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Items: 21

1.

The Clonal Invariant NKT Cell Repertoire in People with Type 1 Diabetes Is Characterized by a Loss of Clones Expressing High-Affinity TCRs.

Tocheva AS, Mansour S, Holt TG, Jones S, Chancellor A, Sanderson JP, Eren E, Elliott TJ, Holt RI, Gadola SD.

J Immunol. 2017 Feb 15;198(4):1452-1459. doi: 10.4049/jimmunol.1600255. Epub 2017 Jan 6.

2.

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
3.

Pharmacological activation and genetic manipulation of cystathionine beta-synthase alter circulating levels of homocysteine and hydrogen sulfide in mice.

Jensen KK, Geoghagen NS, Jin L, Holt TG, Luo Q, Malkowitz L, Ni W, Quan S, Waters MG, Zhang A, Zhou HH, Cheng K, Luo MJ.

Eur J Pharmacol. 2011 Jan 10;650(1):86-93. doi: 10.1016/j.ejphar.2010.09.080. Epub 2010 Oct 15.

PMID:
20955694
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.

Anthranilic acid replacements in a niacin receptor agonist.

Schmidt D, Smenton A, Raghavan S, Shen H, Ding FX, Carballo-Jane E, Luell S, Ciecko T, Holt TG, Wolff M, Taggart A, Wilsie L, Krsmanovic M, Ren N, Blom D, Cheng K, McCann PE, Waters MG, Tata J, Colletti S.

Bioorg Med Chem Lett. 2010 Jun 1;20(11):3426-30. doi: 10.1016/j.bmcl.2010.04.001. Epub 2010 Apr 8.

PMID:
20444602
7.

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
8.

Label-free high-throughput screening via mass spectrometry: a single cystathionine quantitative method for multiple applications.

Holt TG, Choi BK, Geoghagen NS, Jensen KK, Luo Q, LaMarr WA, Makara GM, Malkowitz L, Ozbal CC, Xiong Y, Dufresne C, Luo MJ.

Assay Drug Dev Technol. 2009 Oct;7(5):495-506. doi: 10.1089/adt.2009.0200.

PMID:
19715455
9.

Pyrazole acids as niacin receptor agonists for the treatment of dyslipidemia.

Schmidt D, Smenton A, Raghavan S, Carballo-Jane E, Lubell S, Ciecko T, Holt TG, Wolff M, Taggart A, Wilsie L, Krsmanovic M, Ren N, Blom D, Cheng K, McCann PE, Gerard Waters M, Tata J, Colletti S.

Bioorg Med Chem Lett. 2009 Aug 15;19(16):4768-72. doi: 10.1016/j.bmcl.2009.06.054. Epub 2009 Jun 17.

PMID:
19592242
10.

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
11.

2-Substituted piperazine-derived imidazole carboxamides as potent and selective CCK1R agonists for the treatment of obesity.

Berger R, Zhu C, Hansen AR, Harper B, Chen Z, Holt TG, Hubert J, Lee SJ, Pan J, Qian S, Reitman ML, Strack AM, Weingarth DT, Wolff M, Macneil DJ, Weber AE, Edmondson SD.

Bioorg Med Chem Lett. 2008 Sep 1;18(17):4833-7. doi: 10.1016/j.bmcl.2008.07.083. Epub 2008 Jul 24.

PMID:
18684621
12.

Discovery of imidazole carboxamides as potent and selective CCK1R agonists.

Zhu C, Hansen AR, Bateman T, Chen Z, Holt TG, Hubert JA, Karanam BV, Lee SJ, Pan J, Qian S, Reddy VB, Reitman ML, Strack AM, Tong V, Weingarth DT, Wolff MS, MacNeil DJ, Weber AE, Duffy JL, Edmondson SD.

Bioorg Med Chem Lett. 2008 Aug 1;18(15):4393-6. doi: 10.1016/j.bmcl.2008.06.057. Epub 2008 Jun 20.

PMID:
18614364
13.

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
14.

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
15.

A simple in vitro model to study the stability of acylglucuronides.

Chen Z, Holt TG, Pivnichny JV, Leung K.

J Pharmacol Toxicol Methods. 2007 Jan-Feb;55(1):91-5. Epub 2006 Apr 5.

PMID:
16713308
16.

Biomarker discovery in rat plasma for estrogen receptor-alpha action.

Holt TG, Flick RB, Rohde E, Griffin P, Rohrer SP.

Electrophoresis. 2005 Dec;26(23):4486-94.

PMID:
16315174
17.

The design and development of an integrated natural products screening database.

Holt TG, Dufresne C, Liesch JM, Mallow GK.

J Biomol Screen. 2000 Dec;5(6):421-33.

PMID:
11598460
18.

Global changes in gene expression related to antibiotic synthesis in Streptomyces hygroscopicus.

Holt TG, Chang C, Laurent-Winter C, Murakami T, Garrels JI, Davies JE, Thompson CJ.

Mol Microbiol. 1992 Apr;6(8):969-80.

PMID:
1584026
20.

Bioactive compounds from aquatic and terrestrial sources.

Rinehart KL, Holt TG, Fregeau NL, Keifer PA, Wilson GR, Perun TJ Jr, Sakai R, Thompson AG, Stroh JG, Shield LS, et al.

J Nat Prod. 1990 Jul-Aug;53(4):771-92. Review.

PMID:
2095373
21.

Thiostrepton-induced gene expression in Streptomyces lividans.

Murakami T, Holt TG, Thompson CJ.

J Bacteriol. 1989 Mar;171(3):1459-66.

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