Development of Certain Protein Kinase Inhibitors with the Components from Traditional Chinese Medicine
Minghua Liu1, Ge Zhao1, Shousong Cao1
1Department of Pharmacology, School of Pharmacy, Southwest Medical University Luzhou, China.
Abstract:
Traditional Chinese medicines (TCMs) have been used in China for more than two thousand years, and some of them have been confirmed to be effective in cancer treatment. Protein kinases play critical roles in control of cell growth, proliferation, migration, survival, and angiogenesis and mediate their biological effects through their catalytic activity. In recent years, numerous protein kinase inhibitors have been developed and are being used clinically. Anticancer TCMs represent a large class of bioactive substances, and some of them display anticancer activity via inhibiting protein kinases to affect the phosphoinositide 3-kinase, serine/threonine-specific protein kinases, pechanistic target of rapamycin (PI3K/AKT/mTOR), P38, mitogen-activated protein kinase (MAPK) and extracellular signal-regulated kinases (ERK) pathways. In the present article, we comprehensively reviewed several components isolated from anticancer TCMs that exhibited significantly inhibitory activity toward a range of protein kinases. These components, which belong to diverse structural classes, are reviewed herein, based upon the kinases that they inhibit. The prospects and problems in development of the anticancer TCMs are also discussed.
Insights
Traditional Chinese medicines (TCMs) offer potential cancer treatments by inhibiting critical protein kinases. This review explores TCM components that target pathways like PI3K/AKT/mTOR and MAPK, highlighting their therapeutic promise.
Area of Science:
- Pharmacology
- Oncology
- Traditional Medicine
Background:
- Traditional Chinese medicines (TCMs) have a long history of use in cancer treatment.
- Protein kinases are crucial regulators of cell functions and are key targets for cancer therapy.
- Many anticancer TCMs exert their effects by inhibiting specific protein kinases.
Purpose of the Study:
- To comprehensively review components isolated from anticancer TCMs.
- To identify TCM-derived compounds with significant protein kinase inhibitory activity.
- To discuss the prospects and challenges in developing TCMs for cancer treatment.
Main Methods:
- Literature review of studies on anticancer TCMs and their isolated components.
- Analysis of reported protein kinase inhibitory activities of these components.
- Categorization of components based on the protein kinases they inhibit.
Main Results:
- Several diverse structural classes of compounds from anticancer TCMs exhibit potent inhibition of various protein kinases.
- Inhibited kinases include those in the phosphoinositide 3-kinase, serine/threonine-specific protein kinases, mechanistic target of rapamycin (PI3K/AKT/mTOR), P38, mitogen-activated protein kinase (MAPK), and extracellular signal-regulated kinases (ERK) pathways.
- The review details specific TCM components and their corresponding kinase targets.
Conclusions:
- Anticancer TCMs provide a rich source of novel protein kinase inhibitors for cancer therapy.
- Further research and development are needed to overcome challenges in translating TCM-derived kinase inhibitors into clinical practice.
- Targeting key signaling pathways with TCM components offers a promising avenue for cancer drug discovery.
