Recent findings and future directions for interpolar mitotic kinesin inhibitors in cancer therapy

Structural Basis of New Allosteric Inhibition in Kinesin Spindle Protein Eg5

(2015) Hideshi Yokoyama et al.   ACS Chemical Biology

Hitting the brakes: targeting microtubule motors in cancer

(2015) Gayathri Chandrasekaran et al.   BRITISH JOURNAL OF CANCER

KIFC1 is a novel potential therapeutic target for breast cancer

(2015) Yonghe Li et al.   CANCER BIOLOGY & THERAPY

Paradox-Breaking RAF Inhibitors that Also Target SRC Are Effective in Drug-Resistant BRAF Mutant Melanoma

(2015) Maria Romina Girotti et al.   CANCER CELL

Pgp efflux pump decreases the cytostatic effect of CENP-E inhibitor GSK923295

(2015) Sergey O. Tcherniuk et al.   CANCER LETTERS

Eribulin Mesylate: Mechanism of Action of a Unique Microtubule-Targeting Agent

(2015) N. F. Dybdal-Hargreaves et al.   CLINICAL CANCER RESEARCH

First-in-human phase 1 study of filanesib (ARRY-520), a kinesin spindle protein inhibitor, in patients with advanced solid tumors

(2015) Patricia M. LoRusso et al.   INVESTIGATIONAL NEW DRUGS

Structure-Guided Design of Novel l-Cysteine Derivatives as Potent KSP Inhibitors

(2015) Naohisa Ogo et al.   ACS Medicinal Chemistry Letters

HSET overexpression fuels tumor progression via centrosome clustering-independent mechanisms in breast cancer patients

(2015) Vaishali Pannu et al.   Oncotarget

A phase 1 and dose-finding study of LY2523355 (litronesib), an Eg5 inhibitor, in Japanese patients with advanced solid tumors

(2014) Hiroshi Wakui et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Mitotic Kinesins: A Reason to Delve into Kinesin-12

(2014) William O. Hancock   CURRENT BIOLOGY

Discovery of Potent KIFC1 Inhibitors Using a Method of Integrated High-Throughput Synthesis and Screening

(2014) Bin Yang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synergism between inhibitors of Aurora A and KIF11 overcomes KIF15-dependent drug resistance

(2014) Hoi Tang Ma et al.   Molecular Oncology

Prime movers: the mechanochemistry of mitotic kinesins

(2014) Robert A. Cross et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Kinesin Spindle Protein Inhibitors with Diaryl Amine Scaffolds: Crystal Packing Analysis for Improved Aqueous Solubility

(2014) Tomoki Takeuchi et al.   ACS Medicinal Chemistry Letters

KIFCI, a novel putative prognostic biomarker for ovarian adenocarcinomas: delineating protein interaction networks and signaling circuitries

(2014) Shrikant Pawar et al.   Journal of Ovarian Research

Discovery and Mechanistic Study of a Small Molecule Inhibitor for Motor Protein KIFC1

(2013) Jiaquan Wu et al.   ACS Chemical Biology

STLC-resistant cell lines as tools to classify chemically divergent Eg5 targeting agents according to their mode of action and target specificity

(2013) Rose-Laure Indorato et al.   BIOCHEMICAL PHARMACOLOGY

"A fortuitous combination of circumstances"

(2013) S. Lonial   BLOOD

Design, Synthesis, and Biological Evaluation of an Allosteric Inhibitor of HSET that Targets Cancer Cells with Supernumerary Centrosomes

(2013) Ciorsdaidh A. Watts et al.   CHEMISTRY & BIOLOGY

Genome-based cancer therapeutics: targets, kinase drug resistance and future strategies for precision oncology

(2013) Paul Workman et al.   CURRENT OPINION IN PHARMACOLOGY

Advances in the discovery of kinesin spindle protein (Eg5) inhibitors as antitumor agents

(2013) Hala Bakr El-Nassan   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Kinesin-5: Cross-bridging mechanism to targeted clinical therapy

(2013) Edward J. Wojcik et al.   GENE

A phase I, dose-escalation study of the Eg5-inhibitor EMD 534085 in patients with advanced solid tumors or lymphoma

(2013) A. Hollebecque et al.   INVESTIGATIONAL NEW DRUGS

Resistance by Allostery: A Novel Perspective for Eg5-Targeted Drug Design

(2013) Ambily Nath Indu Viswanath et al.   JOURNAL OF MEDICINAL CHEMISTRY

Mitotic Kinesin Eg5 Overcomes Inhibition to the Phase I/II Clinical Candidate SB743921 by an Allosteric Resistance Mechanism

(2013) Sandeep K. Talapatra et al.   JOURNAL OF MEDICINAL CHEMISTRY

Optimized S-Trityl-l-cysteine-Based Inhibitors of Kinesin Spindle Protein with Potent in Vivo Antitumor Activity in Lung Cancer Xenograft Models

(2013) James A. D. Good et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structural Insights into a Unique Inhibitor Binding Pocket in Kinesin Spindle Protein

(2013) Venkatasubramanian Ulaganathan et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Adenosine Triphosphate Hydrolysis Mechanism in Kinesin Studied by Combined Quantum-Mechanical/Molecular-Mechanical Metadynamics Simulations

(2013) Matthew J. McGrath et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

The expression of Eg5 predicts a poor outcome for patients with renal cell carcinoma

(2013) Dingqi Sun et al.   MEDICAL ONCOLOGY

Calculated treatment

(2013) Natalia L. Komarova et al.   NATURE

Mapping the Structural and Dynamical Features of Kinesin Motor Domains

(2013) Guido Scarabelli et al.   PLoS Computational Biology

The crystal structure and biochemical characterization of Kif15: a bifunctional molecular motor involved in bipolar spindle formation and neuronal development

(2013) Marta Klejnot et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

The structure of the ternary Eg5–ADP–ispinesib complex

(2012) S. K. Talapatra et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Discovery of Allosteric Inhibitors of Kinesin Spindle Protein (KSP) for the Treatment of Taxane-Refractory Cancer: MK-0731 and Analogs

(2012) Christopher D. Cox et al.   Anti-Cancer Agents in Medicinal Chemistry

Let's huddle to prevent a muddle: centrosome declustering as an attractive anticancer strategy

(2012) A Ogden et al.   CELL DEATH AND DIFFERENTIATION

Inhibitors Targeting Mitosis: Tales of How Great Drugs against a Promising Target Were Brought Down by a Flawed Rationale

(2012) E. Komlodi-Pasztor et al.   CLINICAL CANCER RESEARCH

Mitotic Spindle Form and Function

(2012) M. Winey et al.   GENETICS

Acentrosomal spindle organization renders cancer cells dependent on the kinesin HSET

(2012) Julia Kleylein-Sohn et al.   JOURNAL OF CELL SCIENCE

Kinesin spindle protein SiRNA slows tumor progression

(2012) Emanuele Marra et al.   JOURNAL OF CELLULAR PHYSIOLOGY

Triphenylbutanamines: Kinesin Spindle Protein Inhibitors with in Vivo Antitumor Activity

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

The Loop 5 Element Structurally and Kinetically Coordinates Dimers of the Human Kinesin-5, Eg5

(2011) Joshua S. Waitzman et al.   BIOPHYSICAL JOURNAL

Preferential killing of tetraploid tumor cells by targeting the mitotic kinesin Eg5

(2011) Santiago Rello-Varona et al.   CELL CYCLE

Overexpression of Eg5 predicts unfavorable prognosis in non-muscle invasive bladder urothelial carcinoma

(2011) Sentai Ding et al.   INTERNATIONAL JOURNAL OF UROLOGY

Structure–Activity Relationships of Carboline and Carbazole Derivatives as a Novel Class of ATP-Competitive Kinesin Spindle Protein Inhibitors

(2011) Tomoki Takeuchi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of (+)-N-(3-Aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-[1,2]thiazolo[5,4-d]pyrimidin-6-yl)-2-methylpropyl]-4-methylbenzamide (AZD4877), a Kinesin Spindle Protein Inhibitor and Potential Anticancer Agent

(2011) Maria-Elena Theoclitou et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure−Activity Relationship and Multidrug Resistance Study of NewS-trityl-l-Cysteine Derivatives As Inhibitors of Eg5

(2011) Hung Yi Kristal Kaan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Analysis of the interaction of the Eg5 Loop5 with the nucleotide site

(2011) Timothy D. Harrington et al.   JOURNAL OF THEORETICAL BIOLOGY

A novel Aurora kinase A inhibitor MK-8745 predicts TPX2 as a therapeutic biomarker in non-Hodgkin lymphoma cell lines

(2011) Aparajita Chowdhury et al.   LEUKEMIA & LYMPHOMA

Spindle Poisons and Cell Fate: A Tale of Two Pathways

(2011) D. R. Matson et al.   MOLECULAR INTERVENTIONS

Mitosis is not a key target of microtubule agents in patient tumors

(2011) Edina Komlodi-Pasztor et al.   Nature Reviews Clinical Oncology

Elucidating the functionality of kinesins: An overview of small molecule inhibitors

(2011) James A.D. Good et al.   SEMINARS IN CELL & DEVELOPMENTAL BIOLOGY

Novel Benzimidazole Inhibitors Bind to a Unique Site in the Kinesin Spindle Protein Motor Domain

(2010) Payal R. Sheth et al.   BIOCHEMISTRY

The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5

(2010) Kai Schiemann et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Proper Organization of Microtubule Minus Ends Is Needed for Midzone Stability and Cytokinesis

(2010) Shang Cai et al.   CURRENT BIOLOGY

Structural Basis for Inhibition of Eg5 by Dihydropyrimidines: Stereoselectivity of Antimitotic Inhibitors Enastron, Dimethylenastron and Fluorastrol

(2010) Hung Yi Kristal Kaan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Ectopic expression of the microtubule-dependent motor protein Eg5 promotes pancreatic tumourigenesis

(2010) Min Liu et al.   JOURNAL OF PATHOLOGY

RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF

(2010) Poulikos I. Poulikakos et al.   NATURE

RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth

(2010) Georgia Hatzivassiliou et al.   NATURE

Antitumor activity of an allosteric inhibitor of centromere-associated protein-E

(2010) K. W. Wood et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

How kinesin motor proteins drive mitotic spindle function: Lessons from molecular assays

(2010) Linda Wordeman   SEMINARS IN CELL & DEVELOPMENTAL BIOLOGY

Predicting Important Residues and Interaction Pathways in Proteins Using Gaussian Network Model: Binding and Stability of HLA Proteins

(2010) Turkan Haliloglu et al.   PLoS Computational Biology

An allosteric transition trapped in an intermediate state of a new kinesin–inhibitor complex

(2009) Hung Yi Kristal Kaan et al.   BIOCHEMICAL JOURNAL

Mutations in the human kinesin Eg5 that confer resistance to monastrol and S-trityl- l -cysteine in tumor derived cell lines

(2009) Sergey Tcherniuk et al.   BIOCHEMICAL PHARMACOLOGY

Thermodynamics of Nucleotide and Inhibitor Binding to Wild-Type and Ispinesib-Resistant Forms of Human Kinesin Spindle Protein

(2009) Payal R. Sheth et al.   BIOCHEMISTRY

Bis(hetero)aryl derivatives as unique kinesin spindle protein inhibitors

(2009) Kenji Matsuno et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Substituted benzimidazoles: A novel chemotype for small molecule hKSP inhibitors

(2009) Brian R. Lahue et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The discovery of tetrahydro-β-carbolines as inhibitors of the kinesin Eg5

(2009) Paul A. Barsanti et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The Expression of Three Genes in Primary Non-Small Cell Lung Cancer Is Associated with Metastatic Spread to the Brain

(2009) H. Grinberg-Rashi et al.   CLINICAL CANCER RESEARCH

Kif15 Cooperates with Eg5 to Promote Bipolar Spindle Assembly

(2009) Marvin E. Tanenbaum et al.   CURRENT BIOLOGY

The Role of Hklp2 in the Stabilization and Maintenance of Spindle Bipolarity

(2009) David Vanneste et al.   CURRENT BIOLOGY

Structures of kinesin motor proteins

(2009) Alexander Marx et al.   CELL MOTILITY AND THE CYTOSKELETON

Crystal structure of HsEg5 in complex with clinical candidate CK0238273 provides insight into inhibitory mechanism, potency, and specificity

(2008) Bin Zhang et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Targeting the Kinesin Spindle Protein: Basic Principles and Clinical Implications

(2008) V. Sarli et al.   CLINICAL CANCER RESEARCH

Mechanisms to suppress multipolar divisions in cancer cells with extra centrosomes

(2008) M. Kwon et al.   GENES & DEVELOPMENT

Kinesin Spindle Protein (KSP) Inhibitors. 9. Discovery of (2S)-4-(2,5-Difluorophenyl)-N-[(3R,4S)-3-fluoro-1-methylpiperidin-4-yl]-2-(hydroxymethyl)-N-methyl-2-phenyl-2,5-dihydro-1H-pyrrole-1-carboxamide (MK-0731) for the Treatment of Taxane-Refractory Cancer

(2008) Christopher D. Cox et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure–Activity Relationship ofS-Trityl-l-Cysteine Analogues as Inhibitors of the Human Mitotic Kinesin Eg5

(2008) Salvatore DeBonis et al.   JOURNAL OF MEDICINAL CHEMISTRY

Kinesin-14 Family Proteins HSET/XCTK2 Control Spindle Length by Cross-Linking and Sliding Microtubules

(2008) Shang Cai et al.   MOLECULAR BIOLOGY OF THE CELL

Effects of Eg5 knockdown on human prostate cancer xenograft growth and chemosensitivity

(2008) Norihiro Hayashi et al.   PROSTATE