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Items: 4

1.

Evaluation of JAK3 Biology in Autoimmune Disease Using a Highly Selective, Irreversible JAK3 Inhibitor.

Elwood F, Witter DJ, Piesvaux J, Kraybill B, Bays N, Alpert C, Goldenblatt P, Qu Y, Ivanovska I, Lee HH, Chiu CS, Tang H, Scott ME, Deshmukh SV, Zielstorff M, Byford A, Chakravarthy K, Dorosh L, Rivkin A, Klappenbach J, Pan BS, Kariv I, Dinsmore C, Slipetz D, Dandliker PJ.

J Pharmacol Exp Ther. 2017 May;361(2):229-244. doi: 10.1124/jpet.116.239723. Epub 2017 Feb 13.

2.

Identification of an allosteric binding site for RORγt inhibition.

Scheepstra M, Leysen S, van Almen GC, Miller JR, Piesvaux J, Kutilek V, van Eenennaam H, Zhang H, Barr K, Nagpal S, Soisson SM, Kornienko M, Wiley K, Elsen N, Sharma S, Correll CC, Trotter BW, van der Stelt M, Oubrie A, Ottmann C, Parthasarathy G, Brunsveld L.

Nat Commun. 2015 Dec 7;6:8833. doi: 10.1038/ncomms9833.

3.

Macrocyclic BACE inhibitors: Optimization of a micromolar hit to nanomolar leads.

Huang Y, Strobel ED, Ho CY, Reynolds CH, Conway KA, Piesvaux JA, Brenneman DE, Yohrling GJ, Moore Arnold H, Rosenthal D, Alexander RS, Tounge BA, Mercken M, Vandermeeren M, Parker MH, Reitz AB, Baxter EW.

Bioorg Med Chem Lett. 2010 May 15;20(10):3158-60. doi: 10.1016/j.bmcl.2010.03.097. Epub 2010 Mar 30.

PMID:
20399652
4.

Virus-based expression systems facilitate rapid target in vivo functionality validation and high-throughput screening.

Darrow AL, Conway KA, Vaidya AH, Rosenthal D, Wildey MJ, Minor L, Itkin Z, Kong Y, Piesvaux J, Qi J, Mercken M, Andrade-Gordon P, Plata-Salamán C, Ilyin SE.

J Biomol Screen. 2003 Feb;8(1):65-71.

PMID:
12854999

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