Zobrazeno 1 - 10
of 30
pro vyhledávání: '"David J. Witter"'
Autor:
David A Candito, David J. Witter, Josep Saurí, Yu-hong Lam, Surendra B Gadamsetty, Michael H. Reutershan, Yingchun Ye, Ryan V Quiroz, Sebastian Schneider, Rachel L. Palte, Hongming Li
Publikováno v:
The Journal of Organic Chemistry. 86:5142-5151
In the context of a PRMT5 inhibitor program, we describe our efforts to develop a flexible and robust strategy to access tetrahydrofuro[3,4-b]furan nucleoside analogues. Ultimately, it was found that a Wolfe type carboetherification from an alkenol d
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::2be696853f7f2484c20fd532369afef9
https://doi.org/10.1021/acs.joc.0c02969
https://doi.org/10.1021/acs.joc.0c02969
Autor:
Michael Salmon, Hyun-Hee Lee, Meiyao Wang, Hongshi Yu, Michael Caniga, David J. Witter, Peter W. Fan
Publikováno v:
Journal of Aerosol Medicine and Pulmonary Drug Delivery. 32:251-265
Background: A highly potent pan-Janus kinase (JAK) inhibitor with excellent kinome selectivity was developed for topical delivery to treat severe asthma. This poorly soluble drug discovery candidate, iJAK-001, is expected to exhibit long duration of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3e74ccc60d2ee2be4acec1cfdc96247b
https://doi.org/10.1089/jamp.2018.1492
https://doi.org/10.1089/jamp.2018.1492
Autor:
My Sam Mansueto, Brooke M Swalm, Patrick S. Fier, Rachel L. Palte, Sandra Lee, Kristin Geddes, Josep Saurí, Michael H. Reutershan, Charles S. Yeung, Benjamin Nicholson, David J. Witter, Murray Wan, Robert P Hayes, Haiyan Xu, David L. Sloman, Nicole Follmer, Daniel S. Spellman, Danica A. Rankic, Pierre Daublain, Timothy J. Henderson, Jongwon Lim, Dapeng Chen, Erik Munsell, Guo Feng, Steven M. Silverman, Ryan V Quiroz, Doug Linn, Sulagna Sanyal, Michelle R. Machacek, Craig R. Gibeau, Shuhei Kawamura, Yuanwei Gao, Jonathan M E Hughes, Sebastian Schneider, Phieng Siliphaivanh, Yingchun Ye, Brian M. Lacey
Publikováno v:
Journal of medicinal chemistry. 64(7)
Protein arginine methyltransferase 5 (PRMT5) is a type II arginine methyltransferase that catalyzes the post-translational symmetric dimethylation of protein substrates. PRMT5 plays a critical role in regulating biological processes including transcr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::07c9cca5e958fa221091b3803ef442cf
https://pubmed.ncbi.nlm.nih.gov/33755451
https://pubmed.ncbi.nlm.nih.gov/33755451
Autor:
Myles Clancy, Daniel Shao-Weng Tan, Danny Nguyen, David J. Witter, Ross A. Soo, Mark A. Socinski, Leigh Zawel, Helena Alexandra Yu, Jon M. Wigginton, Egbert F. Smit, James Chih-Hsin Yang, John Wrangle, Marianna Koczywas, Zofia Piotrowska, Vamsidhar Velcheti, Alexander I. Spira, Victor Ho-Fun Lee, Asher Page
Publikováno v:
Journal of Clinical Oncology. 39:9077-9077
9077 Background: NSCLC with EGFR ins20 represents a significant area of unmet need, with no approved targeted therapies. While several agents targeting EGFR ins20 are in development, wild-type (WT) EGFR-related adverse events (AEs) have been common a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::91fcf6f85ce5535902e9743fd916fb9c
https://doi.org/10.1200/jco.2021.39.15_suppl.9077
https://doi.org/10.1200/jco.2021.39.15_suppl.9077
Autor:
Peter J. Dandliker, Hao Tang, Christopher J. Dinsmore, Chi-Sung Chiu, Fiona Elwood, Deborah Slipetz, Jennifer Piesvaux, Sujal V. Deshmukh, Ilona Kariv, Bo-Sheng Pan, Carla Alpert, Nathan Bays, Alan Byford, Alexey Rivkin, Peter Goldenblatt, Irena Ivanovska, Mark E. Scott, Joel A. Klappenbach, Hyun-Hee Lee, David J. Witter, Kalyan Chakravarthy, Lauren Dorosh, Yujie Qu, Brian Kraybill, Mark Zielstorff
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 361(2)
Reversible janus associated kinase (JAK) inhibitors such as tofacitinib and decernotinib block cytokine signaling and are efficacious in treating autoimmune diseases. However, therapeutic doses are limited due to inhibition of other JAK/signal transd
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::30dcce0e8183db5060a7c6ebeec57fe3
https://pubmed.ncbi.nlm.nih.gov/28193636
https://pubmed.ncbi.nlm.nih.gov/28193636
Autor:
Shuxia Zhao, Paul Kirschmeier, Ulrike Philippar, Li Xiao, Wang James J-S, Boga Sobhana Babu, Pierre Daublain, Phieng Siliphaivanh, Priya Dayananth, Clifford Restaino, Donna Carr, Lata Jayaraman, Xiaolei Gao, Marc Pelletier, Ling Zhang, Bart Lutterbach, Erick J. Morris, Stuart Black, Rumin Zhang, Weihong Jin, Ahmed A. Samatar, Joe Kelly, Daniel J. Hicklin, Alan B. Cooper, Leigh Zawel, Liang Zhu, Brian Long, Elaine M. Pinheiro, Hugh Y. Zhu, Sharda Jha, Stephen Fawell, Sunil Paliwal, D. Gary Gilliland, Jenny Liu, William T. Windsor, David J. Witter, Edward DiNunzio, Yongi Deng, W. Robert Bishop, Minilik Angagaw, Desai Jagdish A, Alan Hruza, Gerald W. Shipps
Publikováno v:
Cancer Discovery. 3:742-750
The high frequency of activating RAS or BRAF mutations in cancer provides strong rationale for targeting the mitogen-activated protein kinase (MAPK) pathway. Selective BRAF and MAP-ERK kinase (MEK) inhibitors have shown clinical efficacy in patients
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::00ca7ac16344cf7d4ebc028f039418f5
https://doi.org/10.1158/2159-8290.cd-13-0070
https://doi.org/10.1158/2159-8290.cd-13-0070
Publikováno v:
The Journal of Organic Chemistry. 74:6390-6393
The efficient Suzuki cross-coupling of pyrazoline nonaflates with organoboron reagents was achieved to afford diverse 3-substituted-2-pyrazolines in excellent yield. The nonaflates displayed improved reactivity over the corresponding triflates and sm
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::480a211a2f34a7b784fc397e7c00346f
https://doi.org/10.1021/jo9011859
https://doi.org/10.1021/jo9011859
Autor:
David J. Witter, Karin M. Otte, Richard E. Middleton, Bethany Hughes, Jonathan B. Grimm, Alexander A. Szewczak, Phieng Siliphaivanh, Julie E. Hamill, Judith C. Fleming, Jonathan C. Cruz, Melissa Chenard, Astrid M. Kral, William K. Dahlberg, Kevin J. Wilson, J. Paul Secrist, Thomas A. Miller, Andreas Harsch
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:1859-1863
An HTS screening campaign identified a series of low molecular weight phenols that showed excellent selectivity (>100-fold) for HDAC1/HDAC2 over other Class I and Class II HDACs. Evolution and optimization of this HTS hit series provided HDAC1-select
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f265876569a65c8b99cd5d342f8f2e3f
https://doi.org/10.1016/j.bmcl.2008.02.012
https://doi.org/10.1016/j.bmcl.2008.02.012
Autor:
Sandro Belvedere, Liqiang Chen, J. Paul Secrist, Thomas A. Miller, Ralph T. Mosley, David J. Witter
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:4562-4567
Benzo[b]thienyl hydroxamic acids, a novel class of histone deacetylase (HDAC) inhibitors, were identified via a targeted screen of small molecule hydroxamic acids. Various substitutions were explored in the C5- and C6-positions of the benzo[b]thiophe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0f90f365af6bd6f083e18de1613f9fc0
https://doi.org/10.1016/j.bmcl.2007.05.091
https://doi.org/10.1016/j.bmcl.2007.05.091
Publikováno v:
Tetrahedron Letters. 48:4509-4513
The carbonylation of enantiopure phenylglycine-derived aryl triflates was achieved to afford 4-carboxyphenylglycine analogs with high enantiomeric excesses (88 to >99% ee). Amide analogs of phenylglycine were well-tolerated in the hydroxy- and methox
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::44b440bba67645238ab4802c843afd9b
https://doi.org/10.1016/j.tetlet.2007.04.145
https://doi.org/10.1016/j.tetlet.2007.04.145