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Page 1
Target-Based Identification and Optimization of 5-Indazol-5-yl Pyridones as Toll-like Receptor 7 and 8 Antagonists Using a Biochemical TLR8 Antagonist Competition Assay.
Knoepfel T, Nimsgern P, Jacquier S, Bourrel M, Vangrevelinghe E, Glatthar R, Behnke D, Alper PB, Michellys PY, Deane J, Junt T, Zipfel G, Limonta S, Hawtin S, Andre C, Boulay T, Loetscher P, Faller M, Blank J, Feifel R, Betschart C. Knoepfel T, et al. Among authors: hawtin s. J Med Chem. 2020 Aug 13;63(15):8276-8295. doi: 10.1021/acs.jmedchem.0c00130. Epub 2020 Jul 30. J Med Chem. 2020. PMID: 32786235
Discovery of potent, orally bioavailable in vivo efficacious antagonists of the TLR7/8 pathway.
Alper PB, Deane J, Betschart C, Buffet D, Collignon Zipfel G, Gordon P, Hampton J, Hawtin S, Ibanez M, Jiang T, Junt T, Knoepfel T, Liu B, Maginnis J, McKeever U, Michellys PY, Mutnick D, Nayak B, Niwa S, Richmond W, Rush JS, Syka P, Zhang Y, Zhu X. Alper PB, et al. Among authors: hawtin s. Bioorg Med Chem Lett. 2020 Sep 1;30(17):127366. doi: 10.1016/j.bmcl.2020.127366. Epub 2020 Jun 24. Bioorg Med Chem Lett. 2020. PMID: 32738975
Structure-Based Optimization of a Fragment-like TLR8 Binding Screening Hit to an In Vivo Efficacious TLR7/8 Antagonist.
Betschart C, Faller M, Zink F, Hemmig R, Blank J, Vangrevelinghe E, Bourrel M, Glatthar R, Behnke D, Barker K, Heizmann A, Angst D, Nimsgern P, Jacquier S, Junt T, Zipfel G, Ruzzante G, Loetscher P, Limonta S, Hawtin S, Andre CB, Boulay T, Feifel R, Knoepfel T. Betschart C, et al. Among authors: hawtin s. ACS Med Chem Lett. 2022 Mar 10;13(4):658-664. doi: 10.1021/acsmedchemlett.1c00696. eCollection 2022 Apr 14. ACS Med Chem Lett. 2022. PMID: 35450354 Free PMC article.
Modulating ADME Properties by Fluorination: MK2 Inhibitors with Improved Oral Exposure.
Velcicky J, Schlapbach A, Heng R, Revesz L, Pflieger D, Blum E, Hawtin S, Huppertz C, Feifel R, Hersperger R. Velcicky J, et al. Among authors: hawtin s. ACS Med Chem Lett. 2018 Mar 20;9(4):392-396. doi: 10.1021/acsmedchemlett.8b00098. eCollection 2018 Apr 12. ACS Med Chem Lett. 2018. PMID: 29670707 Free PMC article.
Novel 3-aminopyrazole inhibitors of MK-2 discovered by scaffold hopping strategy.
Velcicky J, Feifel R, Hawtin S, Heng R, Huppertz C, Koch G, Kroemer M, Moebitz H, Revesz L, Scheufler C, Schlapbach A. Velcicky J, et al. Among authors: hawtin s. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1293-7. doi: 10.1016/j.bmcl.2009.10.138. Epub 2009 Nov 3. Bioorg Med Chem Lett. 2010. PMID: 20060294
In vivo and in vitro SAR of tetracyclic MAPKAP-K2 (MK2) inhibitors. Part I.
Revesz L, Schlapbach A, Aichholz R, Feifel R, Hawtin S, Heng R, Hiestand P, Jahnke W, Koch G, Kroemer M, Möbitz H, Scheufler C, Velcicky J, Huppertz C. Revesz L, et al. Among authors: hawtin s. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4715-8. doi: 10.1016/j.bmcl.2010.04.024. Epub 2010 Apr 13. Bioorg Med Chem Lett. 2010. PMID: 20594847
Nonhematopoietic IRAK1 drives arthritis via neutrophil chemoattractants.
Hoyler T, Bannert B, André C, Beck D, Boulay T, Buffet D, Caesar N, Calzascia T, Dawson J, Kyburz D, Hennze R, Huppertz C, Littlewood-Evans A, Loetscher P, Mertz KD, Niwa S, Robert G, Rush JS, Ruzzante G, Sarret S, Stein T, Touil I, Wieczorek G, Zipfel G, Hawtin S, Junt T. Hoyler T, et al. Among authors: hawtin s. JCI Insight. 2022 Jul 8;7(13):e149825. doi: 10.1172/jci.insight.149825. JCI Insight. 2022. PMID: 35801586 Free PMC article.
Pyrrolo-pyrimidones: a novel class of MK2 inhibitors with potent cellular activity.
Schlapbach A, Feifel R, Hawtin S, Heng R, Koch G, Moebitz H, Revesz L, Scheufler C, Velcicky J, Waelchli R, Huppertz C. Schlapbach A, et al. Among authors: hawtin s. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6142-6. doi: 10.1016/j.bmcl.2008.10.039. Epub 2008 Oct 11. Bioorg Med Chem Lett. 2008. PMID: 18945615
In vivo and in vitro SAR of tetracyclic MAPKAP-K2 (MK2) inhibitors. Part II.
Revesz L, Schlapbach A, Aichholz R, Dawson J, Feifel R, Hawtin S, Littlewood-Evans A, Koch G, Kroemer M, Möbitz H, Scheufler C, Velcicky J, Huppertz C. Revesz L, et al. Among authors: hawtin s. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4719-23. doi: 10.1016/j.bmcl.2010.04.023. Epub 2010 Apr 11. Bioorg Med Chem Lett. 2010. PMID: 20591669
41 results