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Controlling Intramolecular Interactions in the Design of Selective, High-Affinity, Ligands for the CREBBP Bromodomain

Michael Brand, James Clayton, Mustafa Moroglu, Matthias Schiedel, Sarah Picaud, Joseph Bluck, Anna Skwarska, Anthony Chan, Corentine Laurin, Amy Scorah, Larissa See, Timothy Rooney, Oleg Fedorov, Gabriella Perell, Prakriti Kalra, Wilian Cortopassi, Kirsten Christensen, Richard Cooper, Robert Paton, William Pomerantz, Philip Biggin, Ester M. Hammond, Panagis Filippakopoulos, Stuart Conway

Version 1 posted 06 April 2020

601

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3

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Biological and Medicinal Chemistry

Working Paper

HaloTag-Targeted Sirtuin Rearranging Ligand (SirReal) for the Development of Proteolysis Targeting Chimeras (PROTACs) Against the Lysine Deacetylase Sirtuin 2 (Sirt2)

Matthias Schiedel, Attila Lehotzky, Sándor Szunyogh, Judit Oláh, Sören Hammelmann, Nathalie Wössner, Dina Robaa, Oliver Einsle, Wolfgang Sippl, Judit Ovádi, Manfred Jung

Version 1 posted 27 May 2020

519

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Analytical Chemistry

Working Paper

Validation of Slow Off-Kinetics of Sirtuin Rearranging Ligands (SirReals) by Means of the Label-Free Electrically Switchable Nanolever Technology

Matthias Schiedel, Herwin Daub, Aymelt Itzen, Manfred Jung

Version 1 posted 20 August 2019

374

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Biological and Medicinal Chemistry

Working Paper

Fragment-Based Identification of Ligands for Bromodomain-Containing Factor 3 of Trypanosoma Cruzi

Corentine Laurin, Joseph Bluck, Anthony Chan, Michelle Keller, Andrew Boczek, Amy Scorah, K. F. Larissa See, Laura Jennings, David Hewings, Fern Woodhouse, Matthias Schiedel, Philip Humphreys, Philip Biggin, Stuart Conway

Version 1 posted 03 September 2020

544

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Biological and Medicinal Chemistry

Working Paper

Fluorescent ligands targeting the intracellular allosteric binding site of the chemokine receptor CCR2

Lara Toy, Max E. Huber, Maximilian F. Schmidt, Dorothee Weikert, Matthias Schiedel

Version 3 posted 25 March 2022

587

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Biological and Medicinal Chemistry

Working Paper

Development of First-in-Class Dual Sirt2/HDAC6 Inhibitors as Molecular Tools for Dual Inhibition of Tubulin Deacetylation

Laura Sinatra, Anja Vogelmann, Florian Friedrich, Margarita Tararina, Emilia Neuwirt, Arianna Colcerasa, Philipp König, Lara Toy, Talha Yesiloglu, Sebastian Hilscher, Lena Gaitzsch, Niklas Papenkordt, Shiyang Zhai, Lin Zhang, Christophe Romier, Oliver Einsle, Wolfgang Sippl, Mike Schutkowski, Olaf Groß, Gerd Bendas, David Christianson, Finn Hansen, Manfred Jung, Matthias Schiedel

Version 3 posted 03 October 2023

430

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Biological and Medicinal Chemistry

Working Paper

Fluorescent Ligand Enables Target Engagement Studies for the Intracellular Allosteric Binding Site of the Chemokine Receptor CXCR2

Max Huber, Silas Wurnig, Lara Toy, Corinna Weiler, Nicole Merten, Evi Kostenis, Finn Hansen, Matthias Schiedel

Version 4 posted 28 April 2023

398

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Biological and Medicinal Chemistry

Working Paper

Mutate and Conjugate: A Method to Enable Rapid In-Cell Target Validation

Adam Thomas, Marta Serafini, Emma Grant, Edward Coombs, Joseph Bluck, Matthias Schiedel, Michael McDonough, Jessica Reynolds, Bernadette Lee, Michael Platt, Vassilena Sharlandjieva, Philip Biggin, Fernanda Duarte, Thomas Milne, Jacob Bush, Stuart Conway

Version 1 posted 25 July 2023

382

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Biological and Medicinal Chemistry

Working Paper

Development of a NanoBRET assay to validate inhibitors of Sirt2-mediated lysine deacetylation and defatty-acylation that block prostate cancer cell migration

Anja Vogelmann, Matthias Schiedel, Nathalie Wössner, Annika Merz, Daniel Herp, Sören Hammelmann, Arianna Colcerasa, Garrison Komaniecki, Jun Young Hong, Manuela Sum, Eric Metzger, Emilia Neuwirt, Lin Zhang, Oliver Einsle, Olaf Groß, Roland Schüle, Hening Lin, Wolfgang Sippl, Manfred Jung

Version 2 posted 24 February 2022

634

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Biological and Medicinal Chemistry

Working Paper

Small molecule ligands of the BET-like bromodomain, SmBRD3, affect Schistosoma mansoni survival, oviposition, and development

Matthias Schiedel, Darius McArdle, Gilda Padalino, Anthony Chan, Josephine Forde-Thomas, Michael McDonough, Helen Whiteland, Manfred Beckmann, Rosa Cookson, Karl Hoffmann, Stuart Conway

Version 1 posted 26 June 2023

202

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10 results in Matthias Schiedel in Authors: Matthias Schiedel

Controlling Intramolecular Interactions in the Design of Selective, High-Affinity, Ligands for the CREBBP Bromodomain

HaloTag-Targeted Sirtuin Rearranging Ligand (SirReal) for the Development of Proteolysis Targeting Chimeras (PROTACs) Against the Lysine Deacetylase Sirtuin 2 (Sirt2)

Validation of Slow Off-Kinetics of Sirtuin Rearranging Ligands (SirReals) by Means of the Label-Free Electrically Switchable Nanolever Technology

Fragment-Based Identification of Ligands for Bromodomain-Containing Factor 3 of Trypanosoma Cruzi

Fluorescent ligands targeting the intracellular allosteric binding site of the chemokine receptor CCR2

Development of First-in-Class Dual Sirt2/HDAC6 Inhibitors as Molecular Tools for Dual Inhibition of Tubulin Deacetylation

Fluorescent Ligand Enables Target Engagement Studies for the Intracellular Allosteric Binding Site of the Chemokine Receptor CXCR2

Mutate and Conjugate: A Method to Enable Rapid In-Cell Target Validation

Development of a NanoBRET assay to validate inhibitors of Sirt2-mediated lysine deacetylation and defatty-acylation that block prostate cancer cell migration

Small molecule ligands of the BET-like bromodomain, SmBRD3, affect Schistosoma mansoni survival, oviposition, and development

10 results in Authors: Matthias Schiedel