Peptide substrates for Rho-associated kinase 2 (Rho-kinase 2/ROCK2).

Peptide substrates sensitive for a certain protein kinase could be important for new-drug development and to understand the mechanism of diseases. Rho-associated kinase (Rho-kinase/ROCK) is a serine/threonine kinase, and plays an important part in cardiovascular disease, migration and invasion of tu...

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Autores principales: Jeong-Hun Kang, Daisuke Asai, Akira Tsuchiya, Takeshi Mori, Takuro Niidome, Yoshiki Katayama
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Publicado: Public Library of Science (PLoS) 2011
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Acceso en línea:https://doaj.org/article/43f0dbc4b13144f7803a6986d93cbd81
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spelling oai:doaj.org-article:43f0dbc4b13144f7803a6986d93cbd812021-11-18T06:49:15ZPeptide substrates for Rho-associated kinase 2 (Rho-kinase 2/ROCK2).1932-620310.1371/journal.pone.0022699https://doaj.org/article/43f0dbc4b13144f7803a6986d93cbd812011-01-01T00:00:00Zhttps://www.ncbi.nlm.nih.gov/pmc/articles/pmid/21818369/pdf/?tool=EBIhttps://doaj.org/toc/1932-6203Peptide substrates sensitive for a certain protein kinase could be important for new-drug development and to understand the mechanism of diseases. Rho-associated kinase (Rho-kinase/ROCK) is a serine/threonine kinase, and plays an important part in cardiovascular disease, migration and invasion of tumor cells, and in neurological disorders. The purpose of this study was to find substrates with high affinity and sensitivity for ROCK2. We synthesized 136 peptide substrates from protein substrates for ROCK2 with different lengths and charged peptides. Incorporation of (32)P [counts per minute (CPM)] for each peptide substrate was determined by the radiolabel assay using [γ-(32)P]ATP. When the top five peptide substrates showing high CPMs (R4, R22, R133, R134, and R135) were phosphorylated by other enzymes (PKA, PKCα, and ERK1), R22, R133, and R135 displayed the highest CPM level for ROCK2 compared with other enzymes, whereas R4 and R134 showed similar CPM levels for ROCK2 and PKCα. We hypothesize that R22, R133, and R135 can be useful peptide substrates for ROCK2.Jeong-Hun KangDaisuke AsaiAkira TsuchiyaTakeshi MoriTakuro NiidomeYoshiki KatayamaPublic Library of Science (PLoS)articleMedicineRScienceQENPLoS ONE, Vol 6, Iss 7, p e22699 (2011)
institution DOAJ
collection DOAJ
language EN
topic Medicine
R
Science
Q
spellingShingle Medicine
R
Science
Q
Jeong-Hun Kang
Daisuke Asai
Akira Tsuchiya
Takeshi Mori
Takuro Niidome
Yoshiki Katayama
Peptide substrates for Rho-associated kinase 2 (Rho-kinase 2/ROCK2).
description Peptide substrates sensitive for a certain protein kinase could be important for new-drug development and to understand the mechanism of diseases. Rho-associated kinase (Rho-kinase/ROCK) is a serine/threonine kinase, and plays an important part in cardiovascular disease, migration and invasion of tumor cells, and in neurological disorders. The purpose of this study was to find substrates with high affinity and sensitivity for ROCK2. We synthesized 136 peptide substrates from protein substrates for ROCK2 with different lengths and charged peptides. Incorporation of (32)P [counts per minute (CPM)] for each peptide substrate was determined by the radiolabel assay using [γ-(32)P]ATP. When the top five peptide substrates showing high CPMs (R4, R22, R133, R134, and R135) were phosphorylated by other enzymes (PKA, PKCα, and ERK1), R22, R133, and R135 displayed the highest CPM level for ROCK2 compared with other enzymes, whereas R4 and R134 showed similar CPM levels for ROCK2 and PKCα. We hypothesize that R22, R133, and R135 can be useful peptide substrates for ROCK2.
format article
author Jeong-Hun Kang
Daisuke Asai
Akira Tsuchiya
Takeshi Mori
Takuro Niidome
Yoshiki Katayama
author_facet Jeong-Hun Kang
Daisuke Asai
Akira Tsuchiya
Takeshi Mori
Takuro Niidome
Yoshiki Katayama
author_sort Jeong-Hun Kang
title Peptide substrates for Rho-associated kinase 2 (Rho-kinase 2/ROCK2).
title_short Peptide substrates for Rho-associated kinase 2 (Rho-kinase 2/ROCK2).
title_full Peptide substrates for Rho-associated kinase 2 (Rho-kinase 2/ROCK2).
title_fullStr Peptide substrates for Rho-associated kinase 2 (Rho-kinase 2/ROCK2).
title_full_unstemmed Peptide substrates for Rho-associated kinase 2 (Rho-kinase 2/ROCK2).
title_sort peptide substrates for rho-associated kinase 2 (rho-kinase 2/rock2).
publisher Public Library of Science (PLoS)
publishDate 2011
url https://doaj.org/article/43f0dbc4b13144f7803a6986d93cbd81
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