Development of hypoxia-activated PROTAC exerting a more potent effect in tumor hypoxia than in normoxia
Weiyan Cheng, Shasha Li, Xueqian Wen, Siyuan Han, Suhua Wang, Wei Han, Zhizhen Song, Yueqin Wang, Xin Tian, Xiaojian Zhang
Abstract
in hypoxia than in normoxia in HCC4006 cells. This is the first example of identifying a PROTAC to selectively act on tumors utilizing the characteristic of tumor hypoxia and provides a new approach for PROTAC development.
Topics & Concepts
Hypoxia (environmental)ProdrugChemistryProteolysisTumor hypoxiaCancer researchCell biologyPharmacologyBiochemistryBiologyOxygenInternal medicineMedicineEnzymeOrganic chemistryRadiation therapyProtein Degradation and InhibitorsUbiquitin and proteasome pathwaysPeptidase Inhibition and Analysis