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A Boronic Acid Conjugate of Angiogenin that Shows ROS‐Responsive Neuroprotective Activity
Author(s) -
Hoang Trish T.,
Smith Thomas P.,
Raines Ronald T.
Publication year - 2017
Publication title -
angewandte chemie
Language(s) - English
Resource type - Journals
eISSN - 1521-3757
pISSN - 0044-8249
DOI - 10.1002/ange.201611446
Subject(s) - angiogenin , neuroprotection , oxidative stress , chemistry , neurodegeneration , reactive oxygen species , boronic acid , angiogenesis , pharmacology , biochemistry , conjugate , microbiology and biotechnology , cancer research , combinatorial chemistry , biology , medicine , disease , mathematical analysis , mathematics
Angiogenin (ANG) is a human ribonuclease that is compromised in patients with amyotrophic lateral sclerosis (ALS). ANG also promotes neovascularization, and can induce hemorrhage and encourage tumor growth. The causal neurodegeneration of ALS is associated with reactive oxygen species, which are also known to elicit the oxidative cleavage of carbon–boron bonds. We have developed a synthetic boronic acid mask that restrains the ribonucleolytic activity of ANG. The masked ANG does not stimulate endothelial cell proliferation but protects astrocytes from oxidative stress. By differentiating between the two dichotomous biological activities of ANG, this strategy could provide a viable pharmacological approach for the treatment of ALS.