BC-LI-0186

BC-LI-0186 is a compound that acts as an inhibitor of the GTPase enzyme leucyl-tRNA synthetase (LRS). This enzyme acts as part of the mTOR complex and acts as a leucine sensor which stimulates mTORC1 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 such as leucine, yet without inhibiting the separate catalytic activity of LRS.[1] This may have potential applications in the treatment of cancer,[2] and BC-LI-0186 has also been shown to promote muscle regeneration after injury.[3]

BC-LI-0186
Identifiers
CAS Number
PubChem CID
ChemSpider
Chemical and physical data
FormulaC22H27N3O4S
Molar mass429.54 g·mol−1
3D model (JSmol)

References

  1. Kim JH, Lee C, Lee M, Wang H, Kim K, Park SJ, et al. (September 2017). "Control of leucine-dependent mTORC1 pathway through chemical intervention of leucyl-tRNA synthetase and RagD interaction". Nature Communications. 8 (1): 732. doi:10.1038/s41467-017-00785-0. PMID 28963468.
  2. Kim EY, Lee JG, Lee JM, Kim A, Yoo HC, Kim K, et al. "Therapeutic effects of the novel Leucyl-tRNA synthetase inhibitor BC-LI-0186 in non-small cell lung cancer". Therapeutic Advances in Medical Oncology. 11: 1758835919846798. doi:10.1177/1758835919846798. PMID 31205503.
  3. Son K, You JS, Yoon MS, Dai C, Kim JH, Khanna N, et al. (April 2019). "Nontranslational function of leucyl-tRNA synthetase regulates myogenic differentiation and skeletal muscle regeneration". The Journal of Clinical Investigation. 129 (5): 2088–2093. doi:10.1172/JCI122560. PMID 30985292.
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