Gene M Dubowchik
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Explore the profile of Gene M Dubowchik including associated specialties, affiliations and a list of published articles.
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45
Citations
512
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Recent Articles
1.
Hartz R, Ahuja V, Luo G, Chen L, Sivaprakasam P, Xiao H, et al.
J Med Chem
. 2023 May;
66(11):7534-7552.
PMID: 37235865
Glycogen synthase kinase-3 (GSK-3) is a serine/threonine kinase that serves as an important regulator of a broad range of cellular functions. It has been linked to Alzheimer's disease as well...
2.
Hartz R, Ahuja V, Sivaprakasam P, Xiao H, Krause C, Clarke W, et al.
J Med Chem
. 2023 Mar;
66(6):4231-4252.
PMID: 36950863
Glycogen synthase kinase-3 (GSK-3) is a serine/threonine kinase that regulates numerous cellular processes, including metabolism, proliferation, and cell survival. Due to its multifaceted role, GSK-3 has been implicated in a...
3.
Luo G, Chen L, Jacutin-Porte S, Han Y, Burton C, Xiao H, et al.
Bioorg Med Chem Lett
. 2023 Jan;
81:129143.
PMID: 36669575
In our continuing efforts to explore structure-activity relationships around the novel class of potent, isonicotinamide-based GSK3 inhibitors described in our previous report, we extensively explored structural variations around both 4/5-pyridine...
4.
Luo G, Jiang X, Chen L, Conway C, Gulianello M, Kostich W, et al.
Bioorg Med Chem Lett
. 2021 May;
43:128077.
PMID: 33932522
In our efforts to identify orally bioavailable CGRP receptor antagonists, we previously discovered a novel series of orally available azepinone derivatives that unfortunately also exhibited the unwanted property of potent...
5.
Mercer S, Chaturvedula P, Conway C, Cook D, Davis C, Pin S, et al.
Bioorg Med Chem Lett
. 2020 Oct;
31:127624.
PMID: 33096162
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 K ...
6.
Dubowchik G, Conway C, Xin A
J Med Chem
. 2020 Feb;
63(13):6600-6623.
PMID: 32058712
The pivotal role of calcitonin gene-related peptide (CGRP) in migraine pathophysiology was identified over 30 years ago, but the successful clinical development of targeted therapies has only recently been realized....
7.
Lipton R, Croop R, Stock E, Stock D, Morris B, Frost M, et al.
N Engl J Med
. 2019 Jul;
381(2):142-149.
PMID: 31291516
Background: Calcitonin gene-related peptide receptor has been implicated in the pathogenesis of migraine. Rimegepant is an orally administered, small-molecule, calcitonin gene-related peptide receptor antagonist that may be effective in acute...
8.
Trail P, Dubowchik G, Lowinger T
Pharmacol Ther
. 2017 Aug;
181:126-142.
PMID: 28757155
Breast cancer is a heterogeneous group of malignancies with a spectrum of molecular subtypes, pathologies and outcomes that together comprise the most common non-cutaneous cancer in women. Currently, over 80%...
9.
Luo G, Chen L, Conway C, Kostich W, Johnson B, Ng A, et al.
J Org Chem
. 2017 Mar;
82(7):3710-3720.
PMID: 28306261
An asymmetric synthesis of the major metabolite of the calcitonin gene-related peptide recepotor antagonist BMS-846372 is presented. The variously substituted cyclohepta[b]pyridine ring system represents an underexplored ring system and showed...
10.
Civiello R, Han X, Beno B, Chaturvedula P, Herbst J, Xu C, et al.
Bioorg Med Chem Lett
. 2016 Feb;
26(4):1229-32.
PMID: 26832218
Calcitonin gene-related peptide (CGRP) is a potent neuropeptide implicated in the pathophysiology of migraine. In the course of seeking CGRP antagonists with improved oral bioavailability, metabolic stability, and pharmacokinetic properties,...