The versatility of boron in biological target engagement.
In: Nature chemistry, Jg. 9 (2017-07-25), Heft 8, S. 731-742
academicJournal
Zugriff:
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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The versatility of boron in biological target engagement.
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Autor/in / Beteiligte Person: | Diaz, DB ; Yudin, AK |
Zeitschrift: | Nature chemistry, Jg. 9 (2017-07-25), Heft 8, S. 731-742 |
Veröffentlichung: | London : Nature Pub. Group, 2017 |
Medientyp: | academicJournal |
ISSN: | 1755-4349 (electronic) |
DOI: | 10.1038/nchem.2814 |
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