TY - JOUR
T1 - Preparation and Application of a Chemical Probe for Identifying the Targets of the Marine Cyclic Peptide Kapakahine A
AU - Kamihira, Rie
AU - Nakao, Yoichi
N1 - Funding Information:
Funding: This research was funded by JSPS KAKENHI Grant Numbers 21H02073 and 26221204, and the Waseda University Grants for Special Research Projects 2020C-776.
Publisher Copyright:
© 2022 by the authors. Licensee MDPI, Basel, Switzerland.
PY - 2022/2/1
Y1 - 2022/2/1
N2 - Marine organisms are a rich source of bioactive secondary metabolites. Although many marine natural products with bioactivities have been isolated, successful elucidation of their mechanisms of action remains limited. In this study, we prepared a probe molecule based on the marine cyclic peptide kapakahine A (1) by introducing a linker with an azide terminal group, which enables the introduction of fluorescent groups for the effective monitoring of subcellular localization, or coupling to affinity beads for the pull-down of target proteins. The results of LC/MS/MS measure-ments, ProteinPilot analysis, and Western blotting suggest that kapakahine A interacts with the mi-tochondrial inner membrane proteins PHB1, PHB2, and ANT2, which is consistent with the results of the subcellular localization analysis using a fluorescent probe.
AB - Marine organisms are a rich source of bioactive secondary metabolites. Although many marine natural products with bioactivities have been isolated, successful elucidation of their mechanisms of action remains limited. In this study, we prepared a probe molecule based on the marine cyclic peptide kapakahine A (1) by introducing a linker with an azide terminal group, which enables the introduction of fluorescent groups for the effective monitoring of subcellular localization, or coupling to affinity beads for the pull-down of target proteins. The results of LC/MS/MS measure-ments, ProteinPilot analysis, and Western blotting suggest that kapakahine A interacts with the mi-tochondrial inner membrane proteins PHB1, PHB2, and ANT2, which is consistent with the results of the subcellular localization analysis using a fluorescent probe.
KW - Chemical biology
KW - Chemical fluorescent probe
KW - Cyclic peptide
KW - Marine natural product
KW - Target protein
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U2 - 10.3390/molecules27031072
DO - 10.3390/molecules27031072
M3 - Article
C2 - 35164336
AN - SCOPUS:85124213841
SN - 1420-3049
VL - 27
JO - Molecules
JF - Molecules
IS - 3
M1 - 1072
ER -