Constitutional Dynamic Inhibition/Activation of Carbonic Anhydrases

Dandan Su (1, 2) , Yan Zhang (3) , Sébastien Ulrich (2) , Mihail Barboiu (1, 2)

1 IEM - Institut Européen des membranes
2 IBMM - Institut des Biomolécules Max Mousseron [Pôle Chimie Balard]
3 Jiangnan University

As one important member of metalloenzymes family, carbonic anhydrase (CA) is involved in the treatment of several diseases. Different approaches have therefore emerged to regulate the activity of CA, mostly acting on inner catalytic active site or outer microenvironment of the enzyme, leading to inhibition or activation of CA. In recent years, gradually increased attentions have been drawn into the adoption of constitutional dynamic chemistry (CDC) strategies for the screening and discovery of potent inhibitors or activators. The participation of reversible covalent bonds enabled the enzyme itself to select the optimal ligands obtained from diverse building blocks with comparatively higher degree of variety, resulting in the fittest recognition of enzyme ligands from complex dynamic systems. With the increasing implantation of CDC for enzyme target, it shows great potentials for the drug discovery-or environmental-oriented applications.

Mots clés: Constitutional Dynamic Chemistry; Carbonic Anhydrase; Constitutional Frameworks; Constitutional Dynamic Chemistry

Domaines: Chimie thérapeutique; Biochimie [q-bio.BM]

Dandan Su, Yan Zhang, Sébastien Ulrich, Mihail Barboiu. Constitutional Dynamic Inhibition/Activation of Carbonic Anhydrases. ChemPlusChem, 2021, 86 (11), pp.1500-1510. ⟨10.1002/cplu.202100263⟩. ⟨hal-03749310⟩