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Harnessing Fluorine–Sulfur Contacts and Multipolar Interactions for the Design of p53 Mutant Y220C Rescue Drugs

ACS chemical biology, 2016-08, Vol.11 (8), p.2265-2274

2016

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A bump-and-hole approach to engineer controlled selectivity of BET bromodomain chemical probes

Science (American Association for the Advancement of Science), 2014-10, Vol.346 (6209), p.638-641

2014

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Defining the Mechanism of Action and Enzymatic Selectivity of Psammaplin A against Its Epigenetic Targets

Journal of medicinal chemistry, 2012-02, Vol.55 (4), p.1731-1750

2012

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Toward Photopharmacological Antimicrobial Chemotherapy Using Photoswitchable Amidohydrolase Inhibitors

ACS infectious diseases, 2017-02, Vol.3 (2), p.152-161

2017

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New Synthetic Routes to Triazolo-benzodiazepine Analogues: Expanding the Scope of the Bump-and-Hole Approach for Selective Bromo and Extra-Terminal (BET) Bromodomain Inhibition

Journal of medicinal chemistry, 2016-02, Vol.59 (4), p.1492-1500

2016

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Key Players in the Mutant p53 Team: Small Molecules, Gene Editing, Immunotherapy

Frontiers in oncology, 2020-08, Vol.10, p.1460-1460

2020

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Thioester derivatives of the natural product psammaplin A as potent histone deacetylase inhibitors

Beilstein journal of organic chemistry, 2013-01, Vol.9 (1), p.81-88

2013

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Gram-Scale Laboratory Synthesis of TC AC 28, a High-Affinity BET Bromodomain Ligand

ACS omega, 2017-08, Vol.2 (8), p.4328-4332

2017

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Is NMR Fragment Screening Fine-Tuned to Assess Druggability of Protein–Protein Interactions?

ACS medicinal chemistry letters, 2014-01, Vol.5 (1), p.23-28

2014

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Biophysical Survey of Small-Molecule β‑Catenin Inhibitors: A Cautionary Tale

Journal of medicinal chemistry, 2022-05, Vol.65 (10), p.7246-7261

2022

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Aminobenzothiazole derivatives stabilize the thermolabile p53 cancer mutant Y220C and show anticancer activity in p53-Y220C cell lines

European journal of medicinal chemistry, 2018-05, Vol.152, p.101-114

2018

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Current strategies for the design of PROTAC linkers: a critical review

Exploration of targeted anti-tumor therapy, 2020-10, Vol.1 (5), p.273-312

2020

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Exploiting Transient Protein States for the Design of Small-Molecule Stabilizers of Mutant p53

Structure (London), 2015-12, Vol.23 (12), p.2246-2255

2015

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Dual wavelength asymmetric photochemical synthesis with circularly polarized light

Chemical science (Cambridge), 2015-07, Vol.6 (7), p.3853-3862

2015

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Structure–Reactivity Studies of 2‑Sulfonylpyrimidines Allow Selective Protein Arylation

Bioconjugate chemistry, 2023-09, Vol.34 (9), p.1679-1687

2023

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Exploring 2‑Sulfonylpyrimidine Warheads as Acrylamide Surrogates for Targeted Covalent Inhibition: A BTK Story

Journal of medicinal chemistry, 2024-08, Vol.67 (16), p.13572-13593

2024

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Thermodynamics of ligand binding to histone deacetylase like amidohydrolase from Bordetella/Alcaligenes

Journal of molecular recognition, 2014-03, Vol.27 (3), p.160-172

2014

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Discovery of Nanomolar-Affinity Pharmacological Chaperones Stabilizing the Oncogenic p53 Mutant Y220C

ACS pharmacology & translational science, 2022-11, Vol.5 (11), p.1169-1180

2022

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Kinetic method for the large-scale analysis of the binding mechanism of histone deacetylase inhibitors

Analytical biochemistry, 2014-09, Vol.460, p.39-46

2014

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New synthetic strategies towards psammaplin A, access to natural product analogues for biological evaluation

Organic & biomolecular chemistry, 2011-02, Vol.9 (3), p.659-662

2011

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Highly Ligand Efficient and Selective N-2-(Thioethyl)picolinamide Histone Deacetylase Inhibitors Inspired by the Natural Product Psammaplin A

ChemMedChem, 2013-01, Vol.8 (1), p.149-156

2013

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Highly Ligand Efficient and Selective N-2-(Thioethyl)picolinamide Histone Deacetylase Inhibitors Inspired by the Natural Product PsammaplinA

ChemMedChem, 2013-01, Vol.8 (1), p.149

2013

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Dual wavelength asymmetric photochemical synthesis with circularly polarized lightElectronic supplementary information (ESI) available: Full detailed methods used for the entire study; further discussion of the work not central to the main message of the paper; full derivation of the kinetics models used to predict the dual wavelength enantioselectivity; computational details and energy breakdown; more complete mechanism for the reaction. See DOI: 10.1039/c4sc03897e

2015-06

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Dual wavelength asymmetric photochemical synthesis with circularly polarized light† †Electronic supplementary information (ESI) available: Full detailed methods used for the entire study; further discussion of the work not central to the main message of the paper; full derivation of the kinetics models used to predict the dual wavelength enantioselectivity; computational details and energy breakdown; more complete mechanism for the reaction. See DOI: 10.1039/c4sc03897e

Chemical science (Cambridge), 2015-04, Vol.6 (7), p.3853-3862

2015

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New synthetic strategies towards psammaplin A, access to natural product analogues for biological evaluationElectronic supplementary information (ESI) available: Experimental procedures, biological assay procedures and full characterization for all new compounds. See DOI: 10.1039/c0ob00824a

2011-01

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Harnessing Fluorine–Sulfur Contacts and Multipolar Interactions for the Design of p53 Mutant Y220C Rescue Drugs

A bump-and-hole approach to engineer controlled selectivity of BET bromodomain chemical probes

Defining the Mechanism of Action and Enzymatic Selectivity of Psammaplin A against Its Epigenetic Targets

Toward Photopharmacological Antimicrobial Chemotherapy Using Photoswitchable Amidohydrolase Inhibitors

New Synthetic Routes to Triazolo-benzodiazepine Analogues: Expanding the Scope of the Bump-and-Hole Approach for Selective Bromo and Extra-Terminal (BET) Bromodomain Inhibition

Key Players in the Mutant p53 Team: Small Molecules, Gene Editing, Immunotherapy

Thioester derivatives of the natural product psammaplin A as potent histone deacetylase inhibitors

Gram-Scale Laboratory Synthesis of TC AC 28, a High-Affinity BET Bromodomain Ligand

Is NMR Fragment Screening Fine-Tuned to Assess Druggability of Protein–Protein Interactions?

Biophysical Survey of Small-Molecule β‑Catenin Inhibitors: A Cautionary Tale

Aminobenzothiazole derivatives stabilize the thermolabile p53 cancer mutant Y220C and show anticancer activity in p53-Y220C cell lines

Current strategies for the design of PROTAC linkers: a critical review

Exploiting Transient Protein States for the Design of Small-Molecule Stabilizers of Mutant p53

Dual wavelength asymmetric photochemical synthesis with circularly polarized light

Structure–Reactivity Studies of 2‑Sulfonylpyrimidines Allow Selective Protein Arylation

Exploring 2‑Sulfonylpyrimidine Warheads as Acrylamide Surrogates for Targeted Covalent Inhibition: A BTK Story

Thermodynamics of ligand binding to histone deacetylase like amidohydrolase from Bordetella/Alcaligenes

Discovery of Nanomolar-Affinity Pharmacological Chaperones Stabilizing the Oncogenic p53 Mutant Y220C

Kinetic method for the large-scale analysis of the binding mechanism of histone deacetylase inhibitors

New synthetic strategies towards psammaplin A, access to natural product analogues for biological evaluation

Highly Ligand Efficient and Selective N-2-(Thioethyl)picolinamide Histone Deacetylase Inhibitors Inspired by the Natural Product Psammaplin A

Highly Ligand Efficient and Selective N-2-(Thioethyl)picolinamide Histone Deacetylase Inhibitors Inspired by the Natural Product PsammaplinA

New synthetic strategies towards psammaplin A, access to natural product analogues for biological evaluationElectronic supplementary information (ESI) available: Experimental procedures, biological assay procedures and full characterization for all new compounds. See DOI: 10.1039/c0ob00824a

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