ArticleProceedings of the National Academy of Sciences of the United States of America2016
Highly selective inhibition of myosin motors provides the basis of potential therapeutic application.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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Who cites it
23 citing papers in PubMed, 40 citations in OpenAlex.
- Article
- An allosteric inhibitor of RhoGAP class-IX myosins suppresses the metastatic features of cancer cells.Nature communications · 2024Article
- Omecamtiv mecarbil and Mavacamten target the same myosin pocket despite opposite effects in heart contraction.Nature communications · 2024Article
- A weak coupling mechanism for the early steps of the recovery stroke of myosin VI: A free energy simulation and string method analysis.PLoS computational biology · 2024Article
- Toward physics-based precision medicine: Exploiting protein dynamics to design new therapeutics and interpret variants.Protein science : a publication of the Protein Society · 2024Review
- Omecamtiv mecarbil and Mavacamten target the same myosin pocket despite antagonistic effects in heart contraction.bioRxiv : the preprint server for biology · 2023Article
- Mechanism of small molecule inhibition of Plasmodium falciparum myosin A informs antimalarial drug design.Nature communications · 2023Article
- MyosinA is a druggable target in the widespread protozoan parasite Toxoplasma gondii.PLoS biology · 2023Article
- Article
- Synthesis and Evaluation of 4-Hydroxycoumarin Imines as Inhibitors of Class II Myosins.Journal of medicinal chemistry · 2020Article
- A Semi-High-Throughput Adaptation of the NADH-Coupled ATPase Assay for Screening Small Molecule Inhibitors.Journal of visualized experiments : JoVE · 2019Article
- Plasmodium myosin A drives parasite invasion by an atypical force generating mechanism.Nature communications · 2019Article
- Three perspectives on the molecular basis of hypercontractility caused by hypertrophic cardiomyopathy mutations.Pflugers Archiv : European journal of physiology · 2019Review
- Phenamacril is a reversible and noncompetitive inhibitor ofThe Journal of biological chemistry · 2019Article
- Designed mono- and di-covalent inhibitors trap modeled functional motions for Trypanosoma cruzi proline racemase in crystallography.PLoS neglected tropical diseases · 2018Article
- Actin-Myosin Interaction: Structure, Function and Drug Discovery.International journal of molecular sciences · 2018Review
- An intermediate along the recovery stroke of myosin VI revealed by X-ray crystallography and molecular dynamics.Proceedings of the National Academy of Sciences of the United States of America · 2018Article
- Recovering Actives in Multi-Antitarget and Target Design of Analogs of the Myosin II Inhibitor Blebbistatin.Frontiers in chemistry · 2018Article
- Kinetic signatures of myosin-5B, the motor involved in microvillus inclusion disease.The Journal of biological chemistry · 2017Article
- Allosteric modulation of cardiac myosin dynamics by omecamtiv mecarbil.PLoS computational biology · 2017Article
Corrections and comments
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Authors and funding
16 authors at 4 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Direct inhibition of smooth muscle myosin (SMM) is a potential means to treat hypercontractile smooth muscle diseases. The selective inhibitor CK-2018571 prevents strong binding to actin and promotes muscle relaxation in vitro and in vivo. The crystal structure of the SMM/drug complex reveals that CK-2018571 binds to a novel allosteric pocket that opens up during the "recovery stroke" transition necessary to reprime the motor. Trapped in an intermediate of this fast transition, SMM is inhibited with high selectivity compared with skeletal muscle myosin (IC
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.