Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Katherine J, Watson"'
Autor:
Sichen Chang, Jonathan W. Dickerson, Baker Logan A, Thomas M. Bridges, Craig W. Lindsley, Darren W. Engers, Aidong Qi, Jerri M. Rook, Aaron M. Bender, P. Jeffrey Conn, Katrina A. Bollinger, Colleen M. Niswender, Changho Han, Alice L. Rodriguez, Trever R Carter, Li Peng, Julie L. Engers, Jordan C. O’Neill, Matthew Spock, Katherine J. Watson
Publikováno v:
ACS Med Chem Lett
[Image: see text] Herein, we report the SAR leading to the discovery of VU6028418, a potent M(4) mAChR antagonist with high subtype-selectivity and attractive DMPK properties in vitro and in vivo across multiple species. VU6028418 was subsequently ev
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::388290e5061b99e6a85f95357b9a3b32
https://doi.org/10.1021/acsmedchemlett.1c00363
https://doi.org/10.1021/acsmedchemlett.1c00363
Autor:
Jerri M. Rook, Aaron M. Bender, Colleen M. Niswender, Yuping Donsante, P. Jeffrey Conn, Hyekyung P. Cho, Li Peng, Julie L. Engers, Jonathan W. Dickerson, Thomas M. Bridges, Craig W. Lindsley, Ellen J. Hess, Sichen Chang, Aidong Qi, Weimin Peng, Mark S. Moehle, Jordan C. O’Neill, Daniel J. Foster, Alice L. Rodriguez, Zoey Bryant, Katherine J. Watson, Kaylee J. Stillwell
Publikováno v:
ACS Pharmacology & Translational Science. 4:1306-1321
Nonselective antagonists of muscarinic acetylcholine receptors (mAChRs) that broadly inhibit all five mAChR subtypes provide an efficacious treatment for some movement disorders, including Parkinson's disease and dystonia. Despite their efficacy in t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::f5425dfe0a6fb74da410878130ec6660
https://doi.org/10.1021/acsptsci.0c00162
https://doi.org/10.1021/acsptsci.0c00162
Autor:
Sichen Chang, Ellen J. Hess, Jerri M. Rook, Jonathan W. Dickerson, Colleen M. Niswender, Yuping Donsante, Weimin Peng, Craig W. Lindsley, Li Peng, Julie L. Engers, Thomas M. Bridges, Mark S. Moehle, Daniel J. Foster, P. Jeffrey Conn, Aaron M. Bender, Alice L. Rodriguez, Zoey Bryant, Katherine J. Watson, Jordan C. O’Neill
Non-selective antagonists of muscarinic acetylcholine receptors (mAChRs) that broadly inhibit all five mAChR subtypes provide an efficacious treatment for some movement disorders, including Parkinson disease and dystonia. Despite their efficacy in th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::b2f6ae5b896aa0960348eb4cabab3c6e
https://doi.org/10.1101/2020.10.12.324152
https://doi.org/10.1101/2020.10.12.324152
Autor:
Mark S, Moehle, Aaron M, Bender, Jonathan W, Dickerson, Daniel J, Foster, Aidong, Qi, Hyekyung P, Cho, Yuping, Donsante, Weimin, Peng, Zoey, Bryant, Kaylee J, Stillwell, Thomas M, Bridges, Sichen, Chang, Katherine J, Watson, Jordan C, O'Neill, Julie L, Engers, Li, Peng, Alice L, Rodriguez, Colleen M, Niswender, Craig W, Lindsley, Ellen J, Hess, P Jeffrey, Conn, Jerri M, Rook
Publikováno v:
ACS Pharmacol Transl Sci
[Image: see text] Nonselective antagonists of muscarinic acetylcholine receptors (mAChRs) that broadly inhibit all five mAChR subtypes provide an efficacious treatment for some movement disorders, including Parkinson’s disease and dystonia. Despite
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::201a9605778eafcb97e04614395cae35
https://pubmed.ncbi.nlm.nih.gov/34423268
https://pubmed.ncbi.nlm.nih.gov/34423268
Autor:
Kayla J, Temple, Madeline F, Long, Julie L, Engers, Katherine J, Watson, Sichen, Chang, Vincent B, Luscombe, Alice L, Rodriguez, Colleen M, Niswender, Thomas M, Bridges, P Jeffrey, Conn, Darren W, Engers, Craig W, Lindsley
Publikováno v:
Bioorganicmedicinal chemistry letters. 30(4)
This Letter details our efforts to develop new M
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::7384adfc16b9138de884f35943cb26f7
https://pubmed.ncbi.nlm.nih.gov/31787491
https://pubmed.ncbi.nlm.nih.gov/31787491
Autor:
Kayla J, Temple, Julie L, Engers, Madeline F, Long, Alison R, Gregro, Katherine J, Watson, Sichen, Chang, Matthew T, Jenkins, Vincent B, Luscombe, Alice L, Rodriguez, Colleen M, Niswender, Thomas M, Bridges, P Jeffrey, Conn, Darren W, Engers, Craig W, Lindsley
Publikováno v:
Bioorganicmedicinal chemistry letters. 29(21)
This Letter details our efforts to replace the 2,4-dimethylquinoline carboxamide core of our previous M
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::90183d5613a7cb2ebcf04c4e0ac575f6
https://pubmed.ncbi.nlm.nih.gov/31537424
https://pubmed.ncbi.nlm.nih.gov/31537424
Autor:
Craig W. Lindsley, Thomas M. Bridges, Colleen M. Niswender, Sichen Chang, Darren W. Engers, Kayla J. Temple, P. Jeffrey Conn, Vincent B. Luscombe, Madeline F. Long, Matthew T. Jenkins, Katherine J. Watson, Alice L. Rodriguez, Julie L. Engers
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 30:126812
This Letter details our efforts to discover structurally unique M4 PAMs containing 5,6-heteroaryl ring systems. In an attempt to improve the DMPK profiles of the 2,3-dimethyl-2H-indazole-5-carboxamide and 1-methyl-1H-benzo[d][1,2,3]triazole-6-carboxa
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::5e98c856bb55c440e8275c820fed0152
https://doi.org/10.1016/j.bmcl.2019.126812
https://doi.org/10.1016/j.bmcl.2019.126812
Autor:
P. Jeffrey Conn, Julie L. Engers, Kayla J. Temple, Colleen M. Niswender, Craig W. Lindsley, Darren W. Engers, Madeline F. Long, Thomas M. Bridges, Sichen Chang, Vincent B. Luscombe, Katherine J. Watson, Alice L. Rodriguez
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 30:126811
This Letter details our efforts to develop new M4 PAM scaffolds with improved pharmacological properties. This endeavor involved replacing the 3,4-dimethylpyridazine core with two novel cores: a 2,3-dimethyl-2H-indazole-5-carboxamide core or a 1-meth
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::b357d1915985128a63e2a37346709cc5
https://doi.org/10.1016/j.bmcl.2019.126811
https://doi.org/10.1016/j.bmcl.2019.126811
Autor:
Alice L. Rodriguez, Julie L. Engers, Madeline F. Long, Darren W. Engers, Matthew T. Jenkins, Colleen M. Niswender, Thomas M. Bridges, Kayla J. Temple, Sichen Chang, Alison R. Gregro, Katherine J. Watson, Vincent B. Luscombe, P. Jeffrey Conn, Craig W. Lindsley
This Letter details our efforts to replace the 3-amino moiety, an essential pharmacophore for M4 PAM activity in most M4 PAMs to date, within the thieno[2,3-b]pyridine core, as the β-amino carboxamide motif has been shown to engender poor solubility
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::407d7c57d88c0607fd18163f0250eb7d
https://europepmc.org/articles/PMC5784840/
https://europepmc.org/articles/PMC5784840/
Autor:
Kayla J. Temple, Julie L. Engers, Madeline F. Long, Alison R. Gregro, Katherine J. Watson, Sichen Chang, Matthew T. Jenkins, Vincent B. Luscombe, Alice L. Rodriguez, Colleen M. Niswender, Thomas M. Bridges, P. Jeffrey Conn, Darren W. Engers, Craig W. Lindsley
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 29:126678
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::84481d1131d221b3315c3d32eca00b49
https://doi.org/10.1016/j.bmcl.2019.126678
https://doi.org/10.1016/j.bmcl.2019.126678