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Items: 29

1.

Niacin lipid efficacy is independent of both the niacin receptor GPR109A and free fatty acid suppression.

Lauring B, Taggart AK, Tata JR, Dunbar R, Caro L, Cheng K, Chin J, Colletti SL, Cote J, Khalilieh S, Liu J, Luo WL, Maclean AA, Peterson LB, Polis AB, Sirah W, Wu TJ, Liu X, Jin L, Wu K, Boatman PD, Semple G, Behan DP, Connolly DT, Lai E, Wagner JA, Wright SD, Cuffie C, Mitchel YB, Rader DJ, Paolini JF, Waters MG, Plump A.

Sci Transl Med. 2012 Aug 22;4(148):148ra115. doi: 10.1126/scitranslmed.3003877.

2.

(1aR,5aR)1a,3,5,5a-Tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid (MK-1903): a potent GPR109a agonist that lowers free fatty acids in humans.

Boatman PD, Lauring B, Schrader TO, Kasem M, Johnson BR, Skinner P, Jung JK, Xu J, Cherrier MC, Webb PJ, Semple G, Sage CR, Knudsen J, Chen R, Luo WL, Caro L, Cote J, Lai E, Wagner J, Taggart AK, Carballo-Jane E, Hammond M, Colletti SL, Tata JR, Connolly DT, Waters MG, Richman JG.

J Med Chem. 2012 Apr 26;55(8):3644-66. doi: 10.1021/jm2010964. Epub 2012 Apr 9.

PMID:
22435740
3.

The discovery of high affinity agonists of GPR109a with reduced serum shift and improved ADME properties.

Imbriglio JE, DiRocco D, Bodner R, Raghavan S, Chen W, Marley D, Esser C, Holt TG, Wolff MS, Taggart AK, Waters MG, Tata JR, Colletti SL.

Bioorg Med Chem Lett. 2011 May 1;21(9):2721-4. doi: 10.1016/j.bmcl.2010.11.116. Epub 2010 Dec 4.

PMID:
21185185
4.

GPR109a agonists. Part 2: pyrazole-acids as agonists of the human orphan G-protein coupled receptor GPR109a.

Imbriglio JE, Chang S, Liang R, Raghavan S, Schmidt D, Smenton A, Tria S, Schrader TO, Jung JK, Esser C, Holt TG, Wolff MS, Taggart AK, Cheng K, Carballo-Jane E, Waters MG, Tata JR, Colletti SL.

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4472-4. doi: 10.1016/j.bmcl.2010.06.041. Epub 2010 Jun 10.

PMID:
20615702
5.

Discovery of pyrazolyl propionyl cyclohexenamide derivatives as full agonists for the high affinity niacin receptor GPR109A.

Ding FX, Shen HC, Wilsie LC, Krsmanovic ML, Taggart AK, Ren N, Cai TQ, Wang J, Tong X, Holt TG, Chen Q, Waters MG, Hammond ML, Tata JR, Colletti SL.

Bioorg Med Chem Lett. 2010 Jun 1;20(11):3372-5. doi: 10.1016/j.bmcl.2010.04.013. Epub 2010 Apr 11.

PMID:
20452209
6.

Cholesterol efflux potential and antiinflammatory properties of high-density lipoprotein after treatment with niacin or anacetrapib.

Yvan-Charvet L, Kling J, Pagler T, Li H, Hubbard B, Fisher T, Sparrow CP, Taggart AK, Tall AR.

Arterioscler Thromb Vasc Biol. 2010 Jul;30(7):1430-8. doi: 10.1161/ATVBAHA.110.207142. Epub 2010 May 6.

7.

Potent tricyclic pyrazole tetrazole agonists of the nicotinic acid receptor (GPR109a).

Boatman PD, Schrader TO, Kasem M, Johnson BR, Skinner PJ, Jung JK, Xu J, Cherrier MC, Webb PJ, Semple G, Sage CR, Knudsen J, Chen R, Taggart AK, Carballo-Jane E, Richman JG.

Bioorg Med Chem Lett. 2010 May 1;20(9):2797-800. doi: 10.1016/j.bmcl.2010.03.062. Epub 2010 Mar 20.

PMID:
20363624
8.

Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate.

Shen HC, Ding FX, Raghavan S, Deng Q, Luell S, Forrest MJ, Carballo-Jane E, Wilsie LC, Krsmanovic ML, Taggart AK, Wu KK, Wu TJ, Cheng K, Ren N, Cai TQ, Chen Q, Wang J, Wolff MS, Tong X, Holt TG, Waters MG, Hammond ML, Tata JR, Colletti SL.

J Med Chem. 2010 Mar 25;53(6):2666-70. doi: 10.1021/jm100022r.

PMID:
20184326
9.

Discovery of novel tricyclic full agonists for the G-protein-coupled niacin receptor 109A with minimized flushing in rats.

Shen HC, Ding FX, Deng Q, Wilsie LC, Krsmanovic ML, Taggart AK, Carballo-Jane E, Ren N, Cai TQ, Wu TJ, Wu KK, Cheng K, Chen Q, Wolff MS, Tong X, Holt TG, Waters MG, Hammond ML, Tata JR, Colletti SL.

J Med Chem. 2009 Apr 23;52(8):2587-602. doi: 10.1021/jm900151e.

PMID:
19309152
10.

GPR109a agonists. Part 1: 5-Alkyl and 5-aryl-pyrazole-tetrazoles as agonists of the human orphan G-protein coupled receptor GPR109a.

Imbriglio JE, Chang S, Liang R, Raghavan S, Schmidt D, Smenton A, Tria S, Schrader TO, Jung JK, Esser C, Taggart AK, Cheng K, Carballo-Jane E, Gerard Waters M, Tata JR, Colletti SL.

Bioorg Med Chem Lett. 2009 Apr 15;19(8):2121-4. doi: 10.1016/j.bmcl.2009.03.014. Epub 2009 Mar 9.

PMID:
19307116
11.

Phenolic acids suppress adipocyte lipolysis via activation of the nicotinic acid receptor GPR109A (HM74a/PUMA-G).

Ren N, Kaplan R, Hernandez M, Cheng K, Jin L, Taggart AK, Zhu AY, Gan X, Wright SD, Cai TQ.

J Lipid Res. 2009 May;50(5):908-14. doi: 10.1194/jlr.M800625-JLR200. Epub 2009 Jan 9.

12.

Role of GPR81 in lactate-mediated reduction of adipose lipolysis.

Cai TQ, Ren N, Jin L, Cheng K, Kash S, Chen R, Wright SD, Taggart AK, Waters MG.

Biochem Biophys Res Commun. 2008 Dec 19;377(3):987-91. doi: 10.1016/j.bbrc.2008.10.088. Epub 2008 Oct 24.

PMID:
18952058
13.

Molecular modeling aided design of nicotinic acid receptor GPR109A agonists.

Deng Q, Frie JL, Marley DM, Beresis RT, Ren N, Cai TQ, Taggart AK, Cheng K, Carballo-Jane E, Wang J, Tong X, Waters MG, Tata JR, Colletti SL.

Bioorg Med Chem Lett. 2008 Sep 15;18(18):4963-7. doi: 10.1016/j.bmcl.2008.08.030. Epub 2008 Aug 14.

PMID:
18760600
14.

Discovery of pyrazolopyrimidines as the first class of allosteric agonists for the high affinity nicotinic acid receptor GPR109A.

Shen HC, Taggart AK, Wilsie LC, Waters MG, Hammond ML, Tata JR, Colletti SL.

Bioorg Med Chem Lett. 2008 Sep 15;18(18):4948-51. doi: 10.1016/j.bmcl.2008.08.039. Epub 2008 Aug 14.

PMID:
18752940
15.

3-(1H-tetrazol-5-yl)-1,4,5,6-tetrahydro-cyclopentapyrazole (MK-0354): a partial agonist of the nicotinic acid receptor, G-protein coupled receptor 109a, with antilipolytic but no vasodilatory activity in mice.

Semple G, Skinner PJ, Gharbaoui T, Shin YJ, Jung JK, Cherrier MC, Webb PJ, Tamura SY, Boatman PD, Sage CR, Schrader TO, Chen R, Colletti SL, Tata JR, Waters MG, Cheng K, Taggart AK, Cai TQ, Carballo-Jane E, Behan DP, Connolly DT, Richman JG.

J Med Chem. 2008 Aug 28;51(16):5101-8. doi: 10.1021/jm800258p. Epub 2008 Jul 30.

PMID:
18665582
16.

Tetrahydro anthranilic acid as a surrogate for anthranilic acid: application to the discovery of potent niacin receptor agonists.

Raghavan S, Tria GS, Shen HC, Ding FX, Taggart AK, Ren N, Wilsie LC, Krsmanovic ML, Holt TG, Wolff MS, Waters MG, Hammond ML, Tata JR, Colletti SL.

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3163-7. doi: 10.1016/j.bmcl.2008.04.071. Epub 2008 May 1.

PMID:
18477506
17.

Discovery of orally bioavailable and novel urea agonists of the high affinity niacin receptor GPR109A.

Shen HC, Szymonifka MJ, Kharbanda D, Deng Q, Carballo-Jane E, Wu KK, Wu TJ, Cheng K, Ren N, Cai TQ, Taggart AK, Wang J, Tong X, Waters MG, Hammond ML, Tata JR, Colletti SL.

Bioorg Med Chem Lett. 2007 Dec 15;17(24):6723-8. Epub 2007 Oct 18.

PMID:
18029181
18.

Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptor.

Shen HC, Ding FX, Luell S, Forrest MJ, Carballo-Jane E, Wu KK, Wu TJ, Cheng K, Wilsie LC, Krsmanovic ML, Taggart AK, Ren N, Cai TQ, Deng Q, Chen Q, Wang J, Wolff MS, Tong X, Holt TG, Waters MG, Hammond ML, Tata JR, Colletti SL.

J Med Chem. 2007 Dec 13;50(25):6303-6. Epub 2007 Nov 10.

PMID:
17994679
19.

Comparison of rat and dog models of vasodilatation and lipolysis for the calculation of a therapeutic index for GPR109A agonists.

Carballo-Jane E, Gerckens LS, Luell S, Parlapiano AS, Wolff M, Colletti SL, Tata JR, Taggart AK, Waters MG, Richman JG, McCann ME, Forrest MJ.

J Pharmacol Toxicol Methods. 2007 Nov-Dec;56(3):308-16. Epub 2007 Jun 23.

PMID:
17643322
20.

(D)-beta-Hydroxybutyrate inhibits adipocyte lipolysis via the nicotinic acid receptor PUMA-G.

Taggart AK, Kero J, Gan X, Cai TQ, Cheng K, Ippolito M, Ren N, Kaplan R, Wu K, Wu TJ, Jin L, Liaw C, Chen R, Richman J, Connolly D, Offermanns S, Wright SD, Waters MG.

J Biol Chem. 2005 Jul 22;280(29):26649-52. Epub 2005 Jun 1.

21.

Cell cycle-dependent regulation of yeast telomerase by Ku.

Fisher TS, Taggart AK, Zakian VA.

Nat Struct Mol Biol. 2004 Dec;11(12):1198-205. Epub 2004 Nov 7.

PMID:
15531893
22.

Telomerase: what are the Est proteins doing?

Taggart AK, Zakian VA.

Curr Opin Cell Biol. 2003 Jun;15(3):275-80. Review.

PMID:
12787768
23.

Est1p as a cell cycle-regulated activator of telomere-bound telomerase.

Taggart AK, Teng SC, Zakian VA.

Science. 2002 Aug 9;297(5583):1023-6.

24.
25.

TFIIA regulates TBP and TFIID dimers.

Coleman RA, Taggart AK, Burma S, Chicca JJ 2nd, Pugh BF.

Mol Cell. 1999 Sep;4(3):451-7.

26.

Dimerization of TFIID when not bound to DNA.

Taggart AK, Pugh BF.

Science. 1996 May 31;272(5266):1331-3.

PMID:
8650542
27.

Dimerization of the TATA binding protein.

Coleman RA, Taggart AK, Benjamin LR, Pugh BF.

J Biol Chem. 1995 Jun 9;270(23):13842-9.

28.
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