(Q28552326)

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

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

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infectious disease

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Schistosoma mansoni

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Colette Dissous

7

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9

object named as

David H Drewry

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James H McKerrow

8

object named as

James H McKerrow

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author name string

Thavy Long

1

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R Jeffrey Neitz

2

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Rachel Beasley

3

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Chakrapani Kalyanaraman

4

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Brian M Suzuki

5

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Matthew P Jacobson

6

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William J Zuercher

10

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Rahul Singh

11

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Conor R Caffrey

12

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language of work or name

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publication date

January 2016

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PLoS Neglected Tropical Diseases

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10

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1

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e0004356

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copyright license

Creative Commons Attribution 4.0 International

11 January 2016

1 reference

April 2022 Public Data File from Crossref

copyright status

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Application of RNAi to Genomic Drug Target Validation in Schistosomes

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

19 March 2017

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

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

19 March 2017

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

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

19 March 2017

Chemical and genetic validation of the statin drug target to treat the helminth disease, schistosomiasis

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

19 March 2017

Orally active antischistosomal early leads identified from the open access malaria box

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

19 March 2017

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

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

19 March 2017

Whole organism high-content screening by label-free, image-based Bayesian classification for parasitic diseases

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

19 March 2017

RNA interference in Schistosoma mansoni schistosomula: selectivity, sensitivity and operation for larger-scale screening

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

19 March 2017

A schistosome cAMP-dependent protein kinase catalytic subunit is essential for parasite viability

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

19 March 2017

Drug discovery for schistosomiasis: hit and lead compounds identified in a library of known drugs by medium-throughput phenotypic screening

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

19 March 2017

SmCL3, a gastrodermal cysteine protease of the human blood fluke Schistosoma mansoni

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

19 March 2017

BI 6727, a Polo-like kinase inhibitor with improved pharmacokinetic profile and broad antitumor activity

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

19 March 2017

Taste, a new incentive to switch to (R)-praziquantel in schistosomiasis treatment

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

19 March 2017

Thioredoxin glutathione reductase from Schistosoma mansoni: an essential parasite enzyme and a key drug target

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

19 March 2017

Schistosomiasis mansoni: novel chemotherapy using a cysteine protease inhibitor

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

19 March 2017

Analysis of Relative Gene Expression Data Using Real-Time Quantitative PCR and the 2−ΔΔCT Method

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

19 March 2017

How were new medicines discovered?

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

7 April 2017

Polo-like kinases and the orchestration of cell division

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

7 April 2017

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

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

Synthesis of a sugar-based thiosemicarbazone series and structure-activity relationship versus the parasite cysteine proteases rhodesain, cruzain, and Schistosoma mansoni cathepsin B1.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

Repurposing of the Open Access Malaria Box for Kinetoplastid Diseases Identifies Novel Active Scaffolds against Trypanosomatids

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

Natural products as leads in schistosome drug discovery.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

Understanding the Polo Kinase machine

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

Anthelmintic drug discovery: into the future

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

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

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

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

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

Polo-like kinase 1 as a potential therapeutic target for osteosarcoma

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

Schistosomiasis control: praziquantel forever?

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

Polo-like kinases: structural variations lead to multiple functions

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

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

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

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

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

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

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

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

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

Schistosomiasis chemotherapy.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

Schistosomes: challenges in compound screening

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

Susceptibility or resistance of praziquantel in human schistosomiasis: a review

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

SmSak, the second Polo-like kinase of the helminth parasite Schistosoma mansoni: conserved and unexpected roles in meiosis

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

Polo-like kinases inhibitors.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

Protein kinases as potential targets for novel anti-schistosomal strategies.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

Modern phenotypic drug discovery is a viable, neoclassic pharma strategy

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

Quantification and clustering of phenotypic screening data using time-series analysis for chemotherapy of schistosomiasis.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

Polo-box domain inhibitor poloxin activates the spindle assembly checkpoint and inhibits tumor growth in vivo

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

Schistosomiasis: from drug deployment to drug development

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

From Plk1 to Plk5: functional evolution of polo-like kinases

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

Eukaryotic protein kinases (ePKs) of the helminth parasite Schistosoma mansoni

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

Phase I study of GSK461364, a specific and competitive Polo-like kinase 1 inhibitor, in patients with advanced solid malignancies

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

Praziquantel and schistosomiasis.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

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

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

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

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

Sensitivity of cancer cells to Plk1 inhibitor GSK461364A is associated with loss of p53 function and chromosome instability

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

Distinct concentration-dependent effects of the polo-like kinase 1-specific inhibitor GSK461364A, including differential effect on apoptosis

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

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

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

A pan-specific inhibitor of the polo-box domains of polo-like kinases arrests cancer cells in mitosis

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

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

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

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

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

Towards an understanding of the mechanism of action of praziquantel

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

Discovery of thiophene inhibitors of polo-like kinase

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

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

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

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

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

BI 2536, a potent and selective inhibitor of polo-like kinase 1, inhibits tumor growth in vivo.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

In vitro biological activity of a novel small-molecule inhibitor of polo-like kinase 1.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

A clinical drug library screen identifies astemizole as an antimalarial agent

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

Polo-like kinases (Plks) and cancer

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

Schistosoma mansoni: chemotherapy of infections of different ages

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

29 September 2017

Targeting kinases in Plasmodium and Schistosoma: Same goals, different challenges

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

3 June 2018

Efficacy and mechanism of action of volasertib, a potent and selective inhibitor of Polo-like kinases, in preclinical models of acute myeloid leukemia

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

3 June 2018

An Improved Perfusion Technique for Recovering Adult Schistosomes from Laboratory Animals

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

3 June 2018

Susceptibility of Schistosoma japonicum to different developmental stages to praziquantel.

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4709140

3 June 2018

Schistosomiasis and its treatment

1 reference

https://api.crossref.org/works/10.1371%2FJOURNAL.PNTD.0004356

21 January 2018

1 reference

https://api.crossref.org/works/10.1371%2FJOURNAL.PNTD.0004356

21 January 2018

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

1 reference

https://api.crossref.org/works/10.1371%2FJOURNAL.PNTD.0004356

21 January 2018

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

1 reference

https://api.crossref.org/works/10.1371%2FJOURNAL.PNTD.0004356

21 January 2018

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

1 reference

https://api.crossref.org/works/10.1371%2FJOURNAL.PNTD.0004356

21 January 2018

Segmenting the etiological agent of schistosomiasis for high-content screening

1 reference

https://api.crossref.org/works/10.1371%2FJOURNAL.PNTD.0004356

21 January 2018

Inhibition of polo-like kinase 1 by blocking polo-box domain-dependent protein-protein interactions

1 reference

https://api.crossref.org/works/10.1371%2FJOURNAL.PNTD.0004356

21 January 2018

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

1 reference

https://api.crossref.org/works/10.1371%2FJOURNAL.PNTD.0004356

21 January 2018

Parasitic Helminths

1 reference

https://api.crossref.org/works/10.1371%2FJOURNAL.PNTD.0004356

21 January 2018

The small-molecule inhibitor BI 2536 reveals novel insights into mitotic roles of polo-like kinase 1

1 reference

https://pubmed.ncbi.nlm.nih.gov/26751972

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Schistosoma mansoni: Simplified method for the production of schistosomules

1 reference

https://pubmed.ncbi.nlm.nih.gov/26751972

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Cultivation of Schistosoma mansoni In vitro. I. Establishment of Cultures from Cercariae and Development until Pairing

1 reference

https://pubmed.ncbi.nlm.nih.gov/26751972

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Drug discovery without a molecular target: the road less traveled

1 reference

https://pubmed.ncbi.nlm.nih.gov/26751972

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

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10.1371/JOURNAL.PNTD.0004356

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