Small Molecule-Nanobody Conjugate Inducers of Proximity (SNACIP) and Preparation Methods and Use thereof

Abstract

The disclosure discloses small molecule-nanobody conjugate inducers of proximity (SNACIP) and preparation methods and use thereof, and belongs to the technical field of cell regulation. Chemical inducers of proximity (CIPs) induce dimerization between proteins to regulate biological progresses. However, the CIP has the disadvantages of difficulties in directly regulating endogenous proteins without ligand binding sites, background activity interference of endogenous proteins, difficulties in use for drug development, etc. The SNACIP disclosed herein includes a nanobody targeting moiety, a small molecule binding motif, an intracellular delivery moiety and a linker. In the disclosure, a cRGT general inducer has the advantages of easy cell penetration, rapidity, reversibility, thorough regulation, and dose-dependence; a cRTC-type inducer can specifically regulate an intrinsically disordered protein in the cell; and a bivalent nanobody CTTC inducer is suitable for use in vivo. The SNACIP is a new-generation regulatory inducer of proximity with extensive and extremely important use value.

Dependencies are inferred from the claim text.