Michael A Galella
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Explore the profile of Michael A Galella including associated specialties, affiliations and a list of published articles.
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20
Citations
154
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Recent Articles
1.
Wurtz N, Johnson J, Viet A, Shirude P, Baligar V, Madduri S, et al.
ACS Med Chem Lett
. 2022 Jun;
13(6):943-948.
PMID: 35707160
Formyl peptide receptor 2 (FPR2) agonists have shown efficacy in inflammatory-driven animal disease models and have the potential to treat a range of diseases. Many reported synthetic agonists contain a...
2.
Dilger A, Pabbisetty K, Corte J, De Lucca I, Fang T, Yang W, et al.
J Med Chem
. 2021 Sep;
65(3):1770-1785.
PMID: 34494428
Factor XIa (FXIa) is an enzyme in the coagulation cascade thought to amplify thrombin generation but has a limited role in hemostasis. From preclinical models and human genetics, an inhibitor...
3.
Tora G, Jiang J, Bostwick J, Gargalovic P, Onorato J, Luk C, et al.
Bioorg Med Chem Lett
. 2021 Aug;
50:128325.
PMID: 34403724
Heart failure (HF) treatment remains a critical unmet medical need. Studies in normal healthy volunteers and HF patients have shown that [Pyr]apelin-13, the endogenous ligand for the APJ receptor, improves...
4.
La Cruz T, Gonzalez-Bobes F, Eastgate M, Sfouggatakis C, Zheng B, Kopp N, et al.
J Org Chem
. 2021 Aug;
87(4):1996-2011.
PMID: 34355895
BMS-813160 is a pharmaceutical entity currently in development at Bristol Myers Squibb. Its defining structural feature is a unique chiral all triamino cyclohexane core. Medicinal and process chemistry groups at...
5.
Johnson J, Kim S, Jiang J, Phillips M, Schumacher W, Bostwick J, et al.
J Med Chem
. 2021 Mar;
64(6):3086-3099.
PMID: 33689340
Apelin-13 is an endogenous peptidic agonist of the apelin receptor (APJ) receptor with the potential for improving cardiac function in heart failure patients. However, the low plasma stability of apelin-13...
6.
Srivastava A, Ko S, Watterson S, Pattoli M, Skala S, Cheng L, et al.
ACS Med Chem Lett
. 2020 Nov;
11(11):2195-2203.
PMID: 33214829
Bruton's tyrosine kinase (BTK) has been shown to play a key role in the pathogenesis of autoimmunity. Therefore, the inhibition of the kinase activity of BTK with a small molecule...
7.
Jiang B, Duan J, Stachura S, Karmakar A, Hemagiri H, Raut D, et al.
Bioorg Med Chem Lett
. 2020 Aug;
30(17):127392.
PMID: 32738966
A novel series of cis-3,4-diphenylpyrrolidines were designed as RORγt inverse agonists based on the binding conformation of previously reported bicyclic sulfonamide 1. Preliminary synthesis and structure-activity relationship (SAR) study established...
8.
Watterson S, Liu Q, Bertrand M, Batt D, Li L, Pattoli M, et al.
J Med Chem
. 2019 Mar;
62(7):3228-3250.
PMID: 30893553
Bruton's tyrosine kinase (BTK), a non-receptor tyrosine kinase, is a member of the Tec family of kinases and is essential for B cell receptor (BCR) mediated signaling. BTK also plays...
9.
Duan J, Lu Z, Jiang B, Stachura S, Weigelt C, Sack J, et al.
ACS Med Chem Lett
. 2019 Mar;
10(3):367-373.
PMID: 30891142
A new phenyl (3-phenylpyrrolidin-3-yl)sulfone series of RORγt inverse agonists was discovered utilizing the binding conformation of previously reported bicyclic sulfonamide . Through a combination of structure-based design and structure-activity relationship...
10.
Gong H, Weinstein D, Lu Z, Duan J, Stachura S, Haque L, et al.
Bioorg Med Chem Lett
. 2017 Dec;
28(2):85-93.
PMID: 29233651
We disclose the optimization of a high throughput screening hit to yield benzothiazine and tetrahydroquinoline sulfonamides as potent RORγt inverse agonists. However, a majority of these compounds showed potent activity...