Antibody-drug conjugates (ADCs) constitute an emerging class of anticancer agents that deliver potent payloads selectively to tumors while avoiding systemic toxicity associated with conventional chemotherapeutics. Critical to ADC development is a serum-stable linker designed to decompose inside targeted cells...
Albumin-binding prodrugs of camptothecin and doxorubicin with an Ala-Leu-Ala-Leu-linker that are cleaved by cathepsin B: synthesis and antitumor efficacy. We have recently validated a macromolecular prodrug strategy for improved cancer chemotherapy based on two features: (a) rapid and selective bindin...
The influence of linker length on the properties of cathepsin S cleavable (177)Lu-labeled HPMA copolymers for pancreatic cancer imaging. Biomaterials. 2014;35:5760-5770.Shi W, Ogbomo SM, Wagh NK, Zhou Z, Jia Y, Brusnahan SK, Garrison JC. 2014. The influence of linker length on the ...
The linker, responsible for the connection between the antibody and payload, is a crucial component of ADCs. In certain examples the linker is composed of a cleavable short peptide which imparts an additional aspect of selectivity. Especially prevalent is the cathepsin B cleavable Mc-Val-Cit-PABO...
Dipeptide synthesisDrug-linker constructCleavable linkerEpimerizationAntibody-drug conjugates (ADCs) represent an emergdoi:10.1016/j.tetlet.2018.08.021Mondal DeboprosadFord JacobPinney Kevin G.Tetrahedron Letters
Because of the complex mechanisms mediating cancer onset, prognosis, and metastatic behavior, different therapeutic approaches targeting these mechanisms have been investigated. Recent advancements in nanocarrier-based drug and gene delivery methods have