Aaron S Goetz
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Explore the profile of Aaron S Goetz including associated specialties, affiliations and a list of published articles.
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13
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603
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Recent Articles
1.
Goetz A, Ignar D
Curr Protoc Pharmacol
. 2011 Sep;
Chapter 1:Unit1.28.
PMID: 21956799
This unit describes a Scintillation Proximity Assay (SPA) for the measurement of ligand binding to melanocortin receptors (MCRs) using membranes prepared from cell lines stably expressing recombinant MCRs. It provides...
2.
Ignar D, Goetz A, Noble K, Carballo L, Stroup A, Fisher J, et al.
J Pharmacol Exp Ther
. 2011 Jun;
339(1):24-34.
PMID: 21712426
μ-Opioid receptor (MOR) agonism induces palatable food consumption principally through modulation of the rewarding properties of food. N-{[3,5-difluoro-3'-(1H-1,2,4-triazol-3-yl)-4-biphenylyl]methyl}-2,3-dihydro-1H-inden-2-amine (GSK1521498) is a novel opioid receptor inverse agonist that, on the basis...
3.
Zhang C, Westaway S, Speake J, Bishop M, Goetz A, Carballo L, et al.
Bioorg Med Chem Lett
. 2011 Jan;
21(2):670-6.
PMID: 21193310
Opioid receptors play an important role in both behavioral and homeostatic functions. We herein report tetrahydroquinoline derivatives as opioid receptor antagonists. SAR studies led to the identification of the potent...
4.
Rheault T, Caferro T, Dickerson S, Donaldson K, Gaul M, Goetz A, et al.
Bioorg Med Chem Lett
. 2008 Dec;
19(3):817-20.
PMID: 19111461
Two new series of potent and selective dual EGFR/ErbB-2 kinase inhibitors derived from novel thienopyrimidine cores have been identified. Isomeric thienopyrimidine cores were evaluated as isosteres for a 4-anilinoquinazoline core...
5.
Carlton D, Collin-Smith L, Daniels A, Deaton D, Goetz A, Laudeman C, et al.
Bioorg Med Chem Lett
. 2008 Sep;
18(20):5451-5.
PMID: 18818070
Starting from a weak omeprazole screening hit, replacement of the pyridine with a 1,3-benzodioxole moiety, modification of the thioether linkage, and substitution of the benzimidazole pharmacophore led to the discovery...
6.
McKeown S, Corbett D, Goetz A, Littleton T, Bigham E, Briscoe C, et al.
Bioorg Med Chem Lett
. 2007 Jan;
17(6):1584-9.
PMID: 17240142
The discovery, synthesis and structure-activity relationship (SAR) of novel carboxylic acid agonists for GPR40 are described. Aryl propionic acid 1, identified from a high throughput screen, was selected for chemical...
7.
Tavares F, Al-Barazanji K, Bishop M, S Britt C, Carlton D, Cooper J, et al.
J Med Chem
. 2006 Nov;
49(24):7108-18.
PMID: 17125263
Genetic manipulation studies in mice at both the MCH receptor 1 (MCHR1) as well as the MCH peptide levels have implicated MCHR1 as a key player in energy homeostasis. The...
8.
Tavares F, Al-Barazanji K, Bigham E, Bishop M, S Britt C, Carlton D, et al.
J Med Chem
. 2006 Nov;
49(24):7095-107.
PMID: 17125262
The high expression of MCH in the hypothalamus with the lean hypophagic phenotype coupled with increased resting metabolic rate and resistance to high fat diet-induced obesity of MCH KO mice...
9.
Carpenter A, Al-Barazanji K, Barvian K, Bishop M, S Britt C, Cooper J, et al.
Bioorg Med Chem Lett
. 2006 Aug;
16(19):4994-5000.
PMID: 16904318
The identification of an MCH R1 antagonist screening hit led to the optimization of a class of benzimidazole-based MCH R1 antagonists. Structure-activity relationships and efforts to optimize pharmacokinetic properties are...
10.
Hertzog D, Al-Barazanji K, Bigham E, Bishop M, S Britt C, Carlton D, et al.
Bioorg Med Chem Lett
. 2006 Jul;
16(18):4723-7.
PMID: 16870432
Optimization of a series of constrained melanin-concentrating hormone receptor 1 (MCH R1) antagonists has provided compounds with potent and selective MCH R1 activity. Details of the optimization process are provided...