SORT1-targeted Peptide Drug-Conjugate PQ203

**Semantic type:** Pharmacologic Substance

**Definition:** A peptide-drug conjugate (PDC) composed of a peptide targeting the cell surface receptor sortilin (SORT1) conjugated to monomethylauristatin E (MMAE), an auristatin derivative and a potent microtubule inhibitor, with potential antineoplastic activity. Upon administration of SORT1-targeted PDC PQ203, the peptide selectively targets and binds to SORT1 expressed on tumor cells. Upon internalization and lysosomal payload release, MMAE binds to tubulin and inhibits its polymerization, resulting in G2/M phase arrest and tumor cell apoptosis. SORT1 is overexpressed in a variety of cancers, including triple-negative breast cancer (TNBC), and plays an important role in protein internalization, sorting and trafficking.

**Synonyms:** - PQ 203 - PQ-203 - PQ203 - Peptide Drug-Conjugate PQ203 - SORT1-targeted PDC PQ203 - Sortilin-targeted PDC PQ203