Search Results - "SHEARER, Todd W"
-
1
An orally available, brain-penetrant CAMKK2 inhibitor reduces food intake in rodent model
Published in Bioorganic & medicinal chemistry letters (01-06-2018)“…[Display omitted] Hypothalamic CAMKK2 represents a potential mechanism for chemically affecting satiety and promoting weight loss in clinically obese patients…”
Get full text
Journal Article -
2
Total-body creatine pool size and skeletal muscle mass determination by creatine-(methyl-D3) dilution in rats
Published in Journal of applied physiology (1985) (01-06-2012)“…There is currently no direct, facile method to determine total-body skeletal muscle mass for the diagnosis and treatment of skeletal muscle wasting conditions…”
Get full text
Journal Article -
3
Discovery of 3-Aryl-4-isoxazolecarboxamides as TGR5 Receptor Agonists
Published in Journal of medicinal chemistry (24-12-2009)“…A series of 3-aryl-4-isoxazolecarboxamides identified from a high-throughput screening campaign as novel, potent small molecule agonists of the human TGR5…”
Get full text
Journal Article -
4
Role of Specific Cytochrome P450 Isoforms in the Conversion of Phenoxypropoxybiguanide Analogs in Human Liver Microsomes to Potent Antimalarial Dihydrotriazines
Published in Drug metabolism and disposition (01-02-2008)“…Phenoxypropoxybiguanides, such as PS-15, are antimalarial prodrugs analogous to the relationship of proguanil and its active metabolite cycloguanil. Unlike…”
Get full text
Journal Article -
5
In Vitro Metabolism of Phenoxypropoxybiguanide Analogues in Human Liver Microsomes to Potent Antimalarial Dihydrotriazines
Published in Journal of medicinal chemistry (21-04-2005)“…Phenoxypropoxybiguanides, such as 1 (PS-15), are prodrugs analogous to the relationship of proguanil and its active metabolite cycloguanil. Unlike cycloguanil,…”
Get full text
Journal Article -
6
Discovery of Highly Potent and Selective Small Molecule ADAMTS‑5 Inhibitors That Inhibit Human Cartilage Degradation via Encoded Library Technology (ELT)
Published in Journal of medicinal chemistry (23-08-2012)“…The metalloprotease ADAMTS-5 is considered a potential target for the treatment of osteoarthritis. To identify selective inhibitors of ADAMTS-5, we employed…”
Get full text
Journal Article -
7
Discovery of 4‑Amino-8-quinoline Carboxamides as Novel, Submicromolar Inhibitors of NAD-Hydrolyzing Enzyme CD38
Published in Journal of medicinal chemistry (10-09-2015)“…Starting from the micromolar 8-quinoline carboxamide high-throughput screening hit 1a, a systematic exploration of the structure–activity relationships (SAR)…”
Get full text
Journal Article -
8
Pharmacokinetics, Safety, and Hydrolysis of Oral Pyrroloquinazolinediamines Administered in Single and Multiple Doses in Rats
Published in Antimicrobial Agents and Chemotherapy (01-08-2007)“…Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley Reddit…”
Get full text
Journal Article -
9
Proteome-wide muscle protein fractional synthesis rates predict muscle mass gain in response to a selective androgen receptor modulator in rats
Published in American journal of physiology: endocrinology and metabolism (15-03-2016)“…Biomarkers of muscle protein synthesis rate could provide early data demonstrating anabolic efficacy for treating muscle-wasting conditions. Androgenic…”
Get more information
Journal Article -
10
Longitudinal changes in total body creatine pool size and skeletal muscle mass using the D3-creatine dilution method
Published in Journal of cachexia, sarcopenia and muscle (01-09-2013)“…Background We recently validated in cross-sectional studies a new method to determine total body creatine pool size and skeletal muscle mass based on D 3…”
Get full text
Journal Article -
11
Identification and Characterization of 4-Chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide (GSK3787), a Selective and Irreversible Peroxisome Proliferator-Activated Receptor δ (PPARδ) Antagonist
Published in Journal of medicinal chemistry (25-02-2010)“…4-Chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide 3 (GSK3787) was identified as a potent and selective ligand for PPARδ with good…”
Get full text
Journal Article -
12
Longitudinal changes in total body creatine pool size and skeletal muscle mass using the D 3 -creatine dilution method
Published in Journal of cachexia, sarcopenia and muscle (01-09-2013)“…We recently validated in cross-sectional studies a new method to determine total body creatine pool size and skeletal muscle mass based on D -creatine dilution…”
Get full text
Journal Article -
13
Adenosine A1 Receptor Modulation of MMP-2 Secretion by Trabecular Meshwork Cells
Published in Investigative ophthalmology & visual science (01-09-2002)“…Studies have shown that adenosine A(1) agonists can lower IOP in rabbits, mice, and monkeys, and this response is mediated in part by increases in outflow…”
Get full text
Journal Article -
14
Bradykinin enhancement of PGE2 signalling in bovine trabecular meshwork cells
Published in Experimental eye research (01-03-2003)“…Kinins and prostaglandins activate signalling pathways in cells of the trabecular meshwork and have opposing effects on outflow resistance to aqueous humor…”
Get full text
Journal Article -
15
The role of in vitro ADME assays in antimalarial drug discovery and development
Published in Combinatorial chemistry & high throughput screening (01-02-2005)“…The high level of attrition of drugs in clinical development has led pharmaceutical companies to increase the efficiency of their lead identification and…”
Get more information
Journal Article -
16
Longitudinal determination of total body creatine pool size and skeletal muscle mass in rats by D 3 ‐creatine dilution
Published in The FASEB journal (01-04-2013)“…Abstract only We recently described a new method to determine total body creatine pool size and skeletal muscle mass based on dilution of an oral dose of D 3…”
Get full text
Journal Article -
17
-
18
-
19
Bradykinin enhancement of PGE 2 signalling in bovine trabecular meshwork cells
Published in Experimental eye research (2003)“…Kinins and prostaglandins activate signalling pathways in cells of the trabecular meshwork and have opposing effects on outflow resistance to aqueous humor…”
Get full text
Journal Article -
20
Regulation of ingestive behaviors in the rat by GSK1521498, a novel micro-opioid receptor-selective inverse agonist
Published in The Journal of pharmacology and experimental therapeutics (01-10-2011)“…μ-Opioid receptor (MOR) agonism induces palatable food consumption principally through modulation of the rewarding properties of food…”
Get more information
Journal Article