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Items: 12

1.

Discovery of Tropifexor (LJN452), a Highly Potent Non-bile Acid FXR Agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH).

Tully DC, Rucker PV, Chianelli D, Williams J, Vidal A, Alper PB, Mutnick D, Bursulaya B, Schmeits J, Wu X, Bao D, Zoll J, Kim Y, Groessl T, McNamara P, Seidel HM, Molteni V, Liu B, Phimister A, Joseph SB, Laffitte B.

J Med Chem. 2017 Dec 28;60(24):9960-9973. doi: 10.1021/acs.jmedchem.7b00907. Epub 2017 Dec 8.

PMID:
29148806
2.

Proteasome inhibition for treatment of leishmaniasis, Chagas disease and sleeping sickness.

Khare S, Nagle AS, Biggart A, Lai YH, Liang F, Davis LC, Barnes SW, Mathison CJ, Myburgh E, Gao MY, Gillespie JR, Liu X, Tan JL, Stinson M, Rivera IC, Ballard J, Yeh V, Groessl T, Federe G, Koh HX, Venable JD, Bursulaya B, Shapiro M, Mishra PK, Spraggon G, Brock A, Mottram JC, Buckner FS, Rao SP, Wen BG, Walker JR, Tuntland T, Molteni V, Glynne RJ, Supek F.

Nature. 2016 Sep 8;537(7619):229-233. doi: 10.1038/nature19339. Epub 2016 Aug 8.

3.

Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants for the Treatment of EGFR Mutant Non-Small-Cell Lung Cancers.

Lelais G, Epple R, Marsilje TH, Long YO, McNeill M, Chen B, Lu W, Anumolu J, Badiger S, Bursulaya B, DiDonato M, Fong R, Juarez J, Li J, Manuia M, Mason DE, Gordon P, Groessl T, Johnson K, Jia Y, Kasibhatla S, Li C, Isbell J, Spraggon G, Bender S, Michellys PY.

J Med Chem. 2016 Jul 28;59(14):6671-89. doi: 10.1021/acs.jmedchem.5b01985. Epub 2016 Jul 19.

PMID:
27433829
4.

Use of solubilizers in preclinical formulations: Effect of Cremophor EL on the pharmacokinetic properties on early discovery compounds.

Liu B, Gordon WP, Richmond W, Groessl T, Tuntland T.

Eur J Pharm Sci. 2016 May 25;87:52-7. doi: 10.1016/j.ejps.2015.10.015. Epub 2015 Oct 20.

PMID:
26499309
5.

Antitrypanosomal Treatment with Benznidazole Is Superior to Posaconazole Regimens in Mouse Models of Chagas Disease.

Khare S, Liu X, Stinson M, Rivera I, Groessl T, Tuntland T, Yeh V, Wen B, Molteni V, Glynne R, Supek F.

Antimicrob Agents Chemother. 2015 Oct;59(10):6385-94. doi: 10.1128/AAC.00689-15. Epub 2015 Aug 3.

6.

Novel tricyclic pyrazolopyrimidines as potent and selective GPR119 agonists.

Azimioara M, Alper P, Cow C, Mutnick D, Nikulin V, Lelais G, Mecom J, McNeill M, Michellys PY, Wang Z, Reding E, Paliotti M, Li J, Bao D, Zoll J, Kim Y, Zimmerman M, Groessl T, Tuntland T, Joseph SB, McNamara P, Seidel HM, Epple R.

Bioorg Med Chem Lett. 2014 Dec 1;24(23):5478-83. doi: 10.1016/j.bmcl.2014.10.010. Epub 2014 Oct 13.

PMID:
25455488
7.

Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials.

Marsilje TH, Pei W, Chen B, Lu W, Uno T, Jin Y, Jiang T, Kim S, Li N, Warmuth M, Sarkisova Y, Sun F, Steffy A, Pferdekamper AC, Li AG, Joseph SB, Kim Y, Liu B, Tuntland T, Cui X, Gray NS, Steensma R, Wan Y, Jiang J, Chopiuk G, Li J, Gordon WP, Richmond W, Johnson K, Chang J, Groessl T, He YQ, Phimister A, Aycinena A, Lee CC, Bursulaya B, Karanewsky DS, Seidel HM, Harris JL, Michellys PY.

J Med Chem. 2013 Jul 25;56(14):5675-90. doi: 10.1021/jm400402q. Epub 2013 Jun 26.

PMID:
23742252
8.

A modern in vivo pharmacokinetic paradigm: combining snapshot, rapid and full PK approaches to optimize and expedite early drug discovery.

Li C, Liu B, Chang J, Groessl T, Zimmerman M, He YQ, Isbell J, Tuntland T.

Drug Discov Today. 2013 Jan;18(1-2):71-8. doi: 10.1016/j.drudis.2012.09.004. Epub 2012 Sep 13. Review.

PMID:
22982770
9.

Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery.

Meister S, Plouffe DM, Kuhen KL, Bonamy GM, Wu T, Barnes SW, Bopp SE, Borboa R, Bright AT, Che J, Cohen S, Dharia NV, Gagaring K, Gettayacamin M, Gordon P, Groessl T, Kato N, Lee MC, McNamara CW, Fidock DA, Nagle A, Nam TG, Richmond W, Roland J, Rottmann M, Zhou B, Froissard P, Glynne RJ, Mazier D, Sattabongkot J, Schultz PG, Tuntland T, Walker JR, Zhou Y, Chatterjee A, Diagana TT, Winzeler EA.

Science. 2011 Dec 9;334(6061):1372-7. doi: 10.1126/science.1211936. Epub 2011 Nov 17.

10.

A chemically induced vaccine strategy for prostate cancer.

Dubrovska A, Kim C, Elliott J, Shen W, Kuo TH, Koo DI, Li C, Tuntland T, Chang J, Groessl T, Wu X, Gorney V, Ramirez-Montagut T, Spiegel DA, Cho CY, Schultz PG.

ACS Chem Biol. 2011 Nov 18;6(11):1223-31. doi: 10.1021/cb200222s. Epub 2011 Sep 21.

PMID:
21936526
11.

First-in-class pan caspase inhibitor developed for the treatment of liver disease.

Linton SD, Aja T, Armstrong RA, Bai X, Chen LS, Chen N, Ching B, Contreras P, Diaz JL, Fisher CD, Fritz LC, Gladstone P, Groessl T, Gu X, Herrmann J, Hirakawa BP, Hoglen NC, Jahangiri KG, Kalish VJ, Karanewsky DS, Kodandapani L, Krebs J, McQuiston J, Meduna SP, Nalley K, Robinson ED, Sayers RO, Sebring K, Spada AP, Ternansky RJ, Tomaselli KJ, Ullman BR, Valentino KL, Weeks S, Winn D, Wu JC, Yeo P, Zhang CZ.

J Med Chem. 2005 Nov 3;48(22):6779-82.

PMID:
16250635
12.

Characterization of IDN-6556 (3-[2-(2-tert-butyl-phenylaminooxalyl)-amino]-propionylamino]-4-oxo-5-(2,3,5,6-tetrafluoro-phenoxy)-pentanoic acid): a liver-targeted caspase inhibitor.

Hoglen NC, Chen LS, Fisher CD, Hirakawa BP, Groessl T, Contreras PC.

J Pharmacol Exp Ther. 2004 May;309(2):634-40. Epub 2004 Jan 23.

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