Main Immune Checkpoint Molecules for Drug Development

Introduction to Immune Checkpoints

Immune checkpoints, a group of regulators, have been generated for maintaining immune homeostasis and preventing autoimmunity. These molecules can trigger the T cell activation by controlling the antigen recognition of the T cell receptor (TCR). In general, immune checkpoints can be classified into two main subtypes: co-stimulatory immune checkpoints and co-inhibitory immune checkpoints. For example, batteries of co-stimulatory checkpoint molecules, such as CD28, ICOS, and CD137, have been shown to promote immune progress. Plentiful co-inhibitory checkpoint molecules, like PD1, CTLA-4, and VISTA, have been demonstrated to inhibit immune progress. In particular, these immune checkpoint molecules prevent normal cells or tissues from being killed by the immune system.

Immune checkpoint blockade in cancer. Fig.1 Immune checkpoint blockade in cancer. (Dyck, 2017)

Immune Checkpoint Molecule for Drug Development

Over these years, a number of immune checkpoint molecules have been actively studied for reducing inflammation and discovering novel drugs that directly target disease cells. Recently, drug development targeting immune checkpoint molecules or their ligands is mainly focused on cancer immunotherapies. For instance, CTLA4 and PD-1-based therapies have been established and approved for treating certain types of tumors, like melanoma. Furthermore, current studies have indicated that a series of new checkpoint molecules have been discovered and present anti-tumor activity in pre-clinical studies. More and more immunotherapies based on the immune checkpoint for the treatment of cancers are on the way to the market. Therefore, the ongoing discovery of other checkpoints should be a continued search for therapeutic benefits in cancer. Till now, a wide range of immune checkpoint molecules have been characterized for drug development, including but not limited to:

Creative Biolabs offers a full range of immune checkpoint-based solutions for helping the discovery of various new drugs, including proteins, antibodies, peptides, small-molecule drugs, as well as inhibitors, to help the treatment of different human diseases. Also, equipped with state-of-the-art facilities and highly experienced staff, they are available to assist in all areas of biomarkers and detection assays development for immune checkpoints.


  1. Dyck, L.; et al. Immune checkpoints and their inhibition in cancer and infectious diseases. European journal of immunology. 2017, 47(5): 765-779.

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