GPCR Targeting Monoclonal Antibodies: Using Them to Develop New Drugs

First identified in 1986, Guanine nucleotide binding protein (G-protein) coupled receptors (GPCRs) are complex proteins found in cell membranes. A notable characteristic of these proteins is that they pass through the cell membrane a total of seven times, earning them the name ‘seven-pass-transmembrane domain receptors.’

The function and structure of GPCRs were further clarified by Brian Kobilka and Robert Lefkowitz, who were both awarded the Nobel Prize in Chemistry in 2012.

GPCRs play an important part in signal transmission to G-protein cells where a signal molecule is detected outside the cell itself. More than 800 varieties of proteins are found in the GPCR family. In instances where extracellular signals (for example, neurotransmitters and hormones) are transmitted to the inside of cells via GPCRs, a cascade of biological signal transmission (a chain reaction) will be triggered inside the cell.

A sizeable majority of drugs designed to target GPCRs are antidiabetic drugs and antihypertensive agents. These types of drugs account for over 30% of all drugs currently on the market.

Antibodies are specific proteins that recognize antigens in immunological responses. Drugs based on antibodies are highly efficient while minimizing side effects because these drugs will specifically recognize and bind only to the target molecules.

Mr. Takayama, the founder of NB Health Laboratory Co. Ltd., is working on discovering and manufacturing antibody-based biological drugs rather than chemically synthesized, small molecule drugs.

Antibodies targeting GPCRs makes it possible to directly intervene the transmission of information in diseases involving GPCRs signaling; therefore, discovery of such antibodies can lead to development of extremely effective drugs for these diseases."

Mr. Takayama, Founder, NB Health Laboratory Co. Ltd.

A number of revolutionary Japanese-produced antibody drugs already exist; for example, tocilizumab, the rheumatoid arthritis therapeutic drug (Chugai Pharmaceutical). This drug targets the interleukin-6 (IL-6) cytokine and was discovered by Tadamitsu Kishimoto at Osaka University.

Other drugs include mogamulizumab, the adult T cell leukemia therapeutic drug (Kyowa Hakko Kirin Co., Ltd.), which targets the CCR4 receptor; and nivolumab (Ono Pharmaceutical), a cancer immunotherapeutic antibody drug that was discovered by Tasuku Honjo at Kyoto University...

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Last updated: Jun 9, 2023 at 7:40 AM


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