ALDH1A1, one important member of 19 ALDHs, can metabolize reactive aldehydes to their corresponding carboxylic acid derivatives and play important physiological and toxicological roles in many areas, including CNS, metabolic disorders, and cancers. Overexpression of ALDH1A1 correlates with poor prognosis and tumor aggressiveness, is associated with drug resistance in traditional chemotherapy for cancer treatment and contributes to obesity, diabetes, and inflammation. So, inhibition of ALDH1A1 may offer new therapeutic options for patients with cancer, obesity, diabetes, and inflammation. Up to now, many ALDH1A1 inhibitors with different scaffolds have been identified and developed as useful chemical tools for better understanding of the functions of ALDH1A1 in physiologic and pathophysiologic conditions. In this review, the advances in the discovery and development of selective ALDH1A1 inhibitors are summarized, and opportunities and challenges associated with this field are also discussed.

ALDH1A1是19种ALDH的重要成员之一，可以将反应性醛代谢为相应的羧酸衍生物，并在包括CNS，代谢紊乱和癌症在内的许多领域中发挥重要的生理和毒理作用。ALDH1A1的过度表达与不良预后和肿瘤侵袭性相关，与传统的癌症化疗药物的耐药性有关，并导致肥胖，糖尿病和炎症。因此，抑制ALDH1A1可能为癌症，肥胖，糖尿病和炎症患者提供新的治疗选择。迄今为止，已经鉴定并开发了许多具有不同支架的ALDH1A1抑制剂，作为有用的化学工具，用于更好地了解ALDH1A1在生理和病理生理条件下的功能。在这篇评论中