Small Molecule Activators

Enzymes are macromolecules with biocatalytic function to accelerate chemical reactions. Enzymes are indispensable in various functions of living organisms and play key roles in almost every physiological/pathological process such as signal transduction, cell regulation, metabolism, activity control and digestion. Strict control of enzyme activity is essential for homeostasis. Any malfunction of key enzymes (mutation, overproduction, underproduction or deletion) can lead to diseases. Therefore, enzymes have long been considered as important drug targets for the treatment of major human diseases.

Small molecule activators are opposite to inhibitors. From therapeutic point of view, using small molecular activators to efficiently and selectively activate physiologically relevant biological targets including enzymes has a great therapeutic potential because the low expression of these enzymes is the cause of the observed pathophysiological disorders. The binding of enzyme activators may accelerate enzymatic reaction by leading to the creation of more profitable conformers which can be more effective in carrying out definite steps of the reaction. The combined of small molecule activators as well as inhibitors is helpful to fine-tune the desired expression of these specific enzymes and has great therapeutic implications.

Small molecule activators have great biological potential such as anti-bacterial activity, anti-cancer activity, ion channel activation, protein kinase modulation and apoptosis modulation. They are also invaluable tools for studying protein function in complex signaling pathways. Small molecule activators have been used in the treatment of cancer, diabetes, infectious diseases, metabolic and endocrine diseases, and neurological diseases, and also have enormous potential to treat other clinically important diseases. The research potential of selectively increasing of a specific target/enzyme expression makes small molecule activators advantageous. This is also one of the driving forces behind the design and development of small molecule activators as drugs.

Compared with the common used small molecule inhibitors, especially enzyme inhibitors, small molecules activators have less application therapeutic applications in the treatment of diseases and have great promise for development and therapeutic success.

Proposed mechanism for allosteric SIRT1 activation by sirtuin activating compounds (STACs). Figure 1. Proposed mechanism for allosteric SIRT1 activation by sirtuin activating compounds (STACs). (Hubbard, B. P., et al., 2014)

Creative Biolabs provides powerful risk-based preclinical data verification services for small molecule activator 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 activators and different disease areas. Our services focus on target validation, hit validation, lead validation, safety assessment and efficacy evaluation.

As a global contract research organization with advanced equipment and up-to-date technology, Creative Biolabs’ professional scientific team involving biologists, chemists, and pharmacologists can make sure that our clients will receive fully compliant and trustworthy results in the timelines promised.

Creative Biolabs can offer customized and most suitable methods to meet your specific needs in a cost-effective manner. We are confident to offer our clients with project feasibility assessment through a comprehensive assessment of you drug candidates to help reduce investment risk.

Our services will be of great benefit to you for your drugs research and development projects. If you are interested in our services or have any other questions, please feel free to contact us. We are always there for you and looking forward to working with you in the near future.


  1. Hubbard, B. P.; Sinclair, D. A., 2014. Small molecule SIRT1 activators for the treatment of aging and age-related diseases. Trends in pharmacological sciences, 35(3), pp. 146-154.

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