Keith J Miller
Overview
Explore the profile of Keith J Miller including associated specialties, affiliations and a list of published articles.
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17
Citations
600
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Recent Articles
1.
Carpenter J, Wang Y, Wu G, Feng J, Ye X, Morales C, et al.
J Med Chem
. 2017 Jun;
60(14):6166-6190.
PMID: 28635286
Agonism of the 5-HT receptor represents one of the most well-studied and clinically proven mechanisms for pharmacological weight reduction. Selectivity over the closely related 5-HT and 5-HT receptors is critical...
2.
Wacker D, Wang Y, Broekema M, Rossi K, OConnor S, Hong Z, et al.
J Med Chem
. 2014 Sep;
57(18):7499-508.
PMID: 25208139
G-protein-coupled receptor 119 (GPR119) is expressed predominantly in pancreatic β-cells and in enteroendocrine cells in the gastrointestinal tract. GPR119 agonists have been shown to stimulate glucose-dependent insulin release by direct...
3.
Ye X, Morales C, Wang Y, Rossi K, Malmstrom S, Abousleiman M, et al.
Bioorg Med Chem Lett
. 2014 Apr;
24(11):2539-45.
PMID: 24755425
Through appropriate medicinal chemistry design tactics and computer-assisted conformational modeling, the initial lead A was evolved into a series of dihydrobenzofuran derivatives 3 as potent GPR119 agonists. This Letter describes...
4.
Zhao G, Kwon C, Bisaha S, Stein P, Rossi K, Cao X, et al.
Bioorg Med Chem Lett
. 2013 May;
23(13):3914-9.
PMID: 23683593
The 5-HT2C receptor has been implicated as a critical regulator of appetite. Small molecule activation of the 5-HT2C receptor has been shown to affect food intake and regulate body weight...
5.
Fevig J, Feng J, Rossi K, Miller K, Wu G, Hung C, et al.
Bioorg Med Chem Lett
. 2012 Nov;
23(1):330-5.
PMID: 23177783
A series of 2,3,3a,4-tetrahydro-1H-pyrrolo[3,4-c]isoquinolin-5(9bH)-ones is described, several examples of which exhibit potent 5-HT(2C) agonism with excellent selectivity over the closely related 5-HT(2A) and 5-HT(2B) receptors. Compounds such as 38 and...
6.
Yang Y, Miller K, Zhu Y, Hong Y, Tian Y, Murugesan N, et al.
Bioorg Med Chem Lett
. 2011 Oct;
21(22):6856-60.
PMID: 21962575
Obesity remains a significant public health issue leading to Type II diabetes and cardiovascular disease. CB1 antagonists have been shown to suppress appetite and reduce body weight in animal models...
7.
Miller K, Wacker D
Future Med Chem
. 2011 Mar;
2(12):1761-75.
PMID: 21428799
Ever since the observation of late-onset obesity during the phenotypic characterization of the 5-HT(₂C) knock-out mouse, the serotonin 5-HT(₂C) receptor has been a drug target for obesity. Small-molecule agonists have...
8.
Tricyclic dihydroquinazolinones as novel 5-HT2C selective and orally efficacious anti-obesity agents
Ahmad S, Ngu K, Miller K, Wu G, Hung C, Malmstrom S, et al.
Bioorg Med Chem Lett
. 2009 Dec;
20(3):1128-33.
PMID: 20022752
Agonists of the 5-HT(2C) receptor have been shown to suppress appetite and reduce body weight in animal models as well as in humans. However, agonism of the related 5-HT(2B) receptor...
9.
Miller K, Wu G, Varnes J, Levesque P, Li J, Li D, et al.
Mol Pharmacol
. 2009 Sep;
76(6):1211-9.
PMID: 19767451
Successful development of 5-HT(2C) agonists requires selectivity versus the highly homologous 5-HT(2A) receptor, because agonism at this receptor can result in significant adverse events. (R)-9-Ethyl-1,3,4,10b-tetrahydro-7-trifluoromethylpyrazino[2,1-a]isoindol-6(2H)-one (compound 1) is a potent...
10.
Agonists of the serotonin 5-HT2C receptor: preclinical and clinical progression in multiple diseases
Wacker D, Miller K
Curr Opin Drug Discov Devel
. 2008 Jul;
11(4):438-45.
PMID: 18600561
The serotonin 5-HT2C receptor is a G-protein-coupled receptor and is one of the 14 subtypes that constitutes the serotonin receptor family. Agonists of 5-HT2C have been implicated as potential treatments...