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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

2017

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An Irreversible Inhibitor of HSP72 that Unexpectedly Targets Lysine‐56

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

International ed. in English, 2017

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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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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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Current perspectives in fragment-based lead discovery (FBLD)

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

2017

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Structure-based discovery of cyclin-dependent protein kinase inhibitors

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

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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Protein degradation: a validated therapeutic strategy with exciting prospects

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

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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X-ray free electron laser: opportunities for drug discovery

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

2017

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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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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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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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Mass spectrometry for fragment screening

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

2017

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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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The SGC beyond structural genomics: redefining the role of 3D structures by coupling genomic stratification with fragment-based discovery

Essays in biochemistry, 2017-11, Vol.61 (5), p.495

2017

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Evaluation of APOBEC3B Recognition Motifs by NMR Reveals Preferred Substrates

ACS chemical biology, 2018-09, Vol.13 (9), p.2427-2432

2018

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Rapid Discovery of Pyrido[3,4‑d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach

Journal of medicinal chemistry, 2016-04, Vol.59 (8), p.3671-3688

2016

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Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 In Vivo

Journal of medicinal chemistry, 2022-06, Vol.65 (12), p.8191-8207

2022

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Benzimidazole Inhibitors Induce a DFG-Out Conformation of Never in Mitosis Gene A-Related Kinase 2 (Nek2) without Binding to the Back Pocket and Reveal a Nonlinear Structure−Activity Relationship

Journal of medicinal chemistry, 2011-03, Vol.54 (6), p.1626-1639

2011

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Structure-Based Design of Orally Bioavailable 1 H -Pyrrolo[3,2- c ]pyridine Inhibitors of Mitotic Kinase Monopolar Spindle 1 (MPS1)

Journal of medicinal chemistry, 2013-12, Vol.56 (24), p.10045-10065

2013

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Naturally Occurring Mutations in the MPS1 Gene Predispose Cells to Kinase Inhibitor Drug Resistance

Cancer research (Chicago, Ill.), 2015-08, Vol.75 (16), p.3340-3354

2015

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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

An Irreversible Inhibitor of HSP72 that Unexpectedly Targets Lysine‐56

Structure-based design of molecular cancer therapeutics

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

Current perspectives in fragment-based lead discovery (FBLD)

Structure-based discovery of cyclin-dependent protein kinase inhibitors

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

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

X-ray free electron laser: opportunities for drug discovery

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

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

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

Mass spectrometry for fragment screening

Optimizing Shape Complementarity Enables the Discovery of Potent Tricyclic BCL6 Inhibitors

The SGC beyond structural genomics: redefining the role of 3D structures by coupling genomic stratification with fragment-based discovery

Discovering cell-active BCL6 inhibitors: effectively combining biochemical HTS with multiple biophysical techniques, X-ray crystallography and cell-based assays

Evaluation of APOBEC3B Recognition Motifs by NMR Reveals Preferred Substrates

Discovery of an In Vivo Chemical Probe for BCL6 Inhibition by Optimization of Tricyclic Quinolinones

Rapid Discovery of Pyrido[3,4‑d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach

Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 In Vivo

Benzimidazole Inhibitors Induce a DFG-Out Conformation of Never in Mitosis Gene A-Related Kinase 2 (Nek2) without Binding to the Back Pocket and Reveal a Nonlinear Structure−Activity Relationship

Structure-Based Design of Orally Bioavailable 1 H -Pyrrolo[3,2- c ]pyridine Inhibitors of Mitotic Kinase Monopolar Spindle 1 (MPS1)

Naturally Occurring Mutations in the MPS1 Gene Predispose Cells to Kinase Inhibitor Drug Resistance

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