Chromosome Region Maintenance 1 (XPO1/CRM1) as an Anticancer Target and Discovery of Its Inhibitor

Structure-Guided Design of the First Noncovalent Small-Molecule Inhibitor of CRM1

(2021) Yuqin Lei et al.   JOURNAL OF MEDICINAL CHEMISTRY

Novel Mechanistic Observations and NES-Binding Groove Features Revealed by the CRM1 Inhibitors Plumbagin and Oridonin

(2021) Yuqin Lei et al.   JOURNAL OF NATURAL PRODUCTS

XPO1/CRM1 is a promising prognostic indicator for neuroblastoma and represented a therapeutic target by selective inhibitor verdinexor

(2021) Lijia Pan et al.   JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH

FDA Approval Summary: Selinexor for Relapsed or Refractory Diffuse Large B‐Cell Lymphoma

(2021) Yvette L. Kasamon et al.   ONCOLOGIST

Selinexor for the treatment of multiple myeloma

(2020) Klaus Podar et al.   EXPERT OPINION ON PHARMACOTHERAPY

Small-Molecule Antagonist Targeting Exportin-1 via Rational Structure-Based Discovery

(2020) Xibao Tian et al.   JOURNAL OF MEDICINAL CHEMISTRY

Small Molecule Inhibitors of CRM1

(2020) Bibiana I. Ferreira et al.   Frontiers in Pharmacology

XPO1-dependent nuclear export as a target for cancer therapy

(2020) Nancy G. Azizian et al.   Journal of Hematology & Oncology

Selinexor in patients with relapsed or refractory diffuse large B-cell lymphoma (SADAL): a single-arm, multinational, multicentre, open-label, phase 2 trial

(2020) Nagesh Kalakonda et al.   Lancet Haematology

Sulforaphene inhibits the progression of osteosarcoma via regulating FSTL1/NF-κB pathway

(2020) Guofeng Zhang et al.   LIFE SCIENCES

Plumbagin: A potential anti-cancer compound

(2020) Arpita Roy   MINI-REVIEWS IN MEDICINAL CHEMISTRY

Harmine and Piperlongumine Revert TRIB2-Mediated Drug Resistance

(2020) Susana Machado et al.   Cancers

Targeting FLT3 mutations in AML: review of current knowledge and evidence

(2019) Naval Daver et al.   LEUKEMIA

A Review of Curcumin and Its Derivatives as Anticancer Agents

(2019) Mhd Tomeh et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Structure and Assembly of the Nuclear Pore Complex

(2019) Bernhard Hampoelz et al.   Annual Review of Biophysics

Biology and therapy of multiple myeloma

(2019) Douglas E Joshua et al.   MEDICAL JOURNAL OF AUSTRALIA

Structural prerequisites for CRM1-dependent nuclear export signaling peptides: accessibility, adapting conformation, and the stability at the binding site

(2019) Yoonji Lee et al.   Scientific Reports

Oral Selinexor–Dexamethasone for Triple-Class Refractory Multiple Myeloma

(2019) Ajai Chari et al.   NEW ENGLAND JOURNAL OF MEDICINE

Engineering chromosome region maintenance 1 fragments that bind to nuclear export signals

(2019) Yuqin Lei et al.   PROTEIN SCIENCE

Curcumin and Cancer

(2019) Giordano et al.   Nutrients

Sulforaphene induces apoptosis and inhibits the invasion of esophageal cancer cells through MSK2/CREB/Bcl-2 and cadherin pathway in vivo and in vitro

(2019) Chengjuan Zhang et al.   Cancer Cell International

FoxO-1 contributes to the efficacy of the combination of the XPO1 inhibitor selinexor and cisplatin in ovarian carcinoma preclinical models

(2018) Cristina Corno et al.   BIOCHEMICAL PHARMACOLOGY

SET1A-Mediated Mono-Methylation at K342 Regulates YAP Activation by Blocking Its Nuclear Export and Promotes Tumorigenesis

(2018) Lan Fang et al.   CANCER CELL

Traditional herbal medicine-derived sulforaphene promotes mitophagic cell death in lymphoma cells through CRM1-mediated p62/SQSTM1 accumulation and AMPK activation

(2018) Haina Wang et al.   CHEMICO-BIOLOGICAL INTERACTIONS

Plumbagin suppresses the human large cell lung cancer cell lines by inhibiting IL-6/STAT3 signaling in vitro

(2018) Tao Yu et al.   INTERNATIONAL IMMUNOPHARMACOLOGY

Selective Inhibition of Nuclear Export With Oral Selinexor for Treatment of Relapsed or Refractory Multiple Myeloma

(2018) Dan T. Vogl et al.   JOURNAL OF CLINICAL ONCOLOGY

A phase I study of selinexor in combination with high-dose cytarabine and mitoxantrone for remission induction in patients with acute myeloid leukemia

(2018) Amy Y. Wang et al.   Journal of Hematology & Oncology

Plumbagin inhibits the proliferation and survival of esophageal cancer cells by blocking STAT3-PLK1-AKT signaling

(2018) Ying-Ya Cao et al.   Cell Death & Disease

CRM1/XPO1 expression in pancreatic adenocarcinoma correlates with survivin expression and the proliferative activity

(2018) David M. Saulino et al.   Oncotarget

Decrease of 5-hydroxymethylcytosine and TET1 with nuclear exclusion of TET2 in small intestinal neuroendocrine tumors

(2018) Elham Barazeghi et al.   BMC CANCER

Anti-tumor efficacy of Selinexor (KPT-330) in gastric cancer is dependent on nuclear accumulation of p53 tumor suppressor

(2018) Vinod Vijay Subhash et al.   Scientific Reports

Plumbagin induces autophagy and apoptosis of SMMC‐7721 cells in vitro and in vivo

(2018) Yuning Lin et al.   JOURNAL OF CELLULAR BIOCHEMISTRY

Controlling the Gatekeeper: Therapeutic Targeting of Nuclear Transport

(2018) Friederike Kosyna et al.   Cells

FOXO transcription factors at the interface of metabolism and cancer

(2017) Wolfgang Link et al.   INTERNATIONAL JOURNAL OF CANCER

Anti-tumor activity of selective inhibitor of nuclear export (SINE) compounds, is enhanced in non-Hodgkin lymphoma through combination with mTOR inhibitor and dexamethasone

(2016) Irfana Muqbil et al.   CANCER LETTERS

The Second-Generation Exportin-1 Inhibitor KPT-8602 Demonstrates Potent Activity against Acute Lymphoblastic Leukemia

(2016) Thomas Vercruysse et al.   CLINICAL CANCER RESEARCH

Discovery and development of natural product oridonin-inspired anticancer agents

(2016) Ye Ding et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Phase I Study of Selinexor, a Selective Inhibitor of Nuclear Export, in Combination With Fludarabine and Cytarabine, in Pediatric Relapsed or Refractory Acute Leukemia

(2016) Thomas B. Alexander et al.   JOURNAL OF CLINICAL ONCOLOGY

CRM1/XPO1 is associated with clinical outcome in glioma and represents a therapeutic target by perturbing multiple core pathways

(2016) Xuejiao Liu et al.   Journal of Hematology & Oncology

Structural Biology and Regulation of Protein Import into the Nucleus

(2016) Mary Christie et al.   JOURNAL OF MOLECULAR BIOLOGY

KPT-8602, a second-generation inhibitor of XPO1-mediated nuclear export, is well tolerated and highly active against AML blasts and leukemia-initiating cells

(2016) J Etchin et al.   LEUKEMIA

Importins and exportins as therapeutic targets in cancer

(2016) Amit Mahipal et al.   PHARMACOLOGY & THERAPEUTICS

Piperlongumine induces gastric cancer cell apoptosis and G2/M cell cycle arrest both in vitro and in vivo

(2016) Chaoqin Duan et al.   TUMOR BIOLOGY

Mechanisms of Nuclear Export in Cancer and Resistance to Chemotherapy

(2016) Mohamed El-Tanani et al.   Cancers

Nuclear localization signals for four distinct karyopherin-β nuclear import systems

(2015) Michael Soniat et al.   BIOCHEMICAL JOURNAL

Origin and evolution of metabolic sub-cellular compartmentalization in eukaryotes

(2015) Toni Gabaldón et al.   BIOCHIMIE

KPT-330, a potent and selective exportin-1 (XPO-1) inhibitor, shows antitumor effects modulating the expression of cyclin D1 and survivin in prostate cancer models

(2015) Giovanni Luca Gravina et al.   BMC CANCER

Novel reversible selective inhibitor of nuclear export shows that CRM1 is a target in colorectal cancer cells

(2015) Mingshan Niu et al.   CANCER BIOLOGY & THERAPY

Piperlongumine is a novel nuclear export inhibitor with potent anticancer activity

(2015) Mingshan Niu et al.   CHEMICO-BIOLOGICAL INTERACTIONS

Promyelocytic leukemia zinc finger mediates glucocorticoid-induced cell cycle arrest in the chondroprogenitor cell line ATDC5

(2015) Masako Naito et al.   MOLECULAR AND CELLULAR ENDOCRINOLOGY

Expression, function, and targeting of the nuclear exporter chromosome region maintenance 1 (CRM1) protein

(2015) Jo Ishizawa et al.   PHARMACOLOGY & THERAPEUTICS

p27Kip1 and Ser10-phosphorylated p27Kip1 in breast cancer: clinical significance and expression

(2015) Xiaoxiang Guan et al.   OncoTargets and Therapy

Novel reversible selective inhibitor of CRM1 for targeted therapy in ovarian cancer

(2015) Xuejiao Liu et al.   Journal of Ovarian Research

Structural determinants of nuclear export signal orientation in binding to exportin CRM1

(2015) Ho Yee Joyce Fung et al.   eLife

RNA Export through the NPC in Eukaryotes

(2015) Masumi Okamura et al.   Genes

Structural Basis of Targeting the Exportin CRM1 in Cancer

(2015) Achim Dickmanns et al.   Cells

Targeting Oncogenic Mutant p53 for Cancer Therapy

(2015) Alejandro Parrales et al.   Frontiers in Oncology

Piperlongumine selectively kills cancer cells and increases cisplatin antitumor activity in head and neck cancer

(2015) Jong-Lyel Roh et al.   Oncotarget

KPT-330 has antitumour activity against non-small cell lung cancer

(2014) H Sun et al.   BRITISH JOURNAL OF CANCER

Allosteric control of the exportin CRM1 unraveled by crystal structure analysis

(2014) Thomas Monecke et al.   FEBS Journal

Role of Promyelocytic Leukemia Zinc Finger (PLZF) in Cell Proliferation and Cyclin-dependent Kinase Inhibitor 1A (p21WAF/CDKN1A) Gene Repression

(2014) Won-Il Choi et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Nuclear FAM21 participates in NF- B-dependent gene regulation in pancreatic cancer cells

(2014) Z.-H. Deng et al.   JOURNAL OF CELL SCIENCE

Selective inhibitors of nuclear export (SINE)– a novel class of anti-cancer agents

(2014) Kaushal Parikh et al.   Journal of Hematology & Oncology

CRM1 Is a Direct Cellular Target of the Natural Anti-cancer Agent Plumbagin

(2014) Xuejiao Liu et al.   JOURNAL OF PHARMACOLOGICAL SCIENCES

CBS9106-Induced CRM1 Degradation Is Mediated by Cullin Ring Ligase Activity and the Neddylation Pathway

(2014) N. Saito et al.   MOLECULAR CANCER THERAPEUTICS

XPO1 (CRM1) Inhibition Represses STAT3 Activation to Drive a Survivin-Dependent Oncogenic Switch in Triple-Negative Breast Cancer

(2014) Y. Cheng et al.   MOLECULAR CANCER THERAPEUTICS

Piperlongumine Induces Apoptosis and Synergizes with Cisplatin or Paclitaxel in Human Ovarian Cancer Cells

(2014) Li-Hua Gong et al.   Oxidative Medicine and Cellular Longevity

The evolving role of nuclear transporters in cancer

(2014) Asfar S. Azmi   SEMINARS IN CANCER BIOLOGY

Prognostic impact and targeting of CRM1 in acute myeloid leukemia

(2013) K. Kojima et al.   BLOOD

Knockdown of CRM1 inhibits the nuclear export of p27Kip1 phosphorylated at serine 10 and plays a role in the pathogenesis of epithelial ovarian cancer

(2013) You Wang et al.   CANCER LETTERS

Selective inhibitors of nuclear export for the treatment of non-Hodgkin's lymphomas

(2013) A. S. Azmi et al.   HAEMATOLOGICA

Genome-wide studies in multiple myeloma identify XPO1/CRM1 as a critical target validated using the selective nuclear export inhibitor KPT-276

(2013) J Schmidt et al.   LEUKEMIA

CRM1 inhibition induces tumor cell cytotoxicity and impairs osteoclastogenesis in multiple myeloma: molecular mechanisms and therapeutic implications

(2013) Y-T Tai et al.   LEUKEMIA

FOXOs: signalling integrators for homeostasis maintenance

(2013) Astrid Eijkelenboom et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Nuclear export inhibition through covalent conjugation and hydrolysis of Leptomycin B by CRM1

(2013) Qingxiang Sun et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structural Determinants and Mechanism of Mammalian CRM1 Allostery

(2013) Nicole Dölker et al.   STRUCTURE

Structure of a Truncation Mutant of the Nuclear Export Factor CRM1 Provides Insights into the Auto-Inhibitory Role of Its C-Terminal Helix

(2013) Cyril Dian et al.   STRUCTURE

CRM1 Is a Cellular Target of Curcumin: New Insights for the Myriad of Biological Effects of an Ancient Spice

(2013) Mingshan Niu et al.   TRAFFIC

Selective inhibitors of nuclear export show that CRM1/XPO1 is a target in chronic lymphocytic leukemia

(2012) R. Lapalombella et al.   BLOOD

Preclinical activity of a novel CRM1 inhibitor in acute myeloid leukemia

(2012) P. Ranganathan et al.   BLOOD

Oridonin: targeting programmed cell death pathways as an anti-tumour agent

(2012) Z. Liu et al.   CELL PROLIFERATION

Novel selective inhibitors of nuclear export CRM1 antagonists for therapy in mantle cell lymphoma

(2012) Kejie Zhang et al.   EXPERIMENTAL HEMATOLOGY

Rare germline mutations inPALB2and breast cancer risk: A population-based study

(2012) Marc Tischkowitz et al.   HUMAN MUTATION

Consensus Induced Fit Docking (cIFD): methodology, validation, and application to the discovery of novel Crm1 inhibitors

(2012) Ori Kalid et al.   JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN

A 2.1-Å-Resolution Crystal Structure of Unliganded CRM1 Reveals the Mechanism of Autoinhibition

(2012) Natsumi Saito et al.   JOURNAL OF MOLECULAR BIOLOGY

Antileukemic activity of nuclear export inhibitors that spare normal hematopoietic cells

(2012) J Etchin et al.   LEUKEMIA

Survivin Signaling in Clinical Oncology: A Multifaceted Dragon

(2012) Jagat R. Kanwar et al.   MEDICINAL RESEARCH REVIEWS

Sequence and structural analyses of nuclear export signals in the NESdb database

(2012) Darui Xu et al.   MOLECULAR BIOLOGY OF THE CELL

ValidNESs: a database of validated leucine-rich nuclear export signals

(2012) Szu-Chin Fu et al.   NUCLEIC ACIDS RESEARCH

Nuclear export of proteins and drug resistance in cancer

(2011) Joel G. Turner et al.   BIOCHEMICAL PHARMACOLOGY

FoxO transcription factors; Regulation by AKT and 14-3-3 proteins

(2011) Guri Tzivion et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

CBS9106 is a novel reversible oral CRM1 inhibitor with CRM1 degrading activity

(2011) K. Sakakibara et al.   BLOOD

Identification of Molecular Vulnerabilities in Human Multiple Myeloma Cells by RNA Interference Lethality Screening of the Druggable Genome

(2011) R. E. Tiedemann et al.   CANCER RESEARCH

Hallmarks of Cancer: The Next Generation

(2011) Douglas Hanahan et al.   CELL

Controlling Protein Transport by Small Molecules

(2011) Karl Gademann   CURRENT DRUG TARGETS

p53: Guardian of ploidy

(2011) Yael Aylon et al.   Molecular Oncology

The cytotoxic styryl lactone goniothalamin is an inhibitor of nucleocytoplasmic transport

(2010) Jean-Yves Wach et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

p27: A Barometer of Signaling Deregulation and Potential Predictor of Response to Targeted Therapies

(2010) S. A. Wander et al.   CLINICAL CANCER RESEARCH

A CRM1-dependent nuclear export pathway is involved in the regulation of MutLα subcellular localization

(2010) Angela Brieger et al.   GENES CHROMOSOMES & CANCER

Cytoplasmic p21 expression levels determine cisplatin resistance in human testicular cancer

(2010) Roelof Koster et al.   JOURNAL OF CLINICAL INVESTIGATION

Anguinomycins and Derivatives: Total Syntheses, Modeling, and Biological Evaluation of the Inhibition of Nucleocytoplasmic Transport

(2010) Simone Bonazzi et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Nucleo-Cytoplasmic Localization Domains Regulate Krüppel-Like Factor 6 (KLF6) Protein Stability and Tumor Suppressor Function

(2010) Estefanía Rodríguez et al.   PLoS One

Human Multiple Myeloma Cells Are Sensitized to Topoisomerase II Inhibitors by CRM1 Inhibition

(2009) J. G. Turner et al.   CANCER RESEARCH

Identification of Nuclear Export Inhibitors with Potent Anticancer Activity In vivo

(2009) S. C. Mutka et al.   CANCER RESEARCH

Structural biology of the p53 tumour suppressor

(2009) Andrei L Okorokov et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

Nuclear-Cytoplasmic Shuttling of Menin Regulates Nuclear Translocation of  -Catenin

(2009) Y. Cao et al.   MOLECULAR AND CELLULAR BIOLOGY

Structural basis for leucine-rich nuclear export signal recognition by CRM1

(2009) Xiuhua Dong et al.   NATURE

Structural basis for assembly and disassembly of the CRM1 nuclear export complex

(2009) Xiuhua Dong et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

EXPRESSION OF CRM1 IN HUMAN GLIOMAS AND ITS SIGNIFICANCE IN P27 EXPRESSION AND CLINICAL PROGNOSIS

(2009) Aiguo Shen et al.   NEUROSURGERY

Darwinian evolution in the light of genomics

(2009) E. V. Koonin   NUCLEIC ACIDS RESEARCH

Crystal Structure of the Nuclear Export Receptor CRM1 in Complex with Snurportin1 and RanGTP

(2009) T. Monecke et al.   SCIENCE

Exomic Sequencing Identifies PALB2 as a Pancreatic Cancer Susceptibility Gene

(2009) S. Jones et al.   SCIENCE

TP53 Mutations in Human Cancers: Origins, Consequences, and Clinical Use

(2009) M. Olivier et al.   Cold Spring Harbor Perspectives in Biology

Structural Biology of the Tumor Suppressor p53

(2008) Andreas C. Joerger et al.   Annual Review of Biochemistry

The Karyopherin proteins, Crm1 and Karyopherin β1, are overexpressed in cervical cancer and are critical for cancer cell survival and proliferation

(2008) Pauline J. van der Watt et al.   INTERNATIONAL JOURNAL OF CANCER

Inhibition of Thr-55 phosphorylation restores p53 nuclear localization and sensitizes cancer cells to DNA damage

(2008) X. Cai et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA