Journal
BIOCHIMICA ET BIOPHYSICA ACTA-REVIEWS ON CANCER
Volume 1871, Issue 2, Pages 199-224Publisher
ELSEVIER
DOI: 10.1016/j.bbcan.2018.12.002
Keywords
Immune checkpoint; Small-molecule inhibitor; Combination therapy; Cancer
Categories
Funding
- National Natural Science Foundation of China [81602492]
- National Key Research and Development Program of China [2016YFA0201402]
- National Major Scientific and Technological Special Project for Significant New Drugs Development [2018ZX09733001]
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Initially understood for its physiological maintenance of self-tolerance, the immune checkpoint molecule has recently been recognized as a promising anti-cancer target. There has been considerable interest in the biology and the action mechanism of the immune checkpoint therapy, and their incorporation with other therapeutic regimens. Recently the small-molecule inhibitor (SMI) has been identified as an attractive combination partner for immune checkpoint inhibitors (ICIs) and is becoming a novel direction for the field of combination drug design. In this review, we provide a systematic discussion of the biology and function of major immune checkpoint molecules, and their interactions with corresponding targeting agents. With both preclinical studies and clinical trials, we especially highlight the ICI + SMI combination, with its recent advances as well as its application challenges.
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