M
Michael Forster
Researcher at University of Tübingen
Publications - 16
Citations - 325
Michael Forster is an academic researcher from University of Tübingen. The author has contributed to research in topics: Janus kinase & Kinome. The author has an hindex of 8, co-authored 16 publications receiving 208 citations. Previous affiliations of Michael Forster include German Cancer Research Center.
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Journal ArticleDOI
Selective JAK3 Inhibitors with a Covalent Reversible Binding Mode Targeting a New Induced Fit Binding Pocket
Michael Forster,Apirat Chaikuad,Silke M. Bauer,Julia Holstein,Matthew B. Robers,Cesear Corona,Matthias Gehringer,Ellen Pfaffenrot,Kamran Ghoreschi,Stefan Knapp,Stefan Laufer +10 more
TL;DR: It is confirmed that in vitro activity and selectivity translate well into the cellular environment and suggest that the inhibitors presented are powerful tools to elucidate JAK3-specific functions.
Journal ArticleDOI
Development, Optimization, and Structure-Activity Relationships of Covalent-Reversible JAK3 Inhibitors Based on a Tricyclic Imidazo[5,4- d]pyrrolo[2,3- b]pyridine Scaffold.
Michael Forster,Apirat Chaikuad,Apirat Chaikuad,Teodor Dimitrov,Eva Döring,Julia Holstein,Benedict-Tilman Berger,Benedict-Tilman Berger,Matthias Gehringer,Kamran Ghoreschi,Susanne Müller,Stefan Knapp,Stefan Knapp,Stefan Laufer +13 more
TL;DR: Detailed structure-activity relationships necessary for induction of the arginine pocket and the impact of this structural change on potency, isoform selectivity, and efficacy in cellular models are described.
Journal ArticleDOI
An updated patent review of p38 MAP kinase inhibitors (2014-2019)
TL;DR: P38 MAP kinase inhibitors are a mature field with many pre-clinically validated structural classes, more than 20 candidates in clinical trials but still (except the weak and unselective p38 inhibitor pirfenidone) no approved drug.
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Novel Hinge-Binding Motifs for Janus Kinase 3 Inhibitors: A Comprehensive Structure–Activity Relationship Study on Tofacitinib Bioisosteres
TL;DR: A library of tofacitinib bioisosteres was prepared and tested against JAK3, and most of the compounds proved to be poorly active, but strategies for restoring activity were discovered and crucial structure–activity relationships were deduced.
Journal ArticleDOI
Recent advances in JAK3 inhibition: Isoform selectivity by covalent cysteine targeting
TL;DR: A set of JAK3 inhibitors with excellent selectivity against other JAK isoforms and the kinome was developed during the last three years and used to decipher Jak3-dependent signaling and demonstrates that selective JAK2 inhibition is sufficient to block downstream signaling.