Targeting CXCR1/2: The medicinal potential as cancer immunotherapy agents, antagonists research highlights and challenges ahead.

Immune suppression in the tumor microenvironment (TME) is an intractable issue in anti-cancer immunotherapy. The chemokine receptors CXCR1 and CXCR2 recruit immune suppressive cells such as the myeloid derived suppressor cells (MDSCs) to the TME. Therefore, CXCR1/2 antagonists have aroused pharmaceutical interest in recent years. In this review, the medicinal chemistry of CXCR1/2 antagonists and their relevance in cancer immunotherapy have been summarized. The development of the drug candidates, along with their design rationale, clinical status and current challenges have also been discussed. Image 1 • CXCR1/2 was considered as pivot of recruiting immune suppressive cells to tumor microenvironment. • This review gave an effort along with the classification and SAR discussion of reported CXCR2 antagonists. • The relevance between CXCR2 and cancer immunosuppressive cells such as MDSCs was discussed. [ABSTRACT FROM AUTHOR]