLO), each having a distinct role in cellular biology. Human reticulocyte 15-Lipoxygenase-1 (15-hLO-1), which catalyzes the dioxygenation of 1,4-cis,cis-pentadiene-containing polyunsaturated fat
Autor:
Paul Shinn, Menghang Xia, Danielle van Leer, Susanne C. Miller, Sunita J. Shukla, William Leister, Christopher P. Austin, Srilatha Sakamuru, Matias S. Attene-Ramos, Ruili Huang
Publikováno v:
Biochemical Pharmacology. 79:1272-1280
Nuclear factor-kappa B (NF-kappaB) is a transcription factor that plays a critical role across many cellular processes including embryonic and neuronal development, cell proliferation, apoptosis, and immune responses to infection and inflammation. Dy
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
Autor:
Francesca Deflorian, William Leister, Melissa Perreira, Craig J. Thomas, Kamran Ghoreschi, John J. O'Shea, Zhi Chen, Marko Pesu, Dac-Trung Nguyen, Stefano Costanzi, Jeremy A. Smith, Eric Liu, Jian-kang Jiang
Publikováno v:
Journal of Medicinal Chemistry. 51:8012-8018
Here, we examine the significance that stereochemistry plays within the clinically relevant Janus kinase 3 (Jak3) inhibitor 1 (CP-690,550). A synthesis of all four enantiopure stereoisomers of the drug was carried out and an examination of each compo