M. Schimpl

发表

Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors.

Rhys D O Jones, S. Guichard, W. Shao, 2018, Journal of medicinal chemistry.

Fragment-Based Design of a Potent MAT2a Inhibitor and in Vivo Evaluation in an MTAP Null Xenograft Model.

S. Tentarelli, M. Vázquez‐Chantada, E. Chiarparin, 2021, Journal of medicinal chemistry.

A-loop interactions in Mer tyrosine kinase give rise to inhibitors with two-step mechanism and long residence time of binding

J. Nissink, R. Overman, P. Rawlins, 2020, The Biochemical journal.

Alkynyl Benzoxazines and Dihydroquinazolines as Cysteine Targeting Covalent Warheads and Their Application in Identification of Selective Irreversible Kinase Inhibitors.

David M. Robinson, M. Waring, D. Ogg, 2020, Journal of the American Chemical Society.

Structural and binding characterization of the LacdiNAc-specific adhesin (LabA; HopD) exodomain from Helicobacter pylori

P. Gellert, G. S. Winkler, S. Stolnik, 2020, Current research in structural biology.

Discovery of a Potent and Selective ATAD2 Bromodomain Inhibitor with Antiproliferative Activity in Breast Cancer Models.

Nichola L. Davies, A. Rabow, S. Guichard, 2022, Journal of medicinal chemistry.

O-GlcNAcase: Promiscuous Hexosaminidase or Key Regulator of O-GlcNAc Signaling?

D. V. van Aalten, J. Alonso, M. Schimpl, 2014, The Journal of Biological Chemistry.

O-GlcNAcase: Promiscuous Hexosaminidase or Key Regulator ofO-GlcNAc

J. Alonso, M. Schimpl, D. V. Aalten, 2014 .

Human YKL-39 is a pseudo-chitinase with retained chitooligosaccharide-binding properties.

D. V. van Aalten, I. Eggleston, A. Recklies, 2012, The Biochemical journal.

PARP Power: A Structural Perspective on PARP1, PARP2, and PARP3 in DNA Damage Repair and Nucleosome Remodelling

L. Spagnolo, Taiana Maia de Oliveira, Lotte van Beek, 2021, International journal of molecular sciences.

Generating Selective Leads for Mer Kinase Inhibitors-Example of a Comprehensive Lead-Generation Strategy.

Anthony D. Keefe, E. Hennessy, A. Keefe, 2021, Journal of medicinal chemistry.

GlcNAcstatin: a picomolar, selective O-GlcNAcase inhibitor that modulates intracellular O-glcNAcylation levels.

D. V. van Aalten, N. Shpiro, V. Borodkin, 2006, Journal of the American Chemical Society.

GlcNAcstatins are nanomolar inhibitors of human O-GlcNAcase inducing cellular hyper-O-GlcNAcylation

D. V. van Aalten, V. Borodkin, M. Schimpl, 2009, The Biochemical journal.

Bisubstrate UDP–peptide conjugates as human O-GlcNAc transferase inhibitors

D. Robinson, M. Gundogdu, V. Borodkin, 2013, The Biochemical journal.

Tyrosine glycosylation of Rho by Yersinia toxin impairs blastomere cell behaviour in zebrafish embryos

W. Driever, D. V. van Aalten, S. Wiese, 2015, Nature Communications.

Mapping the binding sites of antibodies utilized in programmed cell death ligand-1 predictive immunohistochemical assays for use with immuno-oncology therapies

C. Stubbs, G. Williams, J. Hunt, 2019, Modern Pathology.

Regulation of Caenorhabditis elegans p53/CEP-1–Dependent Germ Cell Apoptosis by Ras/MAPK Signaling

R. Dickinson, A. Gartner, A. Craig, 2011, PLoS genetics.

Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide (AZD5305): A PARP1-DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs.

Fiona Pachl, A. Pike, M. O’Connor, 2021, Journal of medicinal chemistry.

The active site of O-GlcNAc transferase imposes constraints on substrate sequence

A. W. Schüttelkopf, D. V. van Aalten, J. Alonso, 2015, Nature Structural &Molecular Biology.

Loss of CRMP2 O-GlcNAcylation leads to reduced novel object recognition performance in mice

K. Read, A. Heck, D. V. van Aalten, 2019, Open Biology.

The discovery of 7-methyl-2-[(7-methyl[1,2,4]triazolo[1,5-a]pyridin-6-yl)amino]-9-(tetrahydro-2H-pyran-4-yl)-7,9-dihydro-8H-purin-8-one (AZD7648), a potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor.

B. Davies, M. Vázquez‐Chantada, G. Lamont, 2019, Journal of medicinal chemistry.

Dual functionality of O-GlcNAc transferase is required for Drosophila development

D. V. van Aalten, H. Müller, O. Raimi, 2015, Open Biology.

O-GlcNAc transferase invokes nucleotide sugar pyrophosphate participation in catalysis

A. W. Schüttelkopf, D. V. van Aalten, D. Robinson, 2012, Nature chemical biology.

Dynamics of the HD regulatory subdomain of PARP-1; substrate access and allostery in PARP activation and inhibition

J. Pascal, Ji-Chun Yang, D. Neuhaus, 2020, bioRxiv.

Synergy of Peptide and Sugar in O-GlcNAcase Substrate Recognition

D. V. van Aalten, V. Borodkin, M. Schimpl, 2012, Chemistry & biology.

Human OGA binds substrates in a conserved peptide recognition groove

A. W. Schüttelkopf, D. V. van Aalten, V. Borodkin, 2010, The Biochemical journal.

Development of Specific, Irreversible Inhibitors for a Receptor Tyrosine Kinase EphB3.

F. Ni, R. Overman, Ying-Chu Chen, 2016, Journal of the American Chemical Society.

Cell-Penetrant, Nanomolar O-GlcNAcase Inhibitors Selective against Lysosomal Hexosaminidases

K. Read, D. V. van Aalten, V. Borodkin, 2010, Chemistry & biology.

Optimization of hERG and Pharmacokinetic Properties for Basic Dihydro-8H-purin-8-one Inhibitors of DNA-PK.

B. Davies, M. Vázquez‐Chantada, G. Lamont, 2022, ACS medicinal chemistry letters.

Optimization of an Imidazo[1,2-a]pyridine Series to Afford Highly Selective Type I1/2 Dual Mer/Axl Kinase Inhibitors with In Vivo Efficacy.

E. Hennessy, Nichola L. Davies, A. Doherty, 2021, Journal of medicinal chemistry.

A Chemical-Genetic Approach to Generate Selective Covalent Inhibitors of Protein Kinases.

R. Overman, Ying-Chu Chen, Alvin Kung, 2017, ACS chemical biology.

Combining structural and coevolution information to unveil allosteric sites

H. Gohlke, Christopher Pfleger, J. Janet, 2023, Chemical science.

Human OGA binds substrates in a conserved peptide recognition groove

A. W. Schüttelkopf, D. V. van Aalten, V. Borodkin, 2010, The Biochemical journal.

A Chemical-Genetic Approach to Generate Selective Covalent Inhibitors of Protein Kinases.

R. Overman, Ying-Chu Chen, Alvin Kung, 2017, ACS chemical biology.

Discovery, Optimization, and Biological Evaluation of Arylpyridones as Cbl-b Inhibitors.

V. Kantae, N. Grimster, M. Lamb, 2024, Journal of medicinal chemistry.

Discovery of a Novel Benzodiazepine Series of Cbl-b Inhibitors for the Enhancement of Antitumor Immunity.

Kathryn A. Giblin, N. Grimster, M. Lamb, 2023, ACS medicinal chemistry letters.