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Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays
Published on: October 23, 2019
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PIM kinase inhibitors: Structural and pharmacological perspectives
Vivek Asati1, Debarshi Kar Mahapatra2, Sanjay Kumar Bharti3
1Department of Pharmaceutical Chemistry, NRI Institute of Pharmacy, Bhopal, 462023, Madhya Pradesh, India.
European Journal of Medicinal Chemistry
|April 8, 2019
Summary
PIM kinases (serine/threonine kinases) are crucial in cancer. This review details their role in oncogenesis, highlights PIM inhibitors as therapeutic targets, and explores structure-activity relationships for advanced cancer treatment.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- PIM kinases (PIM-1, PIM-2, PIM-3) are serine/threonine kinases involved in cell proliferation, differentiation, and apoptosis.
- Overexpressed PIM kinases act as oncogenes, contributing to various human cancers.
- PIM kinase isoforms are emerging as clinical biomarkers and therapeutic targets for personalized cancer therapy.
Purpose of the Study:
- To review the pharmacological implications of PIM kinases in oncogenesis.
- To provide structural insights into PIM kinase inhibitors.
- To analyze structure-activity relationships (SARs) of PIM inhibitors.
Main Methods:
- Literature review focusing on PIM kinase roles in cancer.
- Analysis of published data on PIM kinase inhibitors and their synthesis.
- Examination of structure-activity relationships for identified PIM inhibitors.
Main Results:
- PIM kinases play a significant role in cancer development and progression.
- Various heterocyclic scaffolds (e.g., pyrrole, pyrimidine, indole) show PIM inhibitory activity.
- Several PIM inhibitors are in clinical trials for advanced cancer treatment.
Conclusions:
- PIM kinase inhibition represents a promising strategy for cancer therapy.
- Understanding SARs is crucial for developing potent and selective PIM inhibitors.
- Targeting PIM kinases offers potential for personalized medicine in oncology.
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