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Alan D Adams

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Articles 9
Citations 211
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Recent Articles
1.
Szewczyk J, Acton J, Adams A, Chicchi G, Freeman S, Howard A, et al.
Bioorg Med Chem Lett . 2011 Jan; 21(9):2665-9. PMID: 21273063
Screening of the Merck sample collection identified compound 1 as a weakly potent GPR119 agonist (hEC(50)=3600 nM). Dual termini optimization of 1 led to compound 36 having improved potency, selectivity,...
2.
Soisson S, Parthasarathy G, Adams A, Sahoo S, Sitlani A, Sparrow C, et al.
Proc Natl Acad Sci U S A . 2008 Apr; 105(14):5337-42. PMID: 18391212
The farnesoid X receptor (FXR), a member of the nuclear hormone receptor family, plays important roles in the regulation of bile acid and cholesterol homeostasis, glucose metabolism, and insulin sensitivity....
3.
Szewczyk J, Huang S, Chin J, Tian J, Mitnaul L, Rosa R, et al.
Bioorg Med Chem Lett . 2006 Mar; 16(11):3055-60. PMID: 16529931
Counterscreening compounds from a Merck PPAR program discovered lead 1, as a nanomolar LXR/PPAR dual agonist. SAR optimization developed a series of heterocyclic LXR agonists having excellent selectivity over all...
4.
Lund E, Peterson L, Adams A, Lam M, Burton C, Chin J, et al.
Biochem Pharmacol . 2005 Dec; 71(4):453-63. PMID: 16325781
Liver X receptor (LXR) alpha and LXRbeta are closely related nuclear receptors that respond to elevated levels of intracellular cholesterol by enhancing transcription of genes that control cholesterol efflux and...
5.
Chin J, Adams A, Bouffard A, Green A, Lacson R, Smith T, et al.
Assay Drug Dev Technol . 2004 Apr; 1(6):777-87. PMID: 15090224
Activation of liver X receptors (LXRs) induces reverse cholesterol transport and increases high-density lipoprotein cholesterol in vivo. Here, we describe novel, functional, homogeneous cell-based fluorescence resonance energy transfer assays for...
6.
Adams A, Hu Z, Von Langen D, Dadiz A, Elbrecht A, MacNaul K, et al.
Bioorg Med Chem Lett . 2003 Sep; 13(19):3185-90. PMID: 12951090
A new class of O-arylmandelic acid PPAR agonists show excellent anti-hyperglycemic efficacy in a db/db mouse model of DM2. These PPARalpha-weighted agonists do not show the typical PPARgamma associated side...
7.
Adams A, Yuen W, Hu Z, Santini C, Jones A, MacNaul K, et al.
Bioorg Med Chem Lett . 2003 Mar; 13(5):931-5. PMID: 12617924
A series of amphipathic 3-phenylbenzisoxazoles were found to be potent agonists of human PPARalpha, gamma and delta. The optimization of acid proximal structure for in vitro and in vivo potency...
8.
Berger J, Petro A, MacNaul K, Kelly L, Zhang B, Richards K, et al.
Mol Endocrinol . 2003 Jan; 17(4):662-76. PMID: 12554792
Antidiabetic thiazolidinediones (TZDs) and non-TZD compounds have been shown to serve as agonists of the peroxisome proliferator-activated receptor gamma (PPARgamma). Here, we report the identification and characterization of a novel...
9.
Sparrow C, Baffic J, Lam M, Lund E, Adams A, Fu X, et al.
J Biol Chem . 2002 Jan; 277(12):10021-7. PMID: 11790770
The LXR nuclear receptors are intracellular sensors of cholesterol excess and are activated by various oxysterols. LXRs have been shown to regulate multiple genes of lipid metabolism, including ABCA1 (formerly...