Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 54, Issue 5, Pages 1170-1177Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm101284a
Keywords
-
Categories
Funding
- European Union
- CNRS, Centre National de la Recherche Scientifique, France
Ask authors/readers for more resources
Lipoic acid moieties were attached to amine or amino acids showing activating properties against the zinc enzyme carbonic anhydrase (CA, EC 4.2.1.1). The obtained lipoic acid conjugates of histamine, L-histidine methyl ester, and L-carnosine methyl ester were attached to gold nanoparticles (NPs) by reaction with Au(III) salts in reducing conditions. The CA activators (CAAs) coated NPs showed low nanomolar activation (K(A)s of 1-9 nM) of relevant cytosolic, membrane-bound, mitochondrial, and transmembrane CA isoforms, such as CA I, II, IV, VA, VII, and XIV. These NPs also effectively activated CAs ex vivo., in whole blood experiments, with an increase of 200-280% of the CA activity. This is the first example of enzyme activation with nanoparticles and may lead to biomedical applications for condition in which the CA activity is diminished, such as aging, Alzheimer's disease, or CA deficiency syndrome.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available