Inhibition of XPO-1 Mediated Nuclear Export through the Michael-Acceptor Character of Chalcones

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

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

Design, synthesis, and antibacterial evaluation of PFK-158 derivatives as potent agents against drug-resistant bacteria

(2021) Wei Wang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Characterization of Inhibition Reveals Distinctive Properties for Human and Saccharomyces cerevisiae CRM1

(2020) Alaa Shaikhqasem et al.   JOURNAL OF MEDICINAL CHEMISTRY

Noncanonical Cation−π Cyclizations of Alkylidene β-Ketoesters: Synthesis of Spiro-fused and Bridged Bicyclic Ring Systems

(2019) Dylan E. Parsons et al.   ORGANIC LETTERS

Inhibitors of nuclear transport

(2019) David A Jans et al.   CURRENT OPINION IN CELL BIOLOGY

Karyopherins in cancer

(2018) Tolga Çağatay et al.   CURRENT OPINION IN CELL BIOLOGY

Verdinexor Targeting of CRM1 is a Promising Therapeutic Approach against RSV and Influenza Viruses

(2018) et al.   Viruses-Basel

Nuclear Export Inhibition for Pancreatic Cancer Therapy

(2018) Irfana Muqbil et al.   Cancers

Controlling the Gatekeeper: Therapeutic Targeting of Nuclear Transport

(2018) Friederike Kosyna et al.   Cells

Glutathione Adduct Patterns of Michael-Acceptor Carbonyls

(2017) Christian Slawik et al.   ENVIRONMENTAL SCIENCE & TECHNOLOGY

XPO1 in B cell hematological malignancies: from recurrent somatic mutations to targeted therapy

(2017) Vincent Camus et al.   Journal of Hematology & Oncology

CRM1 Inhibitors for Antiviral Therapy

(2017) Cynthia Mathew et al.   Frontiers in Microbiology

Substrate-controlled switchable asymmetric annulations to access polyheterocyclic skeletons

(2016) Kai-Kai Wang et al.   CHEMICAL COMMUNICATIONS

Stereoselective Ketone Rearrangements with Hypervalent Iodine Reagents

(2016) Florence Malmedy et al.   CHEMISTRY-A EUROPEAN JOURNAL

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

(2016) Thomas Vercruysse et al.   CLINICAL CANCER RESEARCH

Next-generation XPO1 inhibitor shows improved efficacy and in vivo tolerability in hematological malignancies

(2016) Z A Hing et al.   LEUKEMIA

Targeting the Nuclear Import Receptor Kpn 1 as an Anticancer Therapeutic

(2016) P. J. van der Watt et al.   MOLECULAR CANCER THERAPEUTICS

Identifying Drug-Target Selectivity of Small-Molecule CRM1/XPO1 Inhibitors by CRISPR/Cas9 Genome Editing

(2015) Jasper E. Neggers et al.   CHEMISTRY & BIOLOGY

Systematic Study of the Glutathione (GSH) Reactivity of N-Arylacrylamides: 1. Effects of Aryl Substitution

(2015) Victor J. Cee et al.   JOURNAL OF MEDICINAL CHEMISTRY

Prolonged and tunable residence time using reversible covalent kinase inhibitors

(2015) J Michael Bradshaw et al.   Nature Chemical Biology

Geminal Dichlorination of Phenyliodonium Ylides of β-Dicarbonyl Compounds through Double Ligand Transfer from (Dichloroiodo)benzene

(2015) Graham Murphy et al.   SYNTHESIS-STUTTGART

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

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

Structural Basis of Targeting the Exportin CRM1 in Cancer

(2015) Achim Dickmanns et al.   Cells

Induction of p53-mediated transcription and apoptosis by exportin-1 (XPO1) inhibition in mantle cell lymphoma

(2014) Mariko Yoshimura et al.   CANCER SCIENCE

Structure-Based Virtual Screening Approach for Discovery of Covalently Bound Ligands

(2014) Dora Toledo Warshaviak et al.   Journal of Chemical Information and Modeling

Docking Covalent Inhibitors: A Parameter Free Approach To Pose Prediction and Scoring

(2014) Kai Zhu et al.   Journal of Chemical Information and Modeling

Opening or Closing the Lock? When Reactivity Is the Key to Biological Activity

(2013) Nafisah Al-Rifai et al.   CHEMISTRY-A EUROPEAN JOURNAL

Synthesis and biological effects of novel 2-amino-3-(4-chlorobenzoyl)-4-substituted thiophenes as allosteric enhancers of the A1 adenosine receptor

(2013) Romeo Romagnoli et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

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

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

(2012) R. Lapalombella et al.   BLOOD

Antileukemic activity of nuclear export inhibitors that spare normal hematopoietic cells

(2012) J Etchin et al.   LEUKEMIA

Development of a Method for the Preparation of Ruthenium Indenylidene-Ether Olefin Metathesis Catalysts

(2012) Leonel R. Jimenez et al.   MOLECULES

Reactivity assessment of chalcones by a kinetic thiol assay

(2012) Sabine Amslinger et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

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

(2011) K. Sakakibara et al.   BLOOD

Kinetic Glutathione Chemoassay To Quantify Thiol Reactivity of Organic ElectrophilesApplication to α,β-Unsaturated Ketones, Acrylates, and Propiolates

(2009) Alexander Böhme et al.   CHEMICAL RESEARCH IN TOXICOLOGY

Structure-Based Design, Synthesis, and Biological Evaluation of a Series of Novel and Reversible Inhibitors for the Severe Acute Respiratory Syndrome−Coronavirus Papain-Like Protease

(2009) Arun K. Ghosh et al.   JOURNAL OF MEDICINAL CHEMISTRY

Inhibition of the CRM1-mediated nucleocytoplasmic transport by N-azolylacrylates: Structure–activity relationship and mechanism of action

(2008) Tine Van Neck et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Structure-activity relationships for hepatocyte toxicity and electrophilic reactivity ofα,β-unsaturated esters, acrylates and methacrylates

(2008) Katie Chan et al.   JOURNAL OF APPLIED TOXICOLOGY