M
Markus Schirle
Researcher at Novartis
Publications - 91
Citations - 16037
Markus Schirle is an academic researcher from Novartis. The author has contributed to research in topics: Ubiquitin ligase & Protein degradation. The author has an hindex of 38, co-authored 80 publications receiving 14202 citations. Previous affiliations of Markus Schirle include University of Tübingen & University of California, Berkeley.
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Journal ArticleDOI
Examining the influence of specificity ligands and ATP-competitive ligands on the overall effectiveness of bivalent kinase inhibitors
Margaret L. Wong,Jason Murphy,Edmund Harrington,Carrie M. Gower,Rishi K. Jain,Markus Schirle,Jason R. Thomas +6 more
TL;DR: This work provides the first insight into the influence of ATP-competitive and specificity ligands binding to their intended target on a proteome-wide scale and suggests that as the potency of the ATP- competitive ligand increases, the contribution of the specificity ligand towards the overall binding affinity of the bivalent inhibitor decreases.
Journal ArticleDOI
Targeted Protein Degradation through E2 Recruitment
Nafsika Forte,Dustin Dovala,Matthew J. Hesse,Jeffrey Mckenna,John A. Tallarico,Markus Schirle,Daniel K. Nomura +6 more
TL;DR: In this paper , a covalent chemoproteomic approach was used to discover a recruiter against the E2 ubiquitin conjugating enzyme UBE2D that targets an allosteric cysteine, C111, without affecting the enzymatic activity of the protein.
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An Activity-Based Oxaziridine Platform for Identifying and Developing Covalent Ligands for Functional Allosteric Methionine Sites: Redox-Dependent Inhibition of Cyclin-Dependent Kinase 4.
Angel Gonzalez-Valero,Audrey G. Reeves,Annika C. S. Page,Patrick J. Moon,Edward B. Miller,Katia Coulonval,Steven W. M. Crossley,Xiao Xie,Dan He,P. Musacchio,Alec H. Christian,Jeffrey Mckenna,Richard A. Lewis,Eric Fang,Dustin Dovala,Yipin Lu,Lynn M. McGregor,Markus Schirle,John A. Tallarico,Pierre P. Roger,F. Dean Toste,Christopher J. Chang +21 more
TL;DR: In this paper , a methionine-directed activity-based protein profiling (ABPP) platform using Redox-Activated Chemical Tagging (ReACT) leverages a biomimetic oxidative ligation strategy for selective methionines modification.
Journal ArticleDOI
Characterizing Drug-Target Interactions: Shifting towards the Clinic.
TL;DR: This study demonstrates for the first time that TPP enables organ-specific drug target engagement and identification studies during the later stages of drug discovery and even in a clinical setting.
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Identification of Tumor-Associated HLA-Ligands in the Post-Genomic Era
TL;DR: This review tries to give an overview over available conventional strategies as well as current developments that utilize the potent large-scale screening tools of the post-genomic era.