Michele McElvain
Overview
Explore the profile of Michele McElvain including associated specialties, affiliations and a list of published articles.
Author names and details appear as published. Due to indexing inconsistencies, multiple individuals may share a name, and a single author may have variations. MedLuna displays this data as publicly available, without modification or verification
Snapshot
Snapshot
Articles
10
Citations
84
Followers
0
Related Specialties
Related Specialties
Top 10 Co-Authors
Top 10 Co-Authors
Published In
Published In
Affiliations
Affiliations
Soon will be listed here.
Recent Articles
1.
Harrington P, Croghan M, Fotsch C, Frohn M, Lanman B, Pennington L, et al.
ACS Med Chem Lett
. 2014 Jun;
3(1):74-8.
PMID: 24900374
The optimization of a series of S1P1 agonists with limited activity against S1P3 is reported. A polar headgroup was used to improve the physicochemical and pharmacokinetic parameters of lead quinolinone...
2.
Cee V, Frohn M, Lanman B, Golden J, Muller K, Neira S, et al.
ACS Med Chem Lett
. 2014 Jun;
2(2):107-12.
PMID: 24900288
The optimization of a series of thiazolopyridine S1P1 agonists with limited activity at the S1P3 receptor is reported. These efforts resulted in the discovery of 1-(3-fluoro-4-(5-(1-phenylcyclopropyl)thiazolo-[5,4-b]pyridin-2-yl)benzyl)azetidine-3-carboxylic acid (5d, AMG 369),...
3.
Lanman B, Cee V, Cheruku S, Frohn M, Golden J, Lin J, et al.
ACS Med Chem Lett
. 2014 Jun;
2(2):102-6.
PMID: 24900287
Optimization of a benzofuranyl S1P1 agonist lead compound (3) led to the discovery of 1-(3-fluoro-4-(5-(2-fluorobenzyl)benzo[d]thiazol-2-yl)benzyl)azetidine-3-carboxylic acid (14), a potent S1P1 agonist with minimal activity at S1P3. Dosed orally at 0.3...
4.
Saha A, Yu X, Lin J, Lobera M, Sharadendu A, Chereku S, et al.
ACS Med Chem Lett
. 2014 Jun;
2(2):97-101.
PMID: 24900286
We have discovered novel benzofuran-based S1P1 agonists with excellent in vitro potency and selectivity. 1-((4-(5-Benzylbenzofuran-2-yl)-3-fluorophenyl)methyl) azetidine-3-carboxylic acid (18) is a potent S1P1 agonist with >1000× selectivity over S1P3. It demonstrated...
5.
Pennington L, Sham K, Pickrell A, Harrington P, Frohn M, Lanman B, et al.
ACS Med Chem Lett
. 2014 Jun;
2(10):752-7.
PMID: 24900263
The sphingosine-1-phosphate-1 receptor (S1P1) and its endogenous ligand sphingosine-1-phosphate (S1P) cooperatively regulate lymphocyte trafficking from the lymphatic system. Herein, we disclose 4-methoxy-N-[2-(trifluoromethyl)biphenyl-4-ylcarbamoyl]nicotinamide (8), an uncommon example of a synthetic S1P1...
6.
Xu H, McElvain M, Fiorino M, Henkle B, Sherman L, Xu Y, et al.
J Biomol Screen
. 2013 May;
18(9):997-1007.
PMID: 23686102
Surrogate readouts of G-protein-coupled receptor signaling pathways using highly engineered systems are often employed in the drug discovery process. However, accumulating data have demonstrated the importance of selecting relevant biological...
7.
Reed A, Lanman B, Neira S, Harrington P, Sham K, Frohn M, et al.
Bioorg Med Chem Lett
. 2012 Jan;
22(4):1779-83.
PMID: 22257889
Replacement of the azetidine carboxylate of an S1P(1) agonist development candidate, AMG 369, with a range of acyclic head-groups led to the identification of a novel, S1P(3)-sparing S1P(1) agonist, (-)-2-amino-4-(3-fluoro-4-(5-(1-phenylcyclopropyl)thiazolo[5,4-b]pyridin-2-yl)phenyl)-2-methylbutanoic...
8.
Pennington L, Croghan M, Sham K, Pickrell A, Harrington P, Frohn M, et al.
Bioorg Med Chem Lett
. 2011 Nov;
22(1):527-31.
PMID: 22104144
We reveal how a N-scan SAR strategy (systematic substitution of each CH group with a N atom) was employed for quinolinone-based S1P(1) agonist 5 to modulate physicochemical properties and optimize...
9.
Frohn M, Cee V, Lanman B, Pickrell A, Golden J, Rivenzon-Segal D, et al.
Bioorg Med Chem Lett
. 2011 Nov;
22(1):628-33.
PMID: 22100314
An SAR campaign designed to increase polarity in the 'tail' region of benzothiazole 1 resulted in two series of structurally novel 5-and 6-substituted S1P(1) agonists. Structural optimization for potency ultimately...
10.
Burli R, Xu H, Zou X, Muller K, Golden J, Frohn M, et al.
Bioorg Med Chem Lett
. 2006 May;
16(14):3713-8.
PMID: 16697190
We report the discovery of potent agonists for the human formyl-peptide-like 1 receptor (hFPRL1). These compounds did not act at a closely related receptor denoted human formyl peptide receptor (hFPR)...