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Page 1
Discovery of the TLR7/8 Antagonist MHV370 for Treatment of Systemic Autoimmune Diseases.
Alper P, Betschart C, André C, Boulay T, Cheng D, Deane J, Faller M, Feifel R, Glatthar R, Han D, Hemmig R, Jiang T, Knoepfel T, Maginnis J, Mutnick D, Pei W, Ruzzante G, Syka P, Zhang G, Zhang Y, Zink F, Zipfel G, Hawtin S, Junt T, Michellys PY. Alper P, et al. Among authors: hawtin s. ACS Med Chem Lett. 2023 Jul 31;14(8):1054-1062. doi: 10.1021/acsmedchemlett.3c00136. eCollection 2023 Aug 10. ACS Med Chem Lett. 2023. PMID: 37583811 Free PMC article.
Preclinical characterization of the Toll-like receptor 7/8 antagonist MHV370 for lupus therapy.
Hawtin S, André C, Collignon-Zipfel G, Appenzeller S, Bannert B, Baumgartner L, Beck D, Betschart C, Boulay T, Brunner HI, Ceci M, Deane J, Feifel R, Ferrero E, Kyburz D, Lafossas F, Loetscher P, Merz-Stoeckle C, Michellys P, Nuesslein-Hildesheim B, Raulf F, Rush JS, Ruzzante G, Stein T, Zaharevitz S, Wieczorek G, Siegel R, Gergely P, Shisha T, Junt T. Hawtin S, et al. Cell Rep Med. 2023 May 16;4(5):101036. doi: 10.1016/j.xcrm.2023.101036. Cell Rep Med. 2023. PMID: 37196635 Free PMC article.
First-in-Human Study of the Safety, Pharmacokinetics, and Pharmacodynamics of MHV370, a Dual Inhibitor of Toll-Like Receptors 7 and 8, in Healthy Adults.
Shisha T, Posch MG, Lehmann J, Feifel R, Junt T, Hawtin S, Schuemann J, Avrameas A, Danekula R, Misiolek P, Siegel R, Gergely P. Shisha T, et al. Among authors: hawtin s. Eur J Drug Metab Pharmacokinet. 2023 Sep;48(5):553-566. doi: 10.1007/s13318-023-00847-3. Epub 2023 Aug 2. Eur J Drug Metab Pharmacokinet. 2023. PMID: 37532923 Free PMC article. Clinical Trial.
A root cause analysis to identify the mechanistic drivers of immunogenicity against the anti-VEGF biotherapeutic brolucizumab.
Kearns JD, Wassmann P, Olgac U, Fichter M, Christen B, Rubic-Schneider T, Koepke S, Cochin de Billy B, Ledieu D, Andre C, Hawtin S, Fischer B, Moretti F, Hug C, Bepperling A, Brannetti B, Mendez-Garcia C, Littlewood-Evans A, Clemens A, Grosskreutz CL, Mehan P, Schmouder RL, Sasseville V, Brees D, Karle AC. Kearns JD, et al. Among authors: hawtin s. Sci Transl Med. 2023 Feb;15(681):eabq5068. doi: 10.1126/scitranslmed.abq5068. Epub 2023 Feb 1. Sci Transl Med. 2023. PMID: 36724241
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.
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.
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
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.
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
41 results