Title:Small-Molecule CSF1R Inhibitors as Anticancer Agents
VOLUME: 27 ISSUE: 23
Author(s):Qiuju Xun, Zhen Wang, Xianglong Hu, Ke Ding* and Xiaoyun Lu*
Affiliation:International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development of Chinese Ministry of Education (MOE), School of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development of Chinese Ministry of Education (MOE), School of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development of Chinese Ministry of Education (MOE), School of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development of Chinese Ministry of Education (MOE), School of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development of Chinese Ministry of Education (MOE), School of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632
Keywords:Tumor-Associated Macrophages (TAMs), CSF1R, inhibitors, anticancer agents, pharmacophore features,
clinical trials.
Abstract:Persuasive evidence has been presented linking the infiltration of Tumor-Associated
Macrophages (TAMs) with the driving force of tumorigenesis and in the suppression of antitumor
immunity. In this context CSF1R, the cellular receptor for Colony Stimulating Factor-1 (CSF1) and
Interleukin 34 (IL-34), occupies a central role in manipulating the behavior of TAMs and the
dysregulation of CSF1R signaling has been implicated in cancer progression and immunosuppression
in many specific cancers. Consequently, CSF1R kinase has been a target of great interest in
cancer treatment and significant research efforts have focused on the development of smallmolecule
CSF1R inhibitors. In this review, we highlight current progress on the development of
these small molecule CSF1R inhibitors as anticancer agents. Special attention is paid to the compounds
available in advanced clinical trials.
