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[35S]GTP gamma S binding studies of amphiphilic drugs-activated Gi proteins: a caveat.

Abstract：

:This paper documents a serious problem met during the testing of Gi protein-activating properties of a new series of synthetic compounds by measuring the induced binding of [(35)S]GTPgammaS to different subtypes of Gi protein. The problem arose from the strong affinity between [(35)S]GTPgammaS and the tested compounds, that are characterized by several (2-4) positive charges and high lipophilicity. Apparently, such affinity yields insoluble, labelled complexes that, also in the absence of Gi protein, are retained on the filters and give rise to false positive results.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Manetti D,Di Cesare Mannelli L,Dei S,Guandalini L,Martini E,Banchelli M,Ghelardini C

doi

10.1016/j.bmcl.2009.02.097

subject

Has Abstract

pub_date

2009-04-15 00:00:00

pages

2224-9

issue

8

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(09)00262-5

journal_volume

19

pub_type

杂志文章

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