Co-inhibition of HDAC and MLL-menin interaction targets MLL-rearranged acute myeloid leukemia cells via disruption of DNA damage checkpoint and DNA repair

Design of the First-in-Class, Highly Potent Irreversible Inhibitor Targeting the Menin-MLL Protein-Protein Interaction

(2018) Shilin Xu et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

CircNT5E acts as a sponge of microRNA-422a to promote glioblastoma tumorigenesis

(2018) Renjie Wang et al.   CANCER RESEARCH

Complexity of Blocking Bivalent Protein–Protein Interactions: Development of a Highly Potent Inhibitor of the Menin–Mixed-Lineage Leukemia Interaction

(2018) Dmitry Borkin et al.   JOURNAL OF MEDICINAL CHEMISTRY

ATR/CHK1 inhibitors and cancer therapy

(2018) Zhaojun Qiu et al.   RADIOTHERAPY AND ONCOLOGY

Small Molecules Co-targeting CKIα and the Transcriptional Kinases CDK7/9 Control AML in Preclinical Models

(2018) Waleed Minzel et al.   CELL

Distinct pathways affected by menin versus MLL1/MLL2 in MLL-rearranged acute myeloid leukemia

(2018) Yufei Chen et al.   EXPERIMENTAL HEMATOLOGY

Exploring the cytotoxicity, uptake, cellular response, and proteomics of mono- and dinuclear DNA light-switch complexes

(2018) Paul James Jarman et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Combination treatment of acute myeloid leukemia cells with DNMT and HDAC inhibitors: predominant synergistic gene downregulation associated with gene body demethylation

(2018) Nadja Blagitko-Dorfs et al.   LEUKEMIA

Histone Deacetylase Inhibitors as Anticancer Drugs

(2017) Tomas Eckschlager et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Randomized Phase II Study of Clofarabine-Based Consolidation for Younger Adults With Acute Myeloid Leukemia in First Remission

(2017) Xavier Thomas et al.   JOURNAL OF CLINICAL ONCOLOGY

C-terminal BRE overexpression in 11q23-rearranged and t(8;16) acute myeloid leukemia is caused by intragenic transcription initiation

(2017) A E Marneth et al.   LEUKEMIA

Targeting HDAC3, a new partner protein of AKT in the reversal of chemoresistance in acute myeloid leukemia via DNA damage response

(2017) J Long et al.   LEUKEMIA

The HDAC inhibitor panobinostat (LBH589) exerts in vivo anti-leukaemic activity against MLL-rearranged acute lymphoblastic leukaemia and involves the RNF20/RNF40/WAC-H2B ubiquitination axis

(2017) P Garrido Castro et al.   LEUKEMIA

Synergistic antitumor effect of histone deacetylase inhibitor and Doxorubicin in peripheral T-cell lymphoma

(2017) Huilai Zhang et al.   LEUKEMIA RESEARCH

First new drug approval for AML in 15 years

(2017) Cormac Sheridan   NATURE BIOTECHNOLOGY

Low-dose decitabine enhances chidamide-induced apoptosis in adult acute lymphoblast leukemia, especially for p16-deleted patients through DNA damage

(2017) Pengcheng Shi et al.   PHARMACOGENOMICS

ATM-dependent pathways of chromatin remodelling and oxidative DNA damage responses

(2017) N. Daniel Berger et al.   PHILOSOPHICAL TRANSACTIONS OF THE ROYAL SOCIETY B-BIOLOGICAL SCIENCES

Interstrand Crosslink Repair as a Target for HDAC Inhibition

(2017) Teodora Nikolova et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Rad52 competes with Ku70/Ku86 for binding to S-region DSB ends to modulate antibody class-switch DNA recombination

(2017) Hong Zan et al.   Nature Communications

Cooperative effect of chidamide and chemotherapeutic drugs induce apoptosis by DNA damage accumulation and repair defects in acute myeloid leukemia stem and progenitor cells

(2017) Yin Li et al.   Clinical Epigenetics

RAD51 Is a Selective DNA Repair Target to Radiosensitize Glioma Stem Cells

(2017) Harry O. King et al.   Stem Cell Reports

Activation of mPTP-dependent mitochondrial apoptosis pathway by a novel pan HDAC inhibitor resminostat in hepatocellular carcinoma cells

(2016) Meili Fu et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

The NAE inhibitor pevonedistat interacts with the HDAC inhibitor belinostat to target AML cells by disrupting the DDR

(2016) L. Zhou et al.   BLOOD

Association of downregulated HDAC 2 with the impaired mitochondrial function and cytokine secretion in the monocytes/macrophages from gestational diabetes mellitus patients

(2016) Xin Qu et al.   CELL BIOLOGY INTERNATIONAL

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

Complementary activities of DOT1L and Menin inhibitors in MLL-rearranged leukemia

(2016) C Dafflon et al.   LEUKEMIA

SON and Its Alternatively Spliced Isoforms Control MLL Complex-Mediated H3K4me3 and Transcription of Leukemia-Associated Genes

(2016) Jung-Hyun Kim et al.   MOLECULAR CELL

HDAC Inhibitors as Epigenetic Regulators of the Immune System: Impacts on Cancer Therapy and Inflammatory Diseases

(2016) Elizabeth E. Hull et al.   Biomed Research International

Designed to Kill: Novel Menin-MLL Inhibitors Target MLL -Rearranged Leukemia

(2015) Michael W.M. Kühn et al.   CANCER CELL

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

(2015) Dmitry Borkin et al.   CANCER CELL

Mitochondrial ROS Signaling in Organismal Homeostasis

(2015) Gerald S. Shadel et al.   CELL

The interleukin (IL)-1 cytokine family – Balance between agonists and antagonists in inflammatory diseases

(2015) Jennifer Palomo et al.   CYTOKINE

Molecular mechanisms of MLL-associated leukemia

(2015) Akihiko Yokoyama   INTERNATIONAL JOURNAL OF HEMATOLOGY

Signaling pathway of MAPK/ERK in cell proliferation, differentiation, migration, senescence and apoptosis

(2015) Yu Sun et al.   JOURNAL OF RECEPTORS AND SIGNAL TRANSDUCTION

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

(2015) S He et al.   LEUKEMIA

Analysis of class I and II histone deacetylase gene expression in human leukemia

(2015) Hui Yang et al.   LEUKEMIA & LYMPHOMA

HDAC inhibitors still need a home run, despite recent approval

(2015) Malini Guha   NATURE REVIEWS DRUG DISCOVERY

HDAC Inhibitors as Novel Anti-Cancer Therapeutics

(2015) Cristabelle Souza et al.   Recent Patents on Anti-Cancer Drug Discovery

Histone Acetylation Enzymes Coordinate Metabolism and Gene Expression

(2015) Yuan Shen et al.   TRENDS IN PLANT SCIENCE

Small biotech steers HDAC inhibitor to clinic

(2014) Mark Ratner   NATURE BIOTECHNOLOGY

Reversal of Female Infertility by Chk2 Ablation Reveals the Oocyte DNA Damage Checkpoint Pathway

(2014) E. Bolcun-Filas et al.   SCIENCE

NF- B, an Active Player in Human Cancers

(2014) Y. Xia et al.   Cancer Immunology Research

The MLL recombinome of acute leukemias in 2013

(2013) C Meyer et al.   LEUKEMIA

SnapShot: Acute Myeloid Leukemia

(2012) Bernd B. Zeisig et al.   CANCER CELL

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

(2012) Jolanta Grembecka et al.   Nature Chemical Biology

The Pathogenesis of Mixed-Lineage Leukemia

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

The super elongation complex (SEC) and MLL in development and disease

(2011) E. Smith et al.   GENES & DEVELOPMENT

Refinement of cytogenetic classification in acute myeloid leukemia: determination of prognostic significance of rare recurring chromosomal abnormalities among 5876 younger adult patients treated in the United Kingdom Medical Research Council trials

(2010) D. Grimwade et al.   BLOOD

Menin stimulates homology-directed DNA repair

(2010) A. Gallo et al.   FEBS LETTERS

Sulfation of chlorotyrosine and nitrotyrosine by human lung endothelial and epithelial cells: Role of the human SULT1A3

(2010) Shin Yasuda et al.   TOXICOLOGY AND APPLIED PHARMACOLOGY

Novel prognostic subgroups in childhood 11q23/MLL-rearranged acute myeloid leukemia: results of an international retrospective study

(2009) B. V. Balgobind et al.   BLOOD

Characterization of DNA damage-dependent cell cycle checkpoints in a menin-deficient model

(2009) Molly C. Kottemann et al.   DNA REPAIR

Loss of MLL PHD Finger 3 Is Necessary for MLL-ENL-Induced Hematopoietic Stem Cell Immortalization

(2008) J. Chen et al.   CANCER RESEARCH