Edward L Conn
Overview
Explore the profile of Edward L Conn including associated specialties, affiliations and a list of published articles.
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17
Citations
224
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Recent Articles
1.
Aspnes G, Bagley S, Coffey S, Conn E, Curto J, Edmonds D, et al.
Bioorg Med Chem Lett
. 2023 Aug;
94:129454.
PMID: 37591316
Activation of the glucagon-like peptide-1 (GLP-1) receptor stimulates insulin release, lowers plasma glucose levels, delays gastric emptying, increases satiety, suppresses food intake, and affords weight loss in humans. These beneficial...
2.
Conn E, Perry M, Shi K, Wang G, Hoy S, Sach N, et al.
Org Biomol Chem
. 2022 Apr;
20(18):3747-3754.
PMID: 35448901
α-Branched heteroaryl amines are prevalent motifs in drugs and are typically prepared through C-N bond formation. In contrast, C-C bond-forming approaches to branched amines may dramatically expand available chemical space...
3.
Filipski K, Sammons M, Bhattacharya S, Panteleev J, Brown J, Loria P, et al.
ACS Med Chem Lett
. 2018 May;
9(5):440-445.
PMID: 29795756
Sodium-phosphate cotransporter 2a, or NaPi2a (SLC34A1), is a solute-carrier (SLC) transporter located in the kidney proximal tubule that reabsorbs glomerular-filtered phosphate. Inhibition of NaPi2a may enhance urinary phosphate excretion and...
4.
Edmonds D, Kung D, Kalgutkar A, Filipski K, Ebner D, Cabral S, et al.
J Med Chem
. 2018 Feb;
61(6):2372-2383.
PMID: 29466005
Optimization of the pharmacokinetic (PK) properties of a series of activators of adenosine monophosphate-activated protein kinase (AMPK) is described. Derivatives of the previously described 5-aryl-indole-3-carboxylic acid clinical candidate (1) were...
5.
Huard K, Ahn K, Amor P, Beebe D, Borzilleri K, Chrunyk B, et al.
J Med Chem
. 2017 Aug;
60(18):7835-7849.
PMID: 28853885
Increased fructose consumption and its subsequent metabolism have been implicated in hepatic steatosis, dyslipidemia, obesity, and insulin resistance in humans. Since ketohexokinase (KHK) is the principal enzyme responsible for fructose...
6.
Cameron K, Kung D, Kalgutkar A, Kurumbail R, Miller R, Salatto C, et al.
J Med Chem
. 2016 Aug;
59(17):8068-81.
PMID: 27490827
Adenosine monophosphate-activated protein kinase (AMPK) is a protein kinase involved in maintaining energy homeostasis within cells. On the basis of human genetic association data, AMPK activators were pursued for the...
7.
Liang S, Chen J, Normandin M, Chang J, Chang G, Taylor C, et al.
Angew Chem Int Ed Engl
. 2016 Jun;
55(33):9601-5.
PMID: 27355874
Glycogen synthase kinase-3 (GSK-3) regulates multiple cellular processes in diabetes, oncology, and neurology. N-(3-(1H-1,2,4-triazol-1-yl)propyl)-5-(3-chloro-4-methoxyphenyl)oxazole-4-carboxamide (PF-04802367 or PF-367) has been identified as a highly potent inhibitor, which is among the most...
8.
Eng H, Sharma R, Wolford A, Di L, Ruggeri R, Buckbinder L, et al.
Drug Metab Dispos
. 2016 Apr;
44(8):1262-9.
PMID: 27079250
N1-Substituted-6-arylthiouracils, represented by compound 1 [6-(2,4-dimethoxyphenyl)-1-(2-hydroxyethyl)-2-thioxo-2,3-dihydropyrimidin-4(1H)-one], are a novel class of selective irreversible inhibitors of human myeloperoxidase. The present account is a summary of our in vitro studies on the...
9.
Ruggeri R, Buckbinder L, Bagley S, Carpino P, Conn E, Dowling M, et al.
J Med Chem
. 2015 Oct;
58(21):8513-28.
PMID: 26509551
Myeloperoxidase (MPO) is a heme peroxidase that catalyzes the production of hypochlorous acid. Clinical evidence suggests a causal role for MPO in various autoimmune and inflammatory disorders including vasculitis and...
10.
Calabrese M, Rajamohan F, Harris M, Caspers N, Magyar R, Withka J, et al.
Structure
. 2014 Jul;
22(8):1161-1172.
PMID: 25066137
AMP-activated protein kinase (AMPK) is a principal metabolic regulator affecting growth and response to cellular stress. Comprised of catalytic and regulatory subunits, each present in multiple forms, AMPK is best...