TY - JOUR AU - Fan, Junwan AU - Li, Haowen AU - Kuang, Lun AU - Zhao, Zichen AU - He, Wenyan AU - Liu, Chen AU - Wang, Yongjun AU - Cheng, Steven Y. AU - Chen, Wei PY - 2021 DA - 2021/03/02 TI - Identification of a potent antagonist of smoothened in hedgehog signaling JO - Cell & Bioscience SP - 46 VL - 11 IS - 1 AB - Hedgehog signaling is essential to the regulation of embryonic development, tissue homeostasis, and stem cell self-renewal, making it a prime target for developing cancer therapeutics. Given the close link between aberrant Hedgehog signaling and cancers, many small molecular compounds have been developed to inhibit Smoothened, a key signal transducer of this pathway, for treating cancer and several such compounds have been approved by the United States Food and Drug Administration (GDC-0449 and LDE-225). However, acquired drug resistance has emerged as an important obstacle to the effective use of these first generation Hedgehog pathway blockers. Thus, new Smoothened inhibitors that can overcome such resistance is an urgent need going forward. SN - 2045-3701 UR - https://doi.org/10.1186/s13578-021-00558-9 DO - 10.1186/s13578-021-00558-9 ID - Fan2021 ER -