Drug intelligence / Profile preview

mRBD3dopa + bortezomib

Development stage
Preclinical
Modality
Small Molecules, Recombinant Proteins and Enzymes
Administration
Intravenous
01

Overview

mRBD3dopa + bortezomib is an experimental protein-drug conjugate (PDC) designed for the targeted treatment of non-small cell lung cancer (NSCLC). It utilizes a mutant version of the SARS-CoV-2 receptor-binding domain (mRBD3) as a targeting ligand, which is genetically engineered to include a 3,4-dihydroxyphenyl-L-alanine (DOPA) linker. This DOPA moiety forms a reversible catechol-boronate ester bond with bortezomib, a potent 26S proteasome inhibitor. The conjugate specifically targets the Angiotensin-converting enzyme-2 (ACE2) receptor, which is frequently overexpressed in lung cancer cells. Upon binding, the complex is internalized via receptor-mediated endocytosis, and the acidic environment of the endosome triggers the controlled release of bortezomib. This targeted delivery approach aims to enhance the therapeutic efficacy of bortezomib in NSCLC while minimizing systemic toxicity and off-target effects in normal ACE2-expressing tissues.

Other names
mutant RBD3-DOPA-bortezomibACE2-targeting bortezomib conjugateACE-2-targeting bortezomib conjugateACE 2-targeting bortezomib conjugate
02

Targets

PSMB5 (Proteasome subunit beta Type-5)ACE2 (Angiotensin-converting enzyme 2)

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