Structure-Bioactivity Relationship for Benzimidazole Thiophene Inhibitors of Polo-Like Kinase 1 (PLK1), a Potential Drug Target in Schistosoma mansoni

Synthesis of a Sugar-Based Thiosemicarbazone Series and Structure-Activity Relationship versus the Parasite Cysteine Proteases Rhodesain, Cruzain, and Schistosoma mansoni Cathepsin B1

(2015) Nayara Cristina Fonseca et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Polo-Like Kinase 1 as a Potential Therapeutic Target for Osteosarcoma

(2015) Li Cheng et al.   CURRENT PHARMACEUTICAL DESIGN

Schistosomiasis and its treatment

(2015) Conor R Caffrey   Future Medicinal Chemistry

Anthelmintic Drug Discovery: Into the Future

(2015) Timothy G. Geary et al.   JOURNAL OF PARASITOLOGY

Natural Products as Leads in Schistosome Drug Discovery

(2015) Bruno Neves et al.   MOLECULES

Anti-Schistosomal Activity of Cinnamic Acid Esters: Eugenyl and Thymyl Cinnamate Induce Cytoplasmic Vacuoles and Death in Schistosomula of Schistosoma mansoni

(2015) Jan Glaser et al.   MOLECULES

Application of RNAi to Genomic Drug Target Validation in Schistosomes

(2015) Alessandra Guidi et al.   PLoS Neglected Tropical Diseases

The QDREC web server: determining dose–response characteristics of complex macroparasites in phenotypic drug screens

(2014) Daniel Asarnow et al.   BIOINFORMATICS

Current assessment of polo-like kinases as anti-tumor drug targets

(2014) Sandra N Craig et al.   Expert Opinion on Drug Discovery

Thoughts on the current assessment of Polo-like kinase inhibitor drug discovery

(2014) Klaus Strebhardt et al.   Expert Opinion on Drug Discovery

Volasertib for the treatment of acute myeloid leukemia: a review of preclinical and clinical development

(2014) Melanie Janning et al.   Future Oncology

The little we know about the pharmacokinetics and pharmacodynamics of praziquantel (racemate and R-enantiomer)

(2014) P. Olliaro et al.   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

Discovery and development of the Polo-like kinase inhibitor volasertib in cancer therapy

(2014) B T Gjertsen et al.   LEUKEMIA

Schistosomiasis control: praziquantel forever?

(2014) Donato Cioli et al.   MOLECULAR AND BIOCHEMICAL PARASITOLOGY

The discovery of first-in-class drugs: origins and evolution

(2014) Jörg Eder et al.   NATURE REVIEWS DRUG DISCOVERY

Polo-like kinases: structural variations lead to multiple functions

(2014) Sihem Zitouni et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Chemical and Genetic Validation of the Statin Drug Target to Treat the Helminth Disease, Schistosomiasis

(2014) Liliana Rojo-Arreola et al.   PLoS One

Repurposing human Aurora kinase inhibitors as leads for anti-protozoan drug discovery

(2014) Gautam Patel et al.   MedChemComm

Orally Active Antischistosomal Early Leads Identified from the Open Access Malaria Box

(2014) Katrin Ingram-Sieber et al.   PLoS Neglected Tropical Diseases

Serum albumin and α-1 acid glycoprotein impede the killing of Schistosoma mansoni by the tyrosine kinase inhibitor Imatinib

(2014) Svenja Beckmann et al.   International Journal for Parasitology-Drugs and Drug Resistance

Compound library screening identified Akt/PKB kinase pathway inhibitors as potential key molecules for the development of new chemotherapeutics against schistosomiasis

(2014) Marion Morel et al.   International Journal for Parasitology-Drugs and Drug Resistance

Schistosomiasis Chemotherapy

(2013) Sophie A.-L. Thétiot-Laurent et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Segmenting the Etiological Agent of Schistosomiasis for High-Content Screening

(2013) D. E. Asarnow et al.   IEEE TRANSACTIONS ON MEDICAL IMAGING

Genetic and Molecular Basis of Drug Resistance and Species-Specific Drug Action in Schistosome Parasites

(2013) C. L. L. Valentim et al.   SCIENCE

Polo-Like Kinases Inhibitors

(2012) L. Garuti et al.   CURRENT MEDICINAL CHEMISTRY

Modern Phenotypic Drug Discovery Is a Viable, Neoclassic Pharma Strategy

(2012) Jonathan A. Lee et al.   JOURNAL OF MEDICINAL CHEMISTRY

Susceptibility or resistance of praziquantel in human schistosomiasis: a review

(2012) Wei Wang et al.   PARASITOLOGY RESEARCH

SmSak, the Second Polo-Like Kinase of the Helminth Parasite Schistosoma mansoni: Conserved and Unexpected Roles in Meiosis

(2012) Thavy Long et al.   PLoS One

Whole Organism High-Content Screening by Label-Free, Image-Based Bayesian Classification for Parasitic Diseases

(2012) Ross A. Paveley et al.   PLoS Neglected Tropical Diseases

Polo-Box Domain Inhibitor Poloxin Activates the Spindle Assembly Checkpoint and Inhibits Tumor Growth in Vivo

(2011) Juping Yuan et al.   AMERICAN JOURNAL OF PATHOLOGY

Schistosoma mansoni polo-like kinases and their function in control of mitosis and parasite reproduction

(2011) Colette Dissous et al.   ANAIS DA ACADEMIA BRASILEIRA DE CIENCIAS

Eukaryotic Protein Kinases (ePKs) of the Helminth Parasite Schistosoma mansoni

(2011) Luiza F Andrade et al.   BMC GENOMICS

From Plk1 to Plk5

(2011) Guillermo de Cárcer et al.   CELL CYCLE

Phase I Study of GSK461364, a Specific and Competitive Polo-like Kinase 1 Inhibitor, in Patients with Advanced Solid Malignancies

(2011) D. Olmos et al.   CLINICAL CANCER RESEARCH

Schistosomiasis

(2011) Conor R. Caffrey et al.   CURRENT OPINION IN INFECTIOUS DISEASES

How were new medicines discovered?

(2011) David C. Swinney et al.   NATURE REVIEWS DRUG DISCOVERY

Heteroaryl-linked 5-(1H-benzimidazol-1-yl)-2-thiophenecarboxamides: Potent inhibitors of polo-like kinase 1 (PLK1) with improved drug-like properties

(2010) Tara R. Rheault et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Praziquantel and Schistosomiasis

(2010) Alexander Dömling et al.   ChemMedChem

Schistosoma mansoni Polo-like kinase 1: A mitotic kinase with key functions in parasite reproduction☆

(2010) Thavy Long et al.   INTERNATIONAL JOURNAL FOR PARASITOLOGY

Sensitivity of Cancer Cells to Plk1 Inhibitor GSK461364A Is Associated with Loss of p53 Function and Chromosome Instability

(2010) Y. Degenhardt et al.   MOLECULAR CANCER THERAPEUTICS

Multifaceted polo-like kinases: drug targets and antitargets for cancer therapy

(2010) Klaus Strebhardt   NATURE REVIEWS DRUG DISCOVERY

RNA Interference in Schistosoma mansoni Schistosomula: Selectivity, Sensitivity and Operation for Larger-Scale Screening

(2010) Saša Štefanić et al.   PLoS Neglected Tropical Diseases

Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding

(2009) Kyle A. Emmitte et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Distinct Concentration-Dependent Effects of the Polo-like Kinase 1-Specific Inhibitor GSK461364A, Including Differential Effect on Apoptosis

(2009) A. G. Gilmartin et al.   CANCER RESEARCH

A Pan-Specific Inhibitor of the Polo-Box Domains of Polo-like Kinases Arrests Cancer Cells in Mitosis

(2009) Wolfgang Reindl et al.   CHEMBIOCHEM

BI 6727, A Polo-like Kinase Inhibitor with Improved Pharmacokinetic Profile and Broad Antitumor Activity

(2009) D. Rudolph et al.   CLINICAL CANCER RESEARCH

Polo-like kinases: conservation and divergence in their functions and regulation

(2009) Vincent Archambault et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Experimentally promising antischistosomal drugs: a review of some drug candidates not reaching the clinical use

(2009) Rashad A. Abdul-Ghani et al.   PARASITOLOGY RESEARCH

A Schistosome cAMP-Dependent Protein Kinase Catalytic Subunit Is Essential for Parasite Viability

(2009) Brett E. Swierczewski et al.   PLoS Neglected Tropical Diseases

SmCL3, a Gastrodermal Cysteine Protease of the Human Blood Fluke Schistosoma mansoni

(2009) Jan Dvořák et al.   PLoS Neglected Tropical Diseases

Drug Discovery for Schistosomiasis: Hit and Lead Compounds Identified in a Library of Known Drugs by Medium-Throughput Phenotypic Screening

(2009) Maha-Hamadien Abdulla et al.   PLoS Neglected Tropical Diseases

Taste, A New Incentive to Switch to (R)-Praziquantel in Schistosomiasis Treatment

(2009) Thorsten Meyer et al.   PLoS Neglected Tropical Diseases

Discovery of thiophene inhibitors of polo-like kinase

(2008) Kyle A. Emmitte et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Inhibition of Polo-like Kinase 1 by Blocking Polo-Box Domain-Dependent Protein-Protein Interactions

(2008) Wolfgang Reindl et al.   CHEMISTRY & BIOLOGY

Praziquantel: mechanisms of action, resistance and new derivatives for schistosomiasis

(2008) Michael J Doenhoff et al.   CURRENT OPINION IN INFECTIOUS DISEASES

Towards an understanding of the mechanism of action of praziquantel

(2008) Anthony D. Aragon et al.   MOLECULAR AND BIOCHEMICAL PARASITOLOGY

Yeast Polo-like kinase substrates are nailed with the right tools

(2008) Vincent Archambault et al.   GENOME BIOLOGY