Protein phosphatase inhibitory activity of tautomycin photoaffinity probes evaluated at femto-molar level.

Protein phosphatase inhibitory activity of tautomycin photoaffinity probes evaluated at femto-molar level. Research Abstract Details 

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Protein phosphatase inhibitory activity of tautomycin photoaffinity probes evaluated at femto-molar level. Abstract Text:

Magne O Sydnes,Masaki Kuse,Masakuni Kurono,Aya Shimomura,Hiroshi Ohinata,Akira Takai,Minoru Isobe,Magne O Sydnes,Masaki Kuse,Masakuni Kurono,Aya Shimomura,Hiroshi Ohinata,Akira Takai,Minoru Isobe,

Herein we describe the further improvement of our in-house developed firefly bioluminescence assay system for the determination of inhibition of protein phosphatase (PP). The advantage with the new system is higher sensitivity as well as being time and sample efficient. The inhibition activity of tautomycin with PP1gamma was determined using the upgraded test system and K(i) was found to be 4.5nM, which compare favorably with the activity reported previously by others using different methods. The test system was then used in order to determine the activity of nine tautomycin (TTM) photoaffinity probes. One of the TTM photoaffinity probes (anti-10) was found to possess higher activity than the natural product itself with a K(i) of 3.4nM, while the remaining photoaffinity probes were found to possess K(i) in the range of 8.0-213nM.

Protein phosphatase inhibitory activity of tautomycin photoaffinity probes evaluated at femto-molar level. Publishing Authors By Initials

MO Sydnes,M Kuse,M Kurono,A Shimomura,H Ohinata,A Takai,M Isobe,MO Sydnes,M Kuse,M Kurono,A Shimomura,H Ohinata,A Takai,M Isobe,

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Protein phosphatase inhibitory activity of tautomycin photoaffinity probes evaluated at femto-molar level. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: Bioorganic & medicinal chemistry

VOLUME: 16

Page Numbers: 1747-55

Journal Abbreviation: Bioorg. Med. Chem.

ISSN: 1464-3391

DAY: 17

MONTH: 11

YEAR: 2007

Protein phosphatase inhibitory activity of tautomycin photoaffinity probes evaluated at femto-molar level. Information

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LANGUAGE: eng

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Grant and Affiliation Information for Protein phosphatase inhibitory activity of tautomycin photoaffinity probes evaluated at femto-molar level.

AFFILIATION: Laboratory of Organic Chemistry, Graduate School of Bioagricultural Sciences, Nagoya University, Furo-cho, Chikusa, Nagoya 464-8601, Japan.

Country: England

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MEDLINETA: Bioorg Med Chem

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