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Targeting HSP70: The second potentially druggable heat shock protein and molecular chaperone?

Cell cycle (Georgetown, Tex.), 2010-04, Vol.9 (8), p.1542-1550

2010

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Structure-based drug design: aiming for a perfect fit

Essays in biochemistry, 2017-11, Vol.61 (5), p.431-437

2017

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Drugging the PI3 Kinome: From Chemical Tools to Drugs in the Clinic

Cancer research (Chicago, Ill.), 2010-03, Vol.70 (6), p.2146-2157

2010

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An Irreversible Inhibitor of HSP72 that Unexpectedly Targets Lysine‐56

Angewandte Chemie International Edition, 2017-03, Vol.56 (13), p.3536-3540

International ed. in English, 2017

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Benzimidazole inhibitors of the protein kinase CHK2: Clarification of the binding mode by flexible side chain docking and protein–ligand crystallography

Bioorganic & medicinal chemistry, 2012-11, Vol.20 (22), p.6630-6639

2012

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High Proliferation Rate and a Compromised Spindle Assembly Checkpoint Confers Sensitivity to the MPS1 Inhibitor BOS172722 in Triple-Negative Breast Cancers

Molecular cancer therapeutics, 2019-10, Vol.18 (10), p.1696-1707

2019

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Structure-based design of molecular cancer therapeutics

Trends in biotechnology (Regular ed.), 2009-05, Vol.27 (5), p.315-328

2009

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C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays

European journal of medicinal chemistry, 2019-09, Vol.177, p.316-337

2019

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iTAG an optimized IMiD-induced degron for targeted protein degradation in human and murine cells

iScience, 2023-07, Vol.26 (7), p.107059-107059, Article 107059

2023

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Molecular recognition of ternary complexes: a new dimension in the structure-guided design of chemical degraders

Essays in biochemistry, 2017-11, Vol.61 (5), p.505-516

2017

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Current perspectives in fragment-based lead discovery (FBLD)

Essays in biochemistry, 2017-11, Vol.61 (5), p.453-464

2017

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Identification of autophosphorylation inhibitors of the inositol-requiring enzyme 1 alpha (IRE1α) by high-throughput screening using a DELFIA assay

Journal of biomolecular screening, 2013-03, Vol.18 (3), p.298-308

2013

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Fragment-based drug discovery and its application to challenging drug targets

Essays in biochemistry, 2017-11, Vol.61 (5), p.475-484

2017

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Structure-based discovery of cyclin-dependent protein kinase inhibitors

Essays in biochemistry, 2017-11, Vol.61 (5), p.439-452

2017

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Achieving In Vivo Target Depletion through the Discovery and Optimization of Benzimidazolone BCL6 Degraders

Journal of medicinal chemistry, 2020-04, Vol.63 (8), p.4047-4068

2020

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Oxidation state of the active-site cysteine in protein tyrosine phosphatase 1B

Nature (London), 2003-06, Vol.423 (6941), p.773-777

2003

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The potential of cryo-electron microscopy for structure-based drug design

Essays in biochemistry, 2017-11, Vol.61 (5), p.543-560

2017

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Protein degradation: a validated therapeutic strategy with exciting prospects

Essays in biochemistry, 2017-11, Vol.61 (5), p.517-527

2017

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Structural and functional characterisation of human RNA helicase DHX8 provides insights into the mechanism of RNA-stimulated ADP release

Biochemical journal, 2019-09, Vol.476 (18), p.2521-2543

2019

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8‑Substituted Pyrido[3,4‑d]pyrimidin-4(3H)‑one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors

Journal of medicinal chemistry, 2016-02, Vol.59 (4), p.1388-1409

2016

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X-ray free electron laser: opportunities for drug discovery

Essays in biochemistry, 2017-11, Vol.61 (5), p.529-542

2017

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Into Deep Water: Optimizing BCL6 Inhibitors by Growing into a Solvated Pocket

Journal of medicinal chemistry, 2021-12, Vol.64 (23), p.17079-17097

2021

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Synthesis and profiling of a 3-aminopyridin-2-one-based kinase targeted fragment library: Identification of 3-amino-5-(pyridin-4-yl)pyridin-2(1H)-one scaffold for monopolar spindle 1 (MPS1) and Aurora kinases inhibition

Bioorganic & medicinal chemistry, 2018-07, Vol.26 (11), p.3021-3029

2018

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Optimizing Shape Complementarity Enables the Discovery of Potent Tricyclic BCL6 Inhibitors

Journal of medicinal chemistry, 2022-06, Vol.65 (12), p.8169-8190

2022

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Mass spectrometry for fragment screening

Essays in biochemistry, 2017-11, Vol.61 (5), p.465-473

2017

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Targeting HSP70: The second potentially druggable heat shock protein and molecular chaperone?

Structure-based drug design: aiming for a perfect fit

Drugging the PI3 Kinome: From Chemical Tools to Drugs in the Clinic

An Irreversible Inhibitor of HSP72 that Unexpectedly Targets Lysine‐56

Benzimidazole inhibitors of the protein kinase CHK2: Clarification of the binding mode by flexible side chain docking and protein–ligand crystallography

High Proliferation Rate and a Compromised Spindle Assembly Checkpoint Confers Sensitivity to the MPS1 Inhibitor BOS172722 in Triple-Negative Breast Cancers

Structure-based design of molecular cancer therapeutics

C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays

iTAG an optimized IMiD-induced degron for targeted protein degradation in human and murine cells

Molecular recognition of ternary complexes: a new dimension in the structure-guided design of chemical degraders

Current perspectives in fragment-based lead discovery (FBLD)

Identification of autophosphorylation inhibitors of the inositol-requiring enzyme 1 alpha (IRE1α) by high-throughput screening using a DELFIA assay

Fragment-based drug discovery and its application to challenging drug targets

Structure-based discovery of cyclin-dependent protein kinase inhibitors

Achieving In Vivo Target Depletion through the Discovery and Optimization of Benzimidazolone BCL6 Degraders

Oxidation state of the active-site cysteine in protein tyrosine phosphatase 1B

The potential of cryo-electron microscopy for structure-based drug design

Protein degradation: a validated therapeutic strategy with exciting prospects

Structural and functional characterisation of human RNA helicase DHX8 provides insights into the mechanism of RNA-stimulated ADP release

8‑Substituted Pyrido[3,4‑d]pyrimidin-4(3H)‑one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors

X-ray free electron laser: opportunities for drug discovery

Into Deep Water: Optimizing BCL6 Inhibitors by Growing into a Solvated Pocket

Synthesis and profiling of a 3-aminopyridin-2-one-based kinase targeted fragment library: Identification of 3-amino-5-(pyridin-4-yl)pyridin-2(1H)-one scaffold for monopolar spindle 1 (MPS1) and Aurora kinases inhibition

Optimizing Shape Complementarity Enables the Discovery of Potent Tricyclic BCL6 Inhibitors

Mass spectrometry for fragment screening

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