Zobrazeno 1 - 10
of 82
pro vyhledávání: '"Lorin A, Thompson"'
Autor:
Anthony Accorsi, Cacace Angela Marie, Erin Valentine, Peter B. Rahl, Aaron N. Chang, Lorin A. Thompson, Lucienne Ronco, Joseph Maglio, Alan J. Robertson, Wallace Owen Brendan, L. Alejandro Rojas, Steven Kazmirski, Diego Cadavid, Rabi Tawil, Ning Shen
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 374:489-498
Facioscapulohumeral muscular dystrophy (FSHD) is caused by the loss of repression at the D4Z4 locus leading to aberrant double homeobox 4 (DUX4) expression in skeletal muscle. Activation of this early embryonic transcription factor results in the exp
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::391910836251b5c32c0c18a31cee0733
https://doi.org/10.1124/jpet.119.264689
https://doi.org/10.1124/jpet.119.264689
Autor:
Carolyn Diane Dzierba, Linda J. Bristow, Ramkumar Rajamani, Jie Chen, Rick L. Pieschl, Sing-Yuen Sit, Brian Lee Venables, Michele Matchett, Ronald J. Knox, Lorin A. Thompson, Nicholas A. Meanwell, Yong-Jin Wu, Jason M. Guernon, James Herrington
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 29:659-663
Screening of 100 acylsulfonamides from the Bristol-Myers Squibb compound collection identified the C3-cyclohexyl indole 6 as a potent Nav1.7 inhibitor. Replacement of the C2 furanyl ring of 6 with a heteroaryl moiety or truncation of this group led t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::2f347d20e2f2ebee9e7e423555c27787
https://doi.org/10.1016/j.bmcl.2018.12.013
https://doi.org/10.1016/j.bmcl.2018.12.013
Autor:
John E. Macor, Yunhui Zhang, James E. Grace, Lorin A. Thompson, Jeremy H. Toyn, Lawrence R. Marcin, Subramaniam Krishnananthan, Jianliang Shi, Dmitry Zuev, Daniel Smith, Jianqing Li, Yong-Jin Wu, Jason M. Guernon, Xiaoliang Zhuo, Tatyana Zvyaga, Xu Li, Arvind Mathur, John Morrison, Jere E. Meredith, Charles F. Albright, S. Roy Kimura, Mendi A. Higgins, Kimberley A. Lentz, Richard E. Olson, Rex Denton, Kenneth M. Boy, Catherine R. Burton, Ashok K. Trehan, Michael K. Ahlijanian
Publikováno v:
ACS Medicinal Chemistry Letters
A triazine hit identified from a screen of the BMS compound collection was optimized for potency, in vivo activity, and off-target profile to produce the bicyclic pyrimidine γ-secretase modulator BMS-932481. The compound showed robust reductions of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ed62d494eee5e78e1c6f0f7838951135
http://europepmc.org/articles/PMC6421538
http://europepmc.org/articles/PMC6421538
Autor:
Jeremy H. Toyn, Lorin A. Thompson, Kimberley A. Lentz, Jere E. Meredith, Catherine R. Burton, Sethu Sankaranararyanan, Valerie Guss, Tracey Hall, Lawrence G. Iben, Carol M. Krause, Rudy Krause, Xu-Alan Lin, Maria Pierdomenico, Craig Polson, Alan S. Robertson, R. Rex Denton, James E. Grace, John Morrison, Joseph Raybon, Xiaoliang Zhuo, Kimberly Snow, Ramesh Padmanabha, Michele Agler, Kim Esposito, David Harden, Margaret Prack, Sam Varma, Victoria Wong, Yingjie Zhu, Tatyana Zvyaga, Samuel Gerritz, Lawrence R. Marcin, Mendi A. Higgins, Jianliang Shi, Cong Wei, Joseph L. Cantone, Dieter M. Drexler, John E. Macor, Richard E. Olson, Michael K. Ahlijanian, Charles F. Albright
Publikováno v:
International Journal of Alzheimer's Disease, Vol 2014 (2014)
Alzheimer’s disease is the most prevalent cause of dementia and is associated with accumulation of amyloid-β peptide (Aβ), particularly the 42-amino acid Aβ1-42, in the brain. Aβ1-42 levels can be decreased by γ-secretase modulators (GSM), whi
Externí odkaz:
https://doaj.org/article/1dce320132d4411583a19dcbfe2b54ae
Autor:
Carolyn Diane Dzierba, Debra J. Post-Munson, Ronald J. Knox, Lorin A. Thompson, Shuya Wang, Matthew G. Soars, Michele Matchett, Linda J. Bristow, James Herrington, Clotilde Bourin, Amy Newton, Rick L. Pieschl, Eric Shields, Amy Easton, Kathy Mosure, Guanglin Luo, Kimberly Newberry, Ling Chen, John D. Graef, Arun K. Senapati, Nicholas A. Meanwell, Digavalli V. Sivarao
Publikováno v:
Journal of Medicinal Chemistry. 62:831-856
3-Aryl-indole and 3-aryl-indazole derivatives were identified as potent and selective Nav1.7 inhibitors. Compound 29 was shown to be efficacious in the mouse formalin assay and also reduced complete Freund’s adjuvant (CFA)-induced thermal hyperalge
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::8738aee38a77abf37b839d8d841c0ca8
https://doi.org/10.1021/acs.jmedchem.8b01550
https://doi.org/10.1021/acs.jmedchem.8b01550
Autor:
Michelle Mellion, Sander Brooks, Diego Cadavid, Shane Raines, Michelle Hage, Geert Jan Groeneveld, Cécile Berends, William G Tracewell, Adefowope Odueyungbo, Lorin A. Thompson, Lucienne Ronco, Michiel J van Esdonk, Lisa Pagan, Umesh A. Badrising, Emilie M J van Brummelen, Baziel G.M. van Engelen
Publikováno v:
British Journal of Clinical Pharmacology, 87(12), 4658-4669. WILEY
Aims Evaluate safety, tolerability, pharmacokinetics (PK) and target engagement (TE) of losmapimod in blood and muscle in facioscapulohumeral dystrophy (FSHD). Methods This study included Part A: 10 healthy volunteers randomized to single oral doses
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bc884dc6eac870563f6d4cc46fe9b44f
http://hdl.handle.net/1887/3248780
http://hdl.handle.net/1887/3248780
Autor:
L Alejandro, Rojas, Erin, Valentine, Anthony, Accorsi, Joseph, Maglio, Ning, Shen, Alan, Robertson, Steven, Kazmirski, Peter, Rahl, Rabi, Tawil, Diego, Cadavid, Lorin A, Thompson, Lucienne, Ronco, Aaron N, Chang, Angela M, Cacace, Owen, Wallace
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 374(3)
Facioscapulohumeral muscular dystrophy (FSHD) is caused by the loss of repression at the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::500c224e145228b85b4151d65af3bc29
https://pubmed.ncbi.nlm.nih.gov/32576599
https://pubmed.ncbi.nlm.nih.gov/32576599
Autor:
Nicholas A. Meanwell, Kevin J. Robbins, Carolyn Diane Dzierba, Rick L. Pieschl, Ramkumar Rajamani, James Herrington, Lorin A. Thompson, Andrea McClure, Yong-Jin Wu, Michele Matchett, Ronald J. Knox, Brian Lee Venables, Jason M. Guernon, Linda J. Bristow, Richard E. Olson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:958-962
Replacement of the piperidine ring in the lead benzenesulfonamide Nav1.7 inhibitor 1 with a weakly basic morpholine core resulted in a significant reduction in Nav1.7 inhibitory activity, but the activity was restored by shortening the linkage from m
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e7ad493840369e26cbfb8ea5aabd0b90
https://doi.org/10.1016/j.bmcl.2018.01.035
https://doi.org/10.1016/j.bmcl.2018.01.035
Autor:
Billy Stuart, Keqiang Xie, David Matson, Paul Bruno, Christopher Moxham, Lorin A. Thompson, Serena J. Silver, Ivan Efremov, Mark S. Roth
Publikováno v:
Blood. 138:2018-2018
Sickle cell disease (SCD) is a genetic disorder of the red blood cells caused by a mutation in the HBB gene, which results in red blood cell sickling, hemolysis, vaso-occlusive crises (VOCs), and other complications. Increasing HbF has the potential
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::365bc9cb3e066b8f3f01df3fd8aae5c0
https://doi.org/10.1182/blood-2021-151426
https://doi.org/10.1182/blood-2021-151426
Autor:
Alan S. Robertson, Dieter M. Drexler, Michael K. Ahlijanian, Lawrence G. Iben, Charles F. Albright, Richard E. Olson, Lorin A. Thompson, Martyn Banks, Gregory D. Vite, Jeremy H. Toyn, Cong Wei, Jere E. Meredith
Publikováno v:
European Journal of Pharmacology. 812:104-112
Alzheimer's disease is associated with the accumulation of amyloid-β (Aβ) in the brain. In particular, the 42-amino acid form, Aβ1-42, is thought to play a key role in the disease. It is therefore of interest that diverse compounds, known as γ-se
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f0ef13a72a3178b74444c96d0fe0f4ee
https://doi.org/10.1016/j.ejphar.2017.07.019
https://doi.org/10.1016/j.ejphar.2017.07.019