Analysis of the Current Status of Approved Small Molecular Drug Targets in the World

Before, Nature Reviews Drug Discovery (IF=47) published an article called “A comprehensive map of molecular drug targets” which comprehensively analyzed the approved small molecular drugs and their targets.

The researchers collected 1, 591 approved drugs (small molecule drugs and biopharmaceuticals) and 893 targets for these drugs, of which 667 were human proteins. It showed that the current drug target is mainly focused on human protein.

Drug target family classification

The researchers counted the family distribution of 667 human target proteins, and found that GPCR screening, ion channels, nuclear receptors and kinases, as the main target protein families accounted for 12%, 19%, 10% and 3%, respectively. Since multiple targeted drugs may be developed at the same target in drug development, researchers statistically classified 999 small molecular drugs and found 33% of the small molecular targeted GPCR, 18% of the small molecular targeted ion channels, 16% of the small molecular targeted nuclear receptors, and 3% small molecular targeted kinases.

In conclusion, we can see that the target proteins are mainly distributed in four families of GPCR, ion channel, nuclear receptor and kinase which account for about half of the total target proteins. 70% of the small molecular drugs are designed for these four types of targets.

Current situation of drug target research

The researchers synthetically counted the approval time of the drug and the situation of the protein family to which the target belongs. Since 2011, GPCR and kinases had been approved more, while nuclear receptors and ion channels had been approved less. It can be seen that the in four dominant families, GPCR and kinase targets have been the focus of research in recent years.

New technology for drug target screening

From the data provided in this paper, we can see that human proteins of kinases and GPCR are still the main targets for the development of small molecular drugs. This highlights the special importance of these two proteins in disease treatment and drug development. Therefore, we systematically study the binding of GPCR and kinase proteins to small molecules, and the regulation of expression and phosphorylation activity of these proteins under the control of small molecules, which is particularly important to accelerate the development and marketing of these small molecular drugs.

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