ArticleACS medicinal chemistry letters2011
Synthesis and Structure-Activity Relationships of Benzothienothiazepinone Inhibitors of Protein Kinase D.
Article in ACS medicinal chemistry letters, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
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Who cites it
22 citing papers in PubMed, 43 citations in OpenAlex.
- Protein Kinase D2 Regulates GRASP65 Phosphorylation and Golgi Ribbon Unlinking During G2/M Transition.Cells · 2026Article
- Potential role for protein kinase D inhibitors in prostate cancer.Journal of molecular medicine (Berlin, Germany) · 2023Review
- Small Molecule Inhibitors of Protein Kinase D: Early Development, Current Approaches, and Future Directions.Journal of medicinal chemistry · 2023Review
- Multifaceted Functions of Protein Kinase D in Pathological Processes and Human Diseases.Biomolecules · 2021Review
- Discovery of the Hedgehog Pathway Inhibitor Pipinib that Targets PI4KIIIß.Angewandte Chemie (International ed. in English) · 2019Review
- PKD1 is a potential biomarker and therapeutic target in triple-negative breast cancer.Oncotarget · 2018Article
- Protein kinase D signaling in cancer: A friend or foe?Biochimica et biophysica acta. Reviews on cancer · 2017Review
- Protein kinase D promotes plasticity-induced F-actin stabilization in dendritic spines and regulates memory formation.The Journal of cell biology · 2015Article
- A computational model of PKD and CERT interactions at the trans-Golgi network of mammalian cells.BMC systems biology · 2015Article
- Article
- An uncharged oxetanyl sulfoxide as a covalent modifier for improving aqueous solubility.ACS medicinal chemistry letters · 2014Article
- Antiproliferative activities of halogenated thieno[3,2-d]pyrimidines.Bioorganic & medicinal chemistry · 2014Article
- Sustained protein kinase D activation mediates respiratory syncytial virus-induced airway barrier disruption.Journal of virology · 2013Article
- Article
- In vitro cytotoxicity, pharmacokinetics, tissue distribution, and metabolism of small-molecule protein kinase D inhibitors, kb-NB142-70 and kb-NB165-09, in mice bearing human cancer xenografts.Cancer chemotherapy and pharmacology · 2013Article
- New pyrazolopyrimidine inhibitors of protein kinase d as potent anticancer agents for prostate cancer cells.PloS one · 2013Article
- Inducible silencing of protein kinase D3 inhibits secretion of tumor-promoting factors in prostate cancer.Molecular cancer therapeutics · 2012Article
- A bifunctional dimethylsulfoxide substitute enhances the aqueous solubility of small organic molecules.Assay and drug development technologies · 2012Article
- Article
- A protein kinase C/protein kinase D pathway protects LNCaP prostate cancer cells from phorbol ester-induced apoptosis by promoting ERK1/2 and NF-{kappa}B activities.Carcinogenesis · 2011Article
Corrections and comments
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Authors and funding
10 authors at 2 institutions in 1 country.
Funding
Abstract
Protein kinase D (PKD) is a member of a novel family of serine/threonine kinases that regulate fundamental cellular processes. PKD is implicated in the pathogenesis of several diseases, including cancer. Progress in understanding the biological functions and therapeutic potential of PKD has been hampered by the lack of specific inhibitors. The benzoxoloazepinolone CID755673 was recently identified as the first potent and selective PKD inhibitor. The study of structure-activity relationships (SAR) of this lead structure led to further improvements in PKD1 potency. We describe herein the synthesis and biological evaluation of novel benzothienothiazepinone analogs. We achieved a ten-fold increase in the in vitro PKD1 inhibitory potency for the second generation lead kb-NB142-70 and accomplished a transition to an almost equally potent novel pyrimidine scaffold, while maintaining excellent target selectivity. These promising results will guide the design of pharmacological tools to dissect PKD function and pave the way for the development of potential anti-cancer agents.
Identifiers
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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.