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A small-molecule inhibitor of skeletal muscle myosin II.
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- Additional Information
- Source:
Publisher: Macmillan Magazines Ltd Country of Publication: England NLM ID: 100890575 Publication Model: Print Cited Medium: Print ISSN: 1465-7392 (Print) Linking ISSN: 14657392 NLM ISO Abbreviation: Nat Cell Biol Subsets: MEDLINE
- Publication Information:
Original Publication: London : Macmillan Magazines Ltd., [1999-
- Subject Terms:
- Abstract:
We screened a small-molecule library for inhibitors of rabbit muscle myosin II subfragment 1 (S1) actin-stimulated ATPase activity. The best inhibitor, N-benzyl-p-toluene sulphonamide (BTS), an aryl sulphonamide, inhibited the Ca2+-stimulated S1 ATPase, and reversibly blocked gliding motility. Although BTS does not compete for the nucleotide-binding site of myosin, it weakens myosin's interaction with F-actin. BTS reversibly suppressed force production in skinned skeletal muscle fibres from rabbit and frog skin at micromolar concentrations. BTS suppressed twitch production of intact frog fibres with minimum alteration of Ca2+ metabolism. BTS is remarkably specific, as it was much less effective in suppressing contraction in rat myocardial or rabbit slow-twitch muscle, and did not inhibit platelet myosin II. The isolation of BTS and the recently discovered Eg5 kinesin inhibitor, monastrol, suggests that motor proteins may be potential targets for therapeutic applications.
- Grant Information:
GM23928 United States GM NIGMS NIH HHS; GM62566 United States GM NIGMS NIH HHS; HL15835 United States HL NHLBI NIH HHS; NS17620 United States NS NINDS NIH HHS
- Accession Number:
0 (Enzyme Inhibitors)
0 (Molecular Motor Proteins)
0 (Myosin Subfragments)
0 (N-benzyl-p-toluene sulfonamide)
0 (Peptide Library)
0 (Sulfonamides)
3FPU23BG52 (Toluene)
EC 3.6.1.- (Adenosine Triphosphatases)
EC 3.6.1.- (Skeletal Muscle Myosins)
SY7Q814VUP (Calcium)
- Publication Date:
Date Created: 20011218 Date Completed: 20020125 Latest Revision: 20141120
- Publication Date:
20231215
- Accession Number:
10.1038/ncb734
- Accession Number:
11744924
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