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Updated: Aug 17, 2026

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays
Published on: October 23, 2019
Drugs targeted against protein kinases
1Department of Tumour Biology, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. chandra.kumar@spcorp.com
Abstract:
Current treatments for cancer (surgery, radiation and chemotherapy) are successful for early stage localised disease but have severe side effects. New treatments are needed to increase the cure rate and life expectancy of patients. With the discovery of oncogenes, tumour suppressor genes and an understanding of their role in the development of the malignant disease, a new era of therapy has begun. Cancer is a manifestation of deregulated signalling pathways that mediate cell growth and programmed cell death. Protein kinases are essential elements in these signalling pathways. In the US, Novartis launched Gleevec (imantinib, STI-571) in May 2001 as the first anticancer drug whose mechanism of action is kinase inhibition. In Phase I trials, 23/24 patients with chronic myelogenous leukaemia (CML) had complete remissions and the drug is relatively non-toxic. Herceptin (trastuzumab) is a monoclonal antibody (mAb) against a member of the growth factor receptor family (HER-2/neu) that was launched in 1998 by Genentech for the treatment of breast cancer. Trastuzumab has an excellent antitumour profile, particularly when used in combination with doxorubicin and paclitaxol. These drugs are pioneering the treatment of cancer based on the molecular understanding of the disease. Numerous drugs that target growth factor receptors and their signalling pathways are in advanced clinical trials. Herein, antibodies against receptors and small molecule inhibitors of kinases in signalling pathways will be summarised. Inter-disciplinary preclinical studies have identified chemicals that target specific kinases. We believe that clinical studies of these agents will yield new anticancer agents that target specific diseases and that are less toxic than current agents.
Insights
New cancer therapies targeting molecular pathways, like kinase inhibitors and monoclonal antibodies, show promise for improved efficacy and reduced toxicity compared to traditional treatments.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Current cancer treatments (surgery, radiation, chemotherapy) are limited by severe side effects and efficacy in advanced disease.
- Understanding oncogenes and tumor suppressor genes has revealed cancer's basis in deregulated cellular signaling pathways.
- Protein kinases are crucial in these signaling pathways, making them key therapeutic targets.
Purpose of the Study:
- To summarize novel cancer therapies targeting molecular pathways, including kinase inhibitors and monoclonal antibodies.
- To highlight the shift towards molecularly targeted cancer treatments.
- To discuss the potential for reduced toxicity and increased efficacy of these new agents.
Main Methods:
- Review of existing literature on targeted cancer therapies.
- Summary of key drugs like Gleevec (imatinib) and Herceptin (trastuzumab).
- Discussion of preclinical and clinical trial findings for kinase inhibitors and receptor antibodies.
Main Results:
- Gleevec (imatinib) demonstrated high remission rates and low toxicity in chronic myelogenous leukemia (CML) by inhibiting kinases.
- Herceptin (trastuzumab), a monoclonal antibody, shows excellent antitumor activity in breast cancer, especially in combination therapies.
- Numerous targeted drugs are in advanced clinical trials, indicating a growing pipeline of molecularly-driven cancer treatments.
Conclusions:
- Targeted therapies, including kinase inhibitors and monoclonal antibodies, represent a new era in cancer treatment.
- These novel agents offer the potential for greater specificity, improved cure rates, and reduced side effects.
- Further clinical studies are expected to yield new, less toxic anticancer agents tailored to specific diseases.
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