BC-LI-0186 is a compound that acts as an
inhibitor
Inhibitor or inhibition may refer to:
In biology
* Enzyme inhibitor, a substance that binds to an enzyme and decreases the enzyme's activity
* Reuptake inhibitor, a substance that increases neurotransmission by blocking the reuptake of a neurotra ...
of the
GTPase enzyme
Enzymes () are proteins that act as biological catalysts by accelerating chemical reactions. The molecules upon which enzymes may act are called substrates, and the enzyme converts the substrates into different molecules known as products. A ...
leucyl-tRNA synthetase
Leucyl-tRNA synthetase, cytoplasmic is an enzyme that in humans is encoded by the ''LARS'' gene.
Function
This gene encodes a cytosolic leucine-tRNA synthetase, a member of the class I aminoacyl-tRNA synthetase family. The encoded enzyme catal ...
(LRS). This enzyme acts as part of the
mTOR
The mammalian target of sirolimus, rapamycin (mTOR), also referred to as the mechanistic target of rapamycin, and sometimes called FK506-binding protein 12-rapamycin-associated protein 1 (FRAP1), is a kinase that in humans is encoded by the ''MT ...
complex and acts as a
leucine sensor which stimulates
mTORC1
mTORC1, also known as mammalian target of rapamycin complex 1 or mechanistic target of rapamycin complex 1, is a protein complex that functions as a nutrient/energy/redox sensor and controls protein synthesis.
mTOR Complex 1 (mTORC1) is compo ...
in the presence of leucine. BC-LI-0186 blocks the docking site for mTORC1 and thereby prevents the mTOR activation and increased protein synthesis which is usually triggered by
branched-chain amino acids
A branched-chain amino acid (BCAA) is an amino acid having an aliphatic side-chain with a branch (a central carbon atom bound to three or more carbon atoms). Among the proteinogenic amino acids, there are three BCAAs: leucine, isoleucine, and va ...
such as leucine, yet without inhibiting the separate catalytic activity of LRS. This may have potential applications in the treatment of
cancer
Cancer is a group of diseases involving abnormal cell growth with the potential to invade or spread to other parts of the body. These contrast with benign tumors, which do not spread. Possible signs and symptoms include a lump, abnormal b ...
, and BC-LI-0186 has also been shown to promote muscle regeneration after injury.
References
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Enzyme inhibitors
Pyrazoles
Sulfonamides