Zobrazeno 1 - 10
of 15
pro vyhledávání: '"Laura J. Signor"'
Autor:
Sokhom S. Pin, Deborah A. Cook, John E. Macor, Laura J. Signor, Carl Davis, Valerie J. Whiterock, Gene M. Dubowchik, Richard Schartman, Ping Chen, Chaturvedula Prasad, Kimberly A. Widmann, George Thalody, Walter Kostich, Robert Macci, John J. Herbst, Stephen E. Mercer, Charles M. Conway, Cen Xu
Publikováno v:
Bioorganicmedicinal chemistry letters. 31
Calcitonin gene-related peptide (CGRP) receptor antagonists have been shown clinically to be effective treatments for migraine. Zavegepant (BHV-3500, BMS-742413) is a high affinity antagonist of the CGRP receptor (hCGRP Ki = 0.023 nM) that has demons
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5f1b018775ed0613c97b43faeac8e918
https://pubmed.ncbi.nlm.nih.gov/33096162
https://pubmed.ncbi.nlm.nih.gov/33096162
Autor:
Yulia Benitex, Michael R. Weed, Laura J. Signor, Richard E. Olson, Deborah Keavy, Robert Zaczek, Linda J. Bristow, Daniel G. Morgan, Joseph Polino, Mark Bookbinder, Dalton King, John E. Macor
Publikováno v:
PLoS ONE
PLoS ONE, Vol 12, Iss 12, p e0187609 (2017)
PLoS ONE, Vol 12, Iss 12, p e0187609 (2017)
Agonists at the nicotinic acetylcholine alpha 7 receptor (nAChR α7) subtype have the potential to treat cognitive deficits in patients with Alzheimer's disease (AD) or schizophrenia. Visuo-spatial paired associates learning (vsPAL) is a task that ha
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::585b43b4db7b4e1142684dfbf105df16
https://pubmed.ncbi.nlm.nih.gov/29261656
https://pubmed.ncbi.nlm.nih.gov/29261656
Autor:
John E. Macor, Chaturvedula Prasad, Rex Denton, Gene M. Dubowchik, Paul Moench, Valerie J. Whiterock, Charlie M. Conway, Cen Xu, Neil Mathias, Glenn H. Cantor, Robert Macci, Richard Schartman, Laura J. Signor, Stephen E. Mercer, George Thalody, Carl D. Davis, Deborah Keavy, Sokhom S. Pin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:3157-3161
Calcitonin gene-related peptide (CGRP) receptor antagonists have been shown to be efficacious as abortive migraine therapeutics with the absence of cardiovascular liabilities that are associated with triptans. Herein, we report the discovery of a hig
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::78ac514e0ff9910e3b128930ebdf5765
https://doi.org/10.1016/j.bmcl.2013.04.012
https://doi.org/10.1016/j.bmcl.2013.04.012
Autor:
George Thalody, Paul Moench, Valerie J. Whiterock, Deborah A. Cook, Charles M. Conway, Xiang-Jun Jiang, Laura J. Signor, Neil Mathias, Richard Schartman, Carl D. Davis, Cen Xu, Robert Macci, Xiaojun Han, George O. Tora, Sokhom S. Pin, John E. Macor, Gene M. Dubowchik, Andrew P. Degnan, Rita L. Civiello
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:1870-1873
Various substituted indazole and benzoxazolone amino acids were investigated as d -tyrosine surrogates in highly potent CGRP receptor antagonists. Compound 3, derived from the 7-methylindazole core, afforded a 30-fold increase in CGRP binding potency
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9efad766cca18838d811178ca1ce78b8
https://doi.org/10.1016/j.bmcl.2013.01.011
https://doi.org/10.1016/j.bmcl.2013.01.011
Autor:
Marc Browning, Richard Schartman, Kimberley A. Lentz, Kenneth S. Santone, John E. Macor, Deborah Keavy, Gene M. Dubowchik, John G. Houston, Gary Tong, Walter Kostich, Charles M. Conway, Laura J. Signor, Guanglin Luo, Rex Denton, Ling Chen
Publikováno v:
Journal of Medicinal Chemistry. 55:10644-10651
Calcitonin gene-related peptide (CGRP) receptor antagonists have demonstrated clinical efficacy in the treatment of acute migraine. Herein, we describe the design, synthesis, and preclinical characterization of a highly potent, oral CGRP receptor ant
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3127659bf95ad7ce1a09e039252cc297
https://doi.org/10.1021/jm3013147
https://doi.org/10.1021/jm3013147
Autor:
Carl D. Davis, Laura J. Signor, Chaturvedula Prasad, George Thalody, Richard Schartman, Gene M. Dubowchik, Rita L. Civiello, John E. Macor, Charles M. Conway, Shelly X. Ren, Robert Macci, Xiaojun Han, Deborah A. Cook, Kimberly A. Widmann, Cen Xu, Sokhom S. Pin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:4723-4727
We have systematically studied the effects of varying the central unnatural amino acid moiety on CGRP receptor antagonist potency and CYP inhibition in a series of ureidoamides. In this Letter, we report the discovery of compound 23, a potent CGRP re
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0bc3bbed405bf048163d0f84953dedba
https://doi.org/10.1016/j.bmcl.2012.05.074
https://doi.org/10.1016/j.bmcl.2012.05.074
Autor:
Neil Mathias, Sokhom S. Pin, Xiaojun Han, Paul Moench, John E. Macor, Richard Schartman, Charles M. Conway, Chaturvedula Prasad, Rex Denton, Kimberly A. Widmann, Laura J. Signor, Gene M. Dubowchik, Deborah A. Cook, Andrew P. Degnan, George Thalody, Robert Macci, Carl D. Davis, Shelly X. Ren, Cen Xu
Publikováno v:
Journal of Medicinal Chemistry. 51:4858-4861
Calcitonin gene-related peptide (CGRP) has been implicated in the pathogenesis of migraine. Early chemistry leads suffered from modest potency, significant CYP3A4 inhibition, and poor aqueous solubility. Herein, we describe the optimization of these
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::fa440795b5aa2edcd0d1f4a3cb63ab67
https://doi.org/10.1021/jm800546t
https://doi.org/10.1021/jm800546t
Autor:
Piyasena Hewawasam, Robert A. Myers, Nicholas J. Lodge, Kimberly Newberry, Shaun Langdon, Alicia V. Lee, Digavalli V. Sivarao, Laura J. Signor, Mary Jane Plym
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 313:840-847
We evaluated the effects of 4-(5-chloro-2-hydroxyphenyl)-3-(2-hydroxyethyl)-6-(trifluoromethyl)-quinolin-2(1H)-one (BMS-223131), an opener of large conductance Ca(2+)-activated potassium (maxi-K) channels, on normal and stress-exacerbated colonic mot
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::6b8a9a219eafe737e533d6c78c27fc68
https://doi.org/10.1124/jpet.104.079285
https://doi.org/10.1124/jpet.104.079285
Autor:
David G. Harden, David Weaver, Ronald J. Knox, Laura J. Signor, Torben R. Neelands, Robert A. Myers, George Thalody, Svetlana Tertyshnikova, Mary Jane Plym, Nicholas J. Lodge, Corinne Griffin
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 313:250-259
BL-1249 [(5,6,7,8-tetrahydro-naphthalen-1-yl)-[2-(1H-tetrazol-5-yl)-phenyl]-amine] produced a concentration-dependent membrane hyperpolarization of cultured human bladder myocytes, assessed as either a reduction in fluorescence of the voltage-sensiti
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c9a13aca937333444f90cdf113315659
https://doi.org/10.1124/jpet.104.078592
https://doi.org/10.1124/jpet.104.078592
Autor:
Richard Schartman, Ling Chen, Kimberley A. Lentz, Deborah Keavy, Michael Gulianello, John E. Macor, Charles M. Conway, Yanling Huang, Laura J. Signor, Guanglin Luo, Rex Denton, Marc Browning, Gene M. Dubowchik, Walter Kostich, Stephen E. Mercer
Publikováno v:
ACS medicinal chemistry letters. 3(4)
Calcitonin gene-related peptide (CGRP) receptor antagonists have been clinically shown to be effective in the treatment of migraine, but identification of potent and orally bioavailable compounds has been challenging. Herein, we describe the conceptu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e182de554c9db033826e9fcf1a0b43f1
https://pubmed.ncbi.nlm.nih.gov/24900474
https://pubmed.ncbi.nlm.nih.gov/24900474