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Identification of Cyclin-dependent Kinase 1 Specific Phosphorylation Sites by an In Vitro Kinase Assay
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Sphingosine Kinases as Druggable Targets.

Susan Pyne1, David R Adams2, Nigel J Pyne3

  • 1Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde , Glasgow, Scotland, UK.

Handbook of Experimental Pharmacology
|February 21, 2018
PubMed
Summary

Sphingosine kinases 1 and 2 are key enzymes in disease. This chapter explores their druggability and the development of isoform-specific inhibitors for various conditions.

Keywords:
CancerInflammationNeurodegenerationPulmonary hypertensionSicklingSphingosine 1-phosphateSphingosine kinase

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Area of Science:

  • Biochemistry
  • Pharmacology
  • Molecular Biology

Background:

  • Sphingosine kinase 1 and 2 (SphK1/2) catalyze the production of sphingosine 1-phosphate (S1P).
  • Sphingosine 1-phosphate is a bioactive lipid mediator implicated in numerous pathophysiological processes.
  • Dysregulation of SphK1/2 activity is linked to various diseases, highlighting their therapeutic relevance.

Purpose of the Study:

  • To evaluate the druggability of sphingosine kinase 1 and 2.
  • To explore the development of isoform-specific inhibitors targeting SphK1/2.
  • To contextualize the therapeutic potential of SphK inhibitors across diverse disease areas.

Main Methods:

  • Appraisal of existing evidence on SphK1 and SphK2 druggability.
  • Analysis of the sphingosine-binding site plasticity for inhibitor design.
  • Review of preclinical and clinical data on SphK inhibitor efficacy.

Main Results:

  • Substantial evidence supports the druggability of both SphK1 and SphK2.
  • The plasticity of the sphingosine-binding site allows for the development of isoform-specific inhibitors.
  • SphK inhibitors show promise in preclinical models of cancer, pulmonary hypertension, neurodegeneration, inflammation, and sickling disorders.

Conclusions:

  • Sphingosine kinases represent viable therapeutic targets.
  • Isoform-specific inhibition strategies are feasible and crucial for targeted therapy.
  • SphK inhibitors hold significant therapeutic potential across a spectrum of human diseases.