Validating Cell Surface Proteases as Drug Targets for Cancer Therapy: What Do We Know, and Where Do We Go? - Sorbonne Université
Journal Articles Cancers Year : 2022

Validating Cell Surface Proteases as Drug Targets for Cancer Therapy: What Do We Know, and Where Do We Go?

Emile Verhulst
  • Function : Author
  • PersonId : 1141063
Delphine Garnier
Ingrid de Meester
  • Function : Author
  • PersonId : 1141064
Brigitte Bauvois

Abstract

Cell surface proteases (also known as ectoproteases) are transmembrane and membrane-bound enzymes involved in various physiological and pathological processes. Several members, most notably dipeptidyl peptidase 4 (DPP4/CD26) and its related family member fibroblast activation protein (FAP), aminopeptidase N (APN/CD13), a disintegrin and metalloprotease 17 (ADAM17/TACE), and matrix metalloproteinases (MMPs) MMP2 and MMP9, are often overexpressed in cancers and have been associated with tumour dysfunction. With multifaceted actions, these ectoproteases have been validated as therapeutic targets for cancer. Numerous inhibitors have been developed to target these enzymes, attempting to control their enzymatic activity. Even though clinical trials with these compounds did not show the expected results in most cases, the field of ectoprotease inhibitors is growing. This review summarizes the current knowledge on this subject and highlights the recent development of more effective and selective drugs targeting ectoproteases among which small molecular weight inhibitors, peptide conjugates, prodrugs, or monoclonal antibodies (mAbs) and derivatives. These promising avenues have the potential to deliver novel therapeutic strategies in the treatment of cancers.
Fichier principal
Vignette du fichier
cancers-14-00624-v2.pdf (1.11 Mo) Télécharger le fichier
Origin Publication funded by an institution

Dates and versions

hal-03577131 , version 1 (16-02-2022)

Identifiers

Cite

Emile Verhulst, Delphine Garnier, Ingrid de Meester, Brigitte Bauvois. Validating Cell Surface Proteases as Drug Targets for Cancer Therapy: What Do We Know, and Where Do We Go?. Cancers, 2022, 14 (3), pp.624. ⟨10.3390/cancers14030624⟩. ⟨hal-03577131⟩
39 View
112 Download

Altmetric

Share

More