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SynB1-ELP1-Dox3

Development stage
Preclinical
Lead developer
University of Mississippi Medical Center
Modality
Peptide-Drug Conjugates → Peptide Conjugates → Peptides, Biodegradable Polymers → Polymer-based Nanoparticles → Nanoparticles → Drug Delivery Systems
Administration
Intravenous
01

Overview

SynB1-ELP1-Dox3 is a thermally responsive macromolecular biopolymer-drug conjugate designed for targeted cancer therapy, particularly breast cancer and glioblastoma. It consists of three main components: the cell-penetrating peptide SynB1 at the N-terminus to enhance cellular uptake, a thermally responsive elastin-like polypeptide (ELP1) carrier that aggregates in response to mild hyperthermia (around 41-42°C), and three molecules of doxorubicin (Dox) conjugated via an acid-sensitive (6-maleimidocaproyl) hydrazone linker (DOXO-EMCH) to terminal cysteine residues. This design allows the conjugate to remain soluble at physiological temperature and selectively aggregate in tumor regions subjected to localized hyperthermia. Following cellular internalization, the pH-sensitive hydrazone linker is cleaved in the acidic environment of endosomes and lysosomes, releasing active doxorubicin to exert its cytotoxic effects while minimizing systemic toxicities, such as cardiotoxicity.

Other names
SynB1-elastin-like polypeptide-doxorubicin conjugateSynB-1-elastin-like polypeptide-doxorubicin conjugateSynB 1-elastin-like polypeptide-doxorubicin conjugateSynB1-ELP-doxorubicin conjugateSynB-1-ELP-doxorubicin conjugateSynB 1-ELP-doxorubicin conjugate
02

Targets

TOP2A (DNA topoisomerase II)DNA

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