Focused Libraries for Epigenetic Drug Discovery: The Importance of Isosteres

Targeting Bromodomain and Extraterminal Proteins for Drug Discovery: From Current Progress to Technological Development

(2021) Pan Tang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Template-Hopping Approach Leads to Potent, Selective, and Highly Soluble Bromo and Extraterminal Domain (BET) Second Bromodomain (BD2) Inhibitors

(2021) Helen E. Aylott et al.   JOURNAL OF MEDICINAL CHEMISTRY

Bidentate Directing Groups: An Efficient Tool in C–H Bond Functionalization Chemistry for the Expedient Construction of C–C Bonds

(2020) Supriya Rej et al.   CHEMICAL REVIEWS

Structurally novel PI3Kδ/γ dual inhibitors characterized by a seven-membered spirocyclic spacer: The SARs investigation and PK evaluation

(2020) Qiangqiang Tao et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Selective targeting of BD1 and BD2 of the BET proteins in cancer and immuno-inflammation

(2020) Omer Gilan et al.   SCIENCE

Epigenetic Chemical Biology: Opportunities Beyond the Advances and Opportunities in Epigenetic Chemical Biology

(2020) Jenna N Beyer et al.   CHEMBIOCHEM

The Design and Synthesis of a Highly Selective and In Vivo Capable Inhibitor of the Second Bromodomain (BD2) of the Bromodomain and Extra Terminal Domain (BET) Family of Proteins

(2020) Alex Preston et al.   JOURNAL OF MEDICINAL CHEMISTRY

Epigenetic Therapies for Cancer

(2020) Susan E. Bates   NEW ENGLAND JOURNAL OF MEDICINE

The dual PI3Kδ/CK1ε inhibitor umbralisib exhibits unique immunomodulatory effects on CLL T cells

(2020) Kamira Maharaj et al.   Blood Advances

Fragment-based discovery of a chemical probe for the PWWP1 domain of NSD3

(2019) Jark Böttcher et al.   Nature Chemical Biology

Phosphatidylinositol 3 kinase (PI3K) inhibitors as new weapon to combat cancer

(2019) Fatma M. Elmenier et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Cancer's epigenetic drugs: where are they in the cancer medicines?

(2019) Sorayya Ghasemi   PHARMACOGENOMICS JOURNAL

Organic synthesis provides opportunities to transform drug discovery

(2018) David C. Blakemore et al.   Nature Chemistry

Profiling and Application of Photoredox C(sp3)–C(sp2) Cross-Coupling in Medicinal Chemistry

(2018) Rui Zhang et al.   ACS Medicinal Chemistry Letters

Inhibitors of histone acetyltransferases KAT6A/B induce senescence and arrest tumour growth

(2018) Jonathan B. Baell et al.   NATURE

Expanding the medicinal chemistry synthetic toolbox

(2018) Jonas Boström et al.   NATURE REVIEWS DRUG DISCOVERY

Beyond the Rule of 5: Lessons Learned from AbbVie’s Drugs and Compound Collection

(2017) David A. DeGoey et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours

(2017) Loren M. Lasko et al.   NATURE

Assay interference and off-target liabilities of reported histone acetyltransferase inhibitors

(2017) Jayme L. Dahlin et al.   Nature Communications

Molecular inflation, attrition and the rule of five

(2016) Paul D. Leeson   ADVANCED DRUG DELIVERY REVIEWS

Kinetic and structural insights into the binding of histone deacetylase 1 and 2 (HDAC1, 2) inhibitors

(2016) Florence F. Wagner et al.   BIOORGANIC & MEDICINAL CHEMISTRY

The medicinal chemist's toolbox for late stage functionalization of drug-like molecules

(2016) Tim Cernak et al.   CHEMICAL SOCIETY REVIEWS

KATching-Up on Small Molecule Modulators of Lysine Acetyltransferases

(2016) Roman P. Simon et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat

(2016) Kevin W. Kuntz et al.   JOURNAL OF MEDICINAL CHEMISTRY

Recent Progress in Histone Demethylase Inhibitors

(2016) Tom E. McAllister et al.   JOURNAL OF MEDICINAL CHEMISTRY

Understanding the Complexity of Epigenetic Target Space

(2016) Vineet Pande   JOURNAL OF MEDICINAL CHEMISTRY

Big Data from Pharmaceutical Patents: A Computational Analysis of Medicinal Chemists’ Bread and Butter

(2016) Nadine Schneider et al.   JOURNAL OF MEDICINAL CHEMISTRY

The molecular hallmarks of epigenetic control

(2016) C. David Allis et al.   NATURE REVIEWS GENETICS

Structure-Guided Discovery of Selective Antagonists for the Chromodomain of Polycomb Repressive Protein CBX7

(2016) Chunyan Ren et al.   ACS Medicinal Chemistry Letters

Chemical Inhibitors of Epigenetic Methyllysine Reader Proteins

(2015) Natalia Milosevich et al.   BIOCHEMISTRY

Kinase hinge binding scaffolds and their hydrogen bond patterns

(2015) Li Xing et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Discovery, design, and synthesis of indole-based EZH2 inhibitors

(2015) Victor S. Gehling et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Small-Molecule Modulators of Methyl-Lysine Binding for the CBX7 Chromodomain

(2015) Chunyan Ren et al.   CHEMISTRY & BIOLOGY

Analysis of Past and Present Synthetic Methodologies on Medicinal Chemistry: Where Have All the New Reactions Gone?

(2015) Dean G. Brown et al.   JOURNAL OF MEDICINAL CHEMISTRY

Small Molecule Inhibitors of Bromodomain–Acetyl-lysine Interactions

(2014) Michael Brand et al.   ACS Chemical Biology

Drugging the undruggable RAS: Mission Possible?

(2014) Adrienne D. Cox et al.   NATURE REVIEWS DRUG DISCOVERY

Late-Stage Fluorination: From Fundamentals to Application

(2014) Michael G. Campbell et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Writers and Readers of Histone Acetylation: Structure, Mechanism, and Inhibition

(2014) R. Marmorstein et al.   Cold Spring Harbor Perspectives in Biology

Small molecule inhibitors of histone acetyltransferases and deacetylases are potential drugs for inflammatory diseases

(2013) Frank J. Dekker et al.   DRUG DISCOVERY TODAY

Discovery of Epigenetic Regulator I-BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the BET Bromodomains

(2013) Olivier Mirguet et al.   JOURNAL OF MEDICINAL CHEMISTRY

Small molecule epigenetic inhibitors targeted to histone lysine methyltransferases and demethylases

(2013) Zhanxin Wang et al.   QUARTERLY REVIEWS OF BIOPHYSICS

Structural Insights into Acetylated-Histone H4 Recognition by the Bromodomain-PHD Finger Module of Human Transcriptional Coactivator CBP

(2013) Alexander N. Plotnikov et al.   STRUCTURE

Development and evaluation of selective, reversible LSD1 inhibitors derived from fragments

(2013) James R. Hitchin et al.   MedChemComm

Lead-Oriented Synthesis: A New Opportunity for Synthetic Chemistry

(2012) Alan Nadin et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Cancer Genetics and Epigenetics: Two Sides of the Same Coin?

(2012) Jueng Soo You et al.   CANCER CELL

A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells

(2012) Sarah K Knutson et al.   Nature Chemical Biology

Vemurafenib: the first drug approved for BRAF-mutant cancer

(2012) Gideon Bollag et al.   NATURE REVIEWS DRUG DISCOVERY

Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation

(2012) W. Qi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2

(2012) Sharad K. Verma et al.   ACS Medicinal Chemistry Letters

Biology-Oriented Synthesis

(2011) Stefan Wetzel et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Small-Molecule Ligands of Methyl-Lysine Binding Proteins

(2011) J. Martin Herold et al.   JOURNAL OF MEDICINAL CHEMISTRY

3,5-Dimethylisoxazoles Act As Acetyl-lysine-mimetic Bromodomain Ligands

(2011) David S. Hewings et al.   JOURNAL OF MEDICINAL CHEMISTRY

What Do Medicinal Chemists Actually Make? A 50-Year Retrospective

(2011) W. Patrick Walters et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Medicinal Chemist’s Toolbox: An Analysis of Reactions Used in the Pursuit of Drug Candidates

(2011) Stephen D. Roughley et al.   JOURNAL OF MEDICINAL CHEMISTRY

Factors Determining the Selection of Organic Reactions by Medicinal Chemists and the Use of These Reactions in Arrays (Small Focused Libraries)

(2010) Tony W. J. Cooper et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Diversity-oriented synthesis as a tool for the discovery of novel biologically active small molecules

(2010) Warren R.J.D. Galloway et al.   Nature Communications

Monocyclic aromatic amines as potential human carcinogens: old is new again

(2009) P. L. Skipper et al.   CARCINOGENESIS

An operational definition of epigenetics

(2009) S. L. Berger et al.   GENES & DEVELOPMENT

Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294

(2009) Yanqi Chang et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Physiochemical drug properties associated with in vivo toxicological outcomes

(2008) Jason D. Hughes et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Exploration of the internal cavity of histone deacetylase (HDAC) with selective HDAC1/HDAC2 inhibitors (SHI-1:2)

(2007) Joey L. Methot et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS