An adjustable release rate linking strategy for cytotoxin–Peptide conjugates
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2021, Bioorganic and Medicinal ChemistryCitation Excerpt :The carbamate linkage was formed between the linker and triptolide, due to carbamates group are generally supposed to be more stable than carbonates (L1-TL). Also, N,N'-Dimethyl-1,2-ethanediamine spacer was introduced to the linker, as it might improve the stability and the biological profile of the linker-drug (L2-TL).23–24 Additionally, the diamine spacer also provides a site to incorporate a branching PEGylated linker (L3-TL).
Advancements in folate receptor targeting for anti-cancer therapy: A small molecule-drug conjugate approach
2021, Bioorganic ChemistryCitation Excerpt :Ester and carbamate bonds can be hydrolyzed enzymatically after internalization by the acidic pH in the lysosomes or by the enzymes such as esterases and cytochrome P450 [155,180–182]. Carbamate linkers of varying stability have been used to connect the tumor-targeting peptide SST with the toxophore camptothecin (CPT) [155]. Alsarraf et al. has developed β-galactosidase-responsive SMDC consisting of phenolic and aniline self-immolative connectors, galactoside trigger, folic acid as ligand targeting and two MMAE molecules based around a chemical amplifier that delivers two drug molecules the potent antineoplastic drug monomethylauristatin E (MMAE) to cancer cells through a single internalization and activation pathway [183].
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