|[Eucuragen]PEG-BHD1028 Peptide Regulates Insulin Resistance and Fatty|
|작성자 : 관리자(firstname.lastname@example.org) 작성일 : 21.04.01 조회수 : 19|
|첨부파일 : 엔큐라젠논문(2nd)_PEG-BHD1028 Peptide Regulates Insulin Resistance and Fatty.pdf|
PEG-BHD1028 Peptide Regulates Insulin Resistance and Fatty Acid β-Oxidation, and Mitochondrial Biogenesis by Binding to Two Heterogeneous Binding Sites of Adiponectin Receptors, AdipoR1 and AdiopR2
In Kyung Lee, Gyuyoup Kim, Do-Hwi Kim and Brian B. Kim
Adiponectin plays multiple critical roles in modulating various physiological processes
by binding to its receptors. The functions of PEG-BHD1028, a potent novel peptid
agonist to AdipoRs, was evaluated using in vitro and in vivo models based on the
reported action spectrum of adiponectin. To confirm the design concept of
PEG-BHD1028, the binding sites and their affinities were analyzed using the SPR( Surface
Plasmon Resonance) assay. The results revealed that PEG-BHD1028 was bound to two
heterogeneous binding sites of AdipoR1 and AdipoR2 with a relatively high affinity. In
C2C12 cells, PEG-BHD1028 significantly activated AMPK and subsequent pathways and
enhanced fatty acid β-oxidation and mitochondrial biogenesis. Furthermore, it also
facilitated glucose uptake by lowering insulin resistance in insulin-resistant C2C12 cells.
PEG_BHD1028 significantly reduced the fasting plasma glucose level in db/db mice
following a single s.c. injection of 50, 100, and 200 ug/Kg and glucose tolerance at a
dose of 50 ug/Kg with significantly decreased insulin production.
The animals received 5, 25, and 50 ug/Kg of PEG-BHD1028 for 21days significantly lost their weight after 18days in a range of 5-7%.
These results imply the development of PEG_BHD1028 as a potential adiponectin replacement therapeutic agent.
*자세한 사항은 첨부파일 참고 부탁드립니다.*
|다음글||[PLOS ONE] Discovery of a novel potent peptide agonist to adiponectin receptor 1|