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

International ed. in English, 2017

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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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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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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 design of molecular cancer therapeutics

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

2009

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Pan RAS-binding compounds selected from a chemical library by inhibiting interaction between RAS and a reduced affinity intracellular antibody

Scientific reports, 2021-01, Vol.11 (1), p.1712-1712, Article 1712

2021

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Scaffold-Focused Virtual Screening: Prospective Application to the Discovery of TTK Inhibitors

Journal of chemical information and modeling, 2013-05, Vol.53 (5), p.1100-1112

2013

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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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A super-potent tetramerized ACE2 protein displays enhanced neutralization of SARS-CoV-2 virus infection

Scientific reports, 2021-05, Vol.11 (1), p.10617-10617, Article 10617

2021

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Structure of the Epigenetic Oncogene MMSET and Inhibition by N‑Alkyl Sinefungin Derivatives

ACS chemical biology, 2016-11, Vol.11 (11), p.3093-3105

2016

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Exploiting Protein Conformational Change to Optimize Adenosine-Derived Inhibitors of HSP70

Journal of medicinal chemistry, 2016-05, Vol.59 (10), p.4625-4636

2016

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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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Implementing a method for engineering multivalency to substantially enhance binding of clinical trial anti-SARS-CoV-2 antibodies to wildtype spike and variants of concern proteins

Scientific reports, 2021-05, Vol.11 (1), p.10475-10475, Article 10475

2021

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

Scientific reports, 2022-11, Vol.12 (1), p.18633-18633, Article 18633

2022

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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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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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Structure-Based Design of Orally Bioavailable 1H‑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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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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Drugging the PI3 Kinome: From Chemical Tools to Drugs in the Clinic

An Irreversible Inhibitor of HSP72 that Unexpectedly Targets Lysine‐56

Structure-based drug design: aiming for a perfect fit

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

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

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

Structure-based design of molecular cancer therapeutics

Pan RAS-binding compounds selected from a chemical library by inhibiting interaction between RAS and a reduced affinity intracellular antibody

Discovery of a Chemical Probe Bisamide (CCT251236): An Orally Bioavailable Efficacious Pirin Ligand from a Heat Shock Transcription Factor 1 (HSF1) Phenotypic Screen

Scaffold-Focused Virtual Screening: Prospective Application to the Discovery of TTK Inhibitors

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

A super-potent tetramerized ACE2 protein displays enhanced neutralization of SARS-CoV-2 virus infection

Structure of the Epigenetic Oncogene MMSET and Inhibition by N‑Alkyl Sinefungin Derivatives

Exploiting Protein Conformational Change to Optimize Adenosine-Derived Inhibitors of HSP70

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

Implementing a method for engineering multivalency to substantially enhance binding of clinical trial anti-SARS-CoV-2 antibodies to wildtype spike and variants of concern proteins

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

Evaluation of APOBEC3B Recognition Motifs by NMR Reveals Preferred Substrates

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

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

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

Optimizing Shape Complementarity Enables the Discovery of Potent Tricyclic BCL6 Inhibitors

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

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

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