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Updated: Aug 17, 2026

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays
Published on: October 23, 2019
Protein kinases in drug discovery and development
1ImClone Systems Inc, 180 Varick Street 6th Floor, New York, NY 10014, USA. yaronh@imclone.com
Abstract:
The Protein Kinases in Drug Discovery and Development meeting highlighted protein kinases as validated therapeutic targets in many types of disease, especially cancer. Drugs designed to inhibit protein kinase activity were widely tested in preclinical and clinical evaluation, demonstrating significant efficacy with acceptable toxicity profiles. More than 600 kinases are encoded by the human genome, some of which are already well established as validated targets due to extensive scientific research from both academic institutions and industrial companies. As demonstrated by several speakers during the meeting, different diseases exhibit mutations or over-expression of the same kinase. Therefore, a drug designed to inhibit these specific kinases can potentially be used as a therapeutic agent in the treatment of more then one disease. The major strategy employed by most companies today in drug discovery is using genomic information, together with clinical research, to identify novel potential targets. A drug discovery project is then established around the chosen target kinase, in order to identify, optimize and deliver novel potential drugs to clinical trials.
Insights
Protein kinases are validated targets for treating diseases like cancer. Inhibiting specific kinases shows efficacy and acceptable toxicity, offering potential for multi-disease therapeutic agents.
Area of Science:
- Biochemistry
- Pharmacology
- Oncology
Background:
- Protein kinases are crucial targets in drug discovery, particularly for cancer therapy.
- Over 600 kinases encoded by the human genome are subjects of extensive academic and industrial research.
- Mutations or overexpression of specific kinases are implicated in various diseases.
Purpose of the Study:
- To highlight protein kinases as validated therapeutic targets.
- To discuss the strategy of using genomic and clinical data for novel target identification.
- To outline the drug discovery process centered around target kinases.
Main Methods:
- Review of preclinical and clinical evaluations of protein kinase inhibitors.
- Identification of novel targets using genomic information and clinical research.
- Establishment of drug discovery projects around chosen target kinases.
Main Results:
- Protein kinase inhibitors demonstrate significant efficacy and acceptable toxicity.
- A single kinase can be a target for multiple diseases.
- Genomic-driven strategies are central to modern drug discovery.
Conclusions:
- Protein kinases represent validated therapeutic targets with broad applicability.
- Targeting specific kinases offers potential for treating diverse diseases.
- Integrated genomic and clinical approaches drive the identification and development of novel kinase-targeted drugs.
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