title: Identification of a molecular target of kurahyne, an apoptosis-inducing lipopeptide from marine cyanobacterial assemblages.
abstract: In 2014, we isolated kurahyne, an acetylene-containing lipopeptide, from a marine cyanobacterial assemblage of Lyngbya sp. Kurahyne exhibited growth-inhibitory activity against human cancer cells, and induced apoptosis in HeLa cells. However, its mode of action is not yet clear. To elucidate its mode of action, we carried out several cell-based assays, and identified the intracellular target molecule of kurahyne as sarco/endoplasmic reticulum Ca(2+) ATPase (SERCA). In addition, we found that kurahyne inhibited the differentiation of macrophages into osteoclasts.
authors.affiliation: Department of Chemistry, Keio University, 3-14-1 Hiyoshi, Yokohama, Kanagawa 223-8522, Japan.
authors.forename: Arihiro
authors.initials: A
authors.lastname: Iwasaki
authors.affiliation: School of Advanced Engineering, Kogakuin University, 2665-1 Nakanocho, Hachioji, Tokyo 192-0015, Japan.
authors.forename: Osamu
authors.initials: O
authors.lastname: Ohno
authors.affiliation: Department of Applied Chemistry, Keio University, 3-14-1 Hiyoshi, Yokohama, Kanagawa 223-8522, Japan.
authors.forename: Shun
authors.initials: S
authors.lastname: Katsuyama
authors.affiliation: Institute of Molecular and Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan.
authors.forename: Maho
authors.initials: M
authors.lastname: Morita
authors.affiliation: Department of Applied Chemistry, Keio University, 3-14-1 Hiyoshi, Yokohama, Kanagawa 223-8522, Japan.
authors.forename: Yukiko
authors.initials: Y
authors.lastname: Sasazawa
authors.affiliation: Cancer Chemotherapy Center, Japanese Foundation for Cancer Research, 3-8-31 Ariake, Koto-ku, Tokyo 135-8550, Japan.
authors.forename: Shingo
authors.initials: S
authors.lastname: Dan
authors.affiliation: Department of Applied Chemistry, Keio University, 3-14-1 Hiyoshi, Yokohama, Kanagawa 223-8522, Japan.
authors.forename: Siro
authors.initials: S
authors.lastname: Simizu
authors.affiliation: Cancer Chemotherapy Center, Japanese Foundation for Cancer Research, 3-8-31 Ariake, Koto-ku, Tokyo 135-8550, Japan.
authors.forename: Takao
authors.initials: T
authors.lastname: Yamori
authors.affiliation: Department of Chemistry, Keio University, 3-14-1 Hiyoshi, Yokohama, Kanagawa 223-8522, Japan. Electronic address: suenaga@chem.keio.ac.jp.
authors.forename: Kiyotake
authors.initials: K
authors.lastname: Suenaga
mesh_terms: D000345:Affinity Labels / Q000737:chemistry; D000480:Alkynes / Q000737:chemistry / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis; D002118:Calcium / Q000378:metabolism; D002454:Cell Differentiation / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D000091342:Endoplasmic Reticulum Chaperone BiP; D059865:Endoplasmic Reticulum Stress / Q000187:drug effects; D006367:HeLa Cells; D006360:Heat-Shock Proteins / Q000235:genetics / Q000378:metabolism; D006801:Humans; D055666:Lipopeptides / Q000737:chemistry / Q000494:pharmacology*; D008264:Macrophages / Q000166:cytology / Q000187:drug effects; D054300:Oscillatoria / Q000737:chemistry*; D010010:Osteoclasts / Q000166:cytology / Q000187:drug effects; D053498:Sarcoplasmic Reticulum Calcium-Transporting ATPases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D051742:Transcription Factor CHOP / Q000235:genetics / Q000378:metabolism; D015533:Transcriptional Activation
chemical_list: D000345:Affinity Labels; D000480:Alkynes; D000970:Antineoplastic Agents; C497249:DDIT3 protein, human; D000091342:Endoplasmic Reticulum Chaperone BiP; D006360:Heat-Shock Proteins; D055666:Lipopeptides; D051742:Transcription Factor CHOP; D053498:Sarcoplasmic Reticulum Calcium-Transporting ATPases; D002118:Calcium
keywords: Apoptosis; ER stress; Kurahyne; Marine natural product; SERCA