Thoma G - Search Results

1

Syk inhibitors with high potency in presence of blood.

Thoma G, Blanz J, Bühlmayer P, Drückes P, Kittelmann M, Smith AB, van Eis M, Vangrevelinghe E, Zerwes HG, Che JJ, He X, Jin Y, Lee CC, Michellys PY, Uno T, Liu H. Thoma G, et al. Bioorg Med Chem Lett. 2014 May 15;24(10):2278-82. doi: 10.1016/j.bmcl.2014.03.075. Epub 2014 Apr 3. Bioorg Med Chem Lett. 2014. PMID: 24726806

2

Reduced cardiac side-effect potential by introduction of polar groups: discovery of NIBR-1282, an orally bioavailable CCR5 antagonist which is active in vivo.

Thoma G, Beerli C, Bigaud M, Bruns C, Cooke NG, Streiff MB, Zerwes HG. Thoma G, et al. Bioorg Med Chem Lett. 2008 Mar 15;18(6):2000-5. doi: 10.1016/j.bmcl.2008.01.108. Epub 2008 Feb 2. Bioorg Med Chem Lett. 2008. PMID: 18267361

3

Orally bioavailable isothioureas block function of the chemokine receptor CXCR4 in vitro and in vivo.

Thoma G, Streiff MB, Kovarik J, Glickman F, Wagner T, Beerli C, Zerwes HG. Thoma G, et al. J Med Chem. 2008 Dec 25;51(24):7915-20. doi: 10.1021/jm801065q. J Med Chem. 2008. PMID: 19053768

4

Special ergolines are highly selective, potent antagonists of the chemokine receptor CXCR3: discovery, characterization and preliminary SAR of a promising lead.

Thoma G, Baenteli R, Lewis I, Wagner T, Oberer L, Blum W, Glickman F, Streiff MB, Zerwes HG. Thoma G, et al. Bioorg Med Chem Lett. 2009 Nov 1;19(21):6185-8. doi: 10.1016/j.bmcl.2009.09.002. Epub 2009 Sep 6. Bioorg Med Chem Lett. 2009. PMID: 19783143

5

Identification of a potent Janus kinase 3 inhibitor with high selectivity within the Janus kinase family.

Thoma G, Nuninger F, Falchetto R, Hermes E, Tavares GA, Vangrevelinghe E, Zerwes HG. Thoma G, et al. J Med Chem. 2011 Jan 13;54(1):284-8. doi: 10.1021/jm101157q. Epub 2010 Dec 14. J Med Chem. 2011. PMID: 21155605

6

Jak1 has a dominant role over Jak3 in signal transduction through γc-containing cytokine receptors.

Haan C, Rolvering C, Raulf F, Kapp M, Drückes P, Thoma G, Behrmann I, Zerwes HG. Haan C, et al. Among authors: thoma g. Chem Biol. 2011 Mar 25;18(3):314-23. doi: 10.1016/j.chembiol.2011.01.012. Chem Biol. 2011. PMID: 21439476

7

Special ergolines efficiently inhibit the chemokine receptor CXCR3 in blood.

Thoma G, Baenteli R, Lewis I, Jones D, Kovarik J, Streiff MB, Zerwes HG. Thoma G, et al. Bioorg Med Chem Lett. 2011 Aug 15;21(16):4745-9. doi: 10.1016/j.bmcl.2011.06.070. Epub 2011 Jun 29. Bioorg Med Chem Lett. 2011. PMID: 21764306

8

Selective inhibitors of the Janus kinase Jak3--Are they effective?

Thoma G, Drückes P, Zerwes HG. Thoma G, et al. Bioorg Med Chem Lett. 2014 Oct 1;24(19):4617-4621. doi: 10.1016/j.bmcl.2014.08.046. Epub 2014 Aug 28. Bioorg Med Chem Lett. 2014. PMID: 25217444 Review.

9

Discovery and profiling of a selective and efficacious Syk inhibitor.

Thoma G, Smith AB, van Eis MJ, Vangrevelinghe E, Blanz J, Aichholz R, Littlewood-Evans A, Lee CC, Liu H, Zerwes HG. Thoma G, et al. J Med Chem. 2015 Feb 26;58(4):1950-63. doi: 10.1021/jm5018863. Epub 2015 Feb 9. J Med Chem. 2015. PMID: 25633741

10

Orally bioavailable Syk inhibitors with activity in a rat PK/PD model.

Thoma G, Veenstra S, Strang R, Blanz J, Vangrevelinghe E, Berghausen J, Lee CC, Zerwes HG. Thoma G, et al. Bioorg Med Chem Lett. 2015 Oct 15;25(20):4642-7. doi: 10.1016/j.bmcl.2015.08.037. Epub 2015 Aug 18. Bioorg Med Chem Lett. 2015. PMID: 26320624

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