Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 52, Issue 20, Pages 6197-6200Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm901233u
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Funding
- European Union
- Royal Thai Government
- Biotechnology and Biological Sciences Research Council (BBSRC), U.K.
- BBSRC [BB/D02014X/1] Funding Source: UKRI
- Biotechnology and Biological Sciences Research Council [BB/D02014X/1] Funding Source: researchfish
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MCoTI-lI is a member of a class of microproteins known as cyclotides that possess a macrolactam-cystine knot scaffold imparting exceptional physiological stability and structural rigidity. Modification of residues in the active loop and engineered truncations have resulted in MCoTI-II analogues that possess potent activity against two therapeutically significant serine proteases: beta-tryptase and human leukocyte elastase. These results suggest that MCoTI-II is a versatile scaffold for the development of protease inhibitors against targets in inflammatory disease.
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