Disclosed are monoacylated Toll-like receptor 2 ligands which can be used in both the development of targeted agents for the imaging and treatment of pancreatic cancer as well as other cancers, and as an adjuvant for cancer immunotherapy. The monoacylated compounds disclosed herein have a higher binding affinity for TLR2 relative to a known potent diacylated agonists, but only -1/2 the bioactivity. Competition of the monoacylated compound with the diacylated compound for binding TLR2 was confirmed. Hence, the reported monoacylated compounds are inhibitors/antagonists of TLR2 activation.
本发明涉及一类单酰化的Toll样受体2
配体,可用于开发针对胰腺癌和其他癌症的靶向剂,用于影像和治疗,以及作为癌症免疫治疗的佐剂。本发明所披露的单酰化化合物与一种已知的有效双酰化激动剂相比,具有更高的TLR2结合亲和力,但仅有1/2的
生物活性。已证实单酰化化合物与双酰化化合物竞争结合TLR2。因此,所报告的单酰化化合物是TLR2激活的
抑制剂/拮抗剂。