Small Molecule Inhibitors

Small molecule inhibitors are a class of small molecules that interact with proteins and reduce the biological activity of target proteins. The structure of small molecule inhibitors has good spatial dispersion, and their chemical properties determine their good pharmacodinemic properties and pharmacokinetic properties. These characteristics make small molecule inhibitors show great advantages in drug research and development process, and these molecules are becoming more and more popular in the market.

Small molecule inhibitors commonly used in drug research and development at present mainly include enzyme inhibitors and transcription factor inhibitors. Enzyme inhibitors are molecules that bind to enzymes and reduce their activity. They can kill pathogens or correct metabolic imbalances by blocking the activity of an enzyme. Transcription factor inhibitors can regulate gene expression by directly or indirectly preventing the binding of transcription factors from binding to DNA.

The emergence of small molecule inhibitors has become one of the important pillars of cell biology research. Small molecule inhibitors provide an excellent opportunity to study many aspects of cell biology, from cell cycle control and mitosis to signaling pathways and gene expression. Speaking of new drug research and development, small molecule inhibitors have many advantages compared with cytotoxic drugs, so they become an important tool for people to deeply understand cell microenvironment and signal transduction pathways. And also they provide hope for patients to obtain better clinical efficacy. Therefore, it is not surprising that the research and development of small molecule inhibitors has witnessed steady growth between the pharmaceutical industry and research institutions.

The discovery and development of small molecule inhibitors has been revolutionized in the past few years. Small-molecules that inhibit specific protein-protein interactions have long been a promising approach for therapeutic intervention in a variety of settings. At present, the indication of small molecule inhibitors tends to be cancer, but there has been increasing interest in their use for non-oncologic diseases as well, such as infectious diseases, inflammatory diseases, neurological diseases and autoimmune diseases. In addition, there is an exciting prospect for small molecule inhibitors to be used in combination with genome sequencing to develop personalized medicine. However, the current small molecule inhibitors application is just the tip of an iceberg that is still unimaginable.

Mechanisms of small molecule inhibition of protein–protein interactions. Figure 1. Mechanisms of small molecule inhibition of protein–protein interactions. (Cesa, L. C., et al., 2015)

Creative Biolabs provides powerful risk-based preclinical data verification services for small molecule inhibitor research and development to deal with data reproducibility crisis which is a big obstacle for drug research and development and may lead to failure and high risk of investment. We have extensive experience in different kinds of small molecule inhibitors and different disease areas. Our services focus on target validation, hit validation, lead validation, safety assessment and efficacy evaluation.

Identification of high-quality drug candidates need a large amount of intellectual and innovative input from experienced scientists from different disciplines and background. Creative Biolabs has seasoned experts, state-of-the-art equipment and advanced technology platform to provide you with professional and reliable services. Fully compliant and trustworthy results will be provided within the promised timeline.

Creative Biolabs offers our clients with project feasibility assessment through a comprehensive assessment of your drug candidates to help foresee challenges, overcome obstacles, and promote our common progress in bringing new drugs to the market with low investment risk.

Our services will be of great benefit to you if you are about to start or you are developing small molecule inhibitor research and development projects. Please feel free to contact us and we are always there for you.


  1. Cesa, L. C., et al., 2015. Direct and propagated effects of small molecules on protein–protein interaction networks. Frontiers in bioengineering and biotechnology, 3: 119

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