Identification of novel small-molecule inhibitors targeting menin–MLL interaction, repurposing the antidiarrheal loperamide

Property Focused Structure-Based Optimization of Small Molecule Inhibitors of the Protein–Protein Interaction between Menin and Mixed Lineage Leukemia (MLL)

(2016) Dmitry Borkin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Progress towards small molecule menin-mixed lineage leukemia (MLL) interaction inhibitors with in vivo utility

(2015) Timothy Senter et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Pharmacologic Inhibition of the Menin-MLL Interaction Blocks Progression of MLL Leukemia In Vivo

(2015) Dmitry Borkin et al.   CANCER CELL

Discovery and development of DNA methyltransferase inhibitors using in silico approaches

(2015) José L. Medina-Franco et al.   DRUG DISCOVERY TODAY

Molecular Mechanism underlying PRMT1 Dimerization for SAM Binding and Methylase Activity

(2015) Ran Zhou et al.   Journal of Chemical Information and Modeling

Rational Design of Orthogonal Multipolar Interactions with Fluorine in Protein–Ligand Complexes

(2015) Jonathan Pollock et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery and Optimization of Novel, Selective Histone Methyltransferase SET7 Inhibitors by Pharmacophore- and Docking-Based Virtual Screening

(2015) Fanwang Meng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Highly Selective Brain-Penetrant Vasopressin 1a Antagonists for the Potential Treatment of Autism via a Chemogenomic and Scaffold Hopping Approach

(2015) Hasane Ratni et al.   JOURNAL OF MEDICINAL CHEMISTRY

Menin-MLL inhibitors block oncogenic transformation by MLL-fusion proteins in a fusion partner-independent manner

(2015) S He et al.   LEUKEMIA

Virtual screening in small molecule discovery for epigenetic targets

(2015) Guo-Bo Li et al.   METHODS

Inhibition of human copper trafficking by a small molecule significantly attenuates cancer cell proliferation

(2015) Jing Wang et al.   Nature Chemistry

Targeting the MLL complex in castration-resistant prostate cancer

(2015) Rohit Malik et al.   NATURE MEDICINE

Epigenetic Medicinal Chemistry

(2015) Robert A. Copeland   ACS Medicinal Chemistry Letters

Discovery of two aminoglycoside antibiotics as inhibitors targeting the menin–mixed lineage leukaemia interface

(2014) Lianchun Li et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Challenges and opportunities in targeting the menin–MLL interaction

(2014) Tomasz Cierpicki et al.   Future Medicinal Chemistry

Cancer epigenetics drug discovery and development: the challenge of hitting the mark

(2014) Robert M. Campbell et al.   JOURNAL OF CLINICAL INVESTIGATION

Targeting DNA Methylation with Small Molecules: What’s Next?

(2014) Alexandre Erdmann et al.   JOURNAL OF MEDICINAL CHEMISTRY

High-Affinity Small-Molecule Inhibitors of the Menin-Mixed Lineage Leukemia (MLL) Interaction Closely Mimic a Natural Protein–Protein Interaction

(2014) Shihan He et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identifying Novel Selective Non-Nucleoside DNA Methyltransferase 1 Inhibitors through Docking-Based Virtual Screening

(2014) Shijie Chen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Astemizole Arrests the Proliferation of Cancer Cells by Disrupting the EZH2-EED Interaction of Polycomb Repressive Complex 2

(2014) Xiangqian Kong et al.   JOURNAL OF MEDICINAL CHEMISTRY

Virtual screening and biological evaluation of novel small molecular inhibitors against protein arginine methyltransferase 1 (PRMT1)

(2014) Yiqian Xie et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Distinct pathways regulated by menin and by MLL1 in hematopoietic stem cells and developing B cells

(2013) B. E. Li et al.   BLOOD

Interplay between the Cancer Genome and Epigenome

(2013) Hui Shen et al.   CELL

Synthesis of 4-Arylpiperidin-4-ol Derivatives of Loperamide as Agents with Potent Antiproliferative Effects against HCT-116 and HL-60 Cells

(2013) Noriyuki Hatae et al.   HETEROCYCLES

Scaffold Hopping by Fragment Replacement

(2013) Mikko J. Vainio et al.   Journal of Chemical Information and Modeling

Discovery of Pteridin-7(8H)-one-Based Irreversible Inhibitors Targeting the Epidermal Growth Factor Receptor (EGFR) Kinase T790M/L858R Mutant

(2013) Wei Zhou et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Novel Small-Molecule Inhibitors of BRD4 Using Structure-Based Virtual Screening

(2013) Lewis R. Vidler et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structural insights into inhibition of the bivalent menin-MLL interaction by small molecules in leukemia

(2012) A. Shi et al.   BLOOD

Cancer Epigenetics: From Mechanism to Therapy

(2012) Mark A. Dawson et al.   CELL

Pharmacophore-Based Virtual Screening and Biological Evaluation of Small Molecule Inhibitors for Protein Arginine Methylation

(2012) Juxian Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure-Based Design of High-Affinity Macrocyclic Peptidomimetics to Block the Menin-Mixed Lineage Leukemia 1 (MLL1) Protein–Protein Interaction

(2012) Haibin Zhou et al.   JOURNAL OF MEDICINAL CHEMISTRY

Chemical and biochemical approaches in the study of histone methylation and demethylation

(2012) Keqin Kathy Li et al.   MEDICINAL RESEARCH REVIEWS

The same pocket in menin binds both MLL and JUND but has opposite effects on transcription

(2012) Jing Huang et al.   NATURE

Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia

(2012) Jolanta Grembecka et al.   Nature Chemical Biology

Epigenetic protein families: a new frontier for drug discovery

(2012) Cheryl H. Arrowsmith et al.   NATURE REVIEWS DRUG DISCOVERY

The Pathogenesis of Mixed-Lineage Leukemia

(2011) Andrew G. Muntean et al.   Annual Review of Pathology-Mechanisms of Disease

Regulation of chromatin by histone modifications

(2011) Andrew J Bannister et al.   CELL RESEARCH

SHAFTS: A Hybrid Approach for 3D Molecular Similarity Calculation. 1. Method and Assessment of Virtual Screening

(2011) Xiaofeng Liu et al.   Journal of Chemical Information and Modeling

LigPlot+: Multiple Ligand–Protein Interaction Diagrams for Drug Discovery

(2011) Roman A. Laskowski et al.   Journal of Chemical Information and Modeling

SHAFTS: A Hybrid Approach for 3D Molecular Similarity Calculation. 2. Prospective Case Study in the Discovery of Diverse p90 Ribosomal S6 Protein Kinase 2 Inhibitors To Suppress Cell Migration

(2011) Weiqiang Lu et al.   JOURNAL OF MEDICINAL CHEMISTRY

4-Aryl piperazine and piperidine amides as novel mGluR5 positive allosteric modulators

(2010) Hui Xiong et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

MLL fusions: Pathways to leukemia

(2010) Han Liu et al.   CANCER BIOLOGY & THERAPY

A validated stability-indicating gas chromatography method for determination of divalproex sodium impurities in pharmaceutical preparation

(2010) Acharya Subasranjan et al.   Drug Testing and Analysis

Molecular Basis of the Mixed Lineage Leukemia-Menin Interaction

(2010) Jolanta Grembecka et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The Role of Histone Modifications and Variants in Regulating Gene Expression in Breast Cancer

(2010) Mathieu Dalvai et al.   JOURNAL OF MAMMARY GLAND BIOLOGY AND NEOPLASIA

Docking-enabled pharmacophore model for histone deacetylase 8 inhibitors and its application in anti-cancer drug discovery

(2010) Thangapandian Sundarapandian et al.   JOURNAL OF MOLECULAR GRAPHICS & MODELLING

Chromatin remodelling during development

(2010) Lena Ho et al.   NATURE

Epigenetic Drugs Take On Cancer

(2010) Jocelyn Kaiser   SCIENCE

New insights to the MLL recombinome of acute leukemias

(2009) C Meyer et al.   LEUKEMIA

Menin Critically Links MLL Proteins with LEDGF on Cancer-Associated Target Genes

(2008) Akihiko Yokoyama et al.   CANCER CELL

H3K79 Methylation Profiles Define Murine and Human MLL-AF4 Leukemias

(2008) Andrei V. Krivtsov et al.   CANCER CELL