ACE-2, TMPRSS2 and Beyond; Promising Targets and Tools for COVID-19 Prophylaxis and Treatment

Gepdiremen A. A., Kumaş M.

Bezmiâlem Science, vol.8, pp.79-83, 2020 (ESCI)

  • Publication Type: Article / Review
  • Volume: 8
  • Publication Date: 2020
  • Doi Number: 10.14235/bas.galenos.2020.4756
  • Journal Name: Bezmiâlem Science
  • Journal Indexes: Emerging Sources Citation Index (ESCI), TR DİZİN (ULAKBİM)
  • Page Numbers: pp.79-83
  • Bezmialem Vakıf University Affiliated: Yes


Several repurposing drugs and ongoing vaccine researches to

combat Coronavirus Disease-19 (COVID-19) are testing clinically,

worldwide. COVID-19 caused by severe acute respiratory failure

syndrome-CoV-2, uses angiotensin-converting enzyme 2 (ACE-

2) as a functional receptor for entry into the cells, followed by its

priming by transmembrane protease serine 2 (TMPRSS2). Most of

the ACE-2 expressing cells are alveolar type II pneumocytes. Viral

S-glycoprotein, TMPRSS2 and ACE-2 inhibition, as extracellular

media components, are potential targets of future therapy. ACE-

2 and/or TMPRSS2 blockade is thought to be beneficial in the

prevention or treating of this infection which will be the most

convenient for pharmacoeconomics and effectiveness, regarding

similar future pandemics. Despite substrate-based design and

synthesis of ACE-2 inhibitor compounds were presented almost

two decades ago, data on renin angiotensin system activation or

its blockers, especially ACE-2, are limited by now. Priority must

be given to design a convenient vaccine soon, but due to the high

mutation ability of such viruses mean that new vaccines may need

to be developed for each outbreak. So, de novo drugs such as ACE-2

or TMPRSS2 blockers need to be developed which can specifically

block spike binding sites of the target cells and prevent virus

intrusion, especially at the extracellular media, for future pandemics.