期刊
NATURE CHEMISTRY
卷 9, 期 8, 页码 731-742出版社
NATURE PUBLISHING GROUP
DOI: 10.1038/NCHEM.2814
关键词
-
资金
- Natural Science and Engineering Research Council (NSERC)
- Canadian Institutes of Health Research (CIHR)
- NSERC
Boron-containing molecules have been extensively used for the purposes of chemical sensing, biological probe development and drug discovery. Due to boron's empty p orbital, it can coordinate to heteroatoms such as oxygen and nitrogen. This reversible covalent mode of interaction has led to the use of boron as bait for nucleophilic residues in disease-associated proteins, culminating in the approval of new therapeutics that work by covalent mechanisms. Our analysis of a wide range of covalent inhibitors with electrophilic groups suggests that boron is a unique electrophile in its chameleonic ability to engage protein targets. Here we review boron's interactions with a range of protein side-chain residues and reveal that boron's properties are nuanced and arise from its uncommon coordination preferences. These mechanistic and structural insights should serve as a guide for the development of selective boron-based bioactive molecules.
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