ArticleOncotarget2012
"Picolog," a synthetically-available bryostatin analog, inhibits growth of MYC-induced lymphoma in vivo.
Article in Oncotarget, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
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
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
18 citing papers in PubMed, 36 citations in OpenAlex.
- Bryostatin 1 Promotes Synaptogenesis and Reduces Dendritic Spine Density in Cortical Cultures through a PKC-Dependent Mechanism.ACS chemical neuroscience · 2020Article
- The Phylum Bryozoa as a Promising Source of Anticancer Drugs.Marine drugs · 2019Review
- The 'Achilles Heel' of Metabolism in Renal Cell Carcinoma: Glutaminase Inhibition as a Rational Treatment Strategy.Kidney cancer (Clifton, Va.) · 2019Review
- Review of bioactive secondary metabolites from marine bryozoans in the progress of new drugs discovery.Future medicinal chemistry · 2018Review
- Deletion of the C26 Methyl Substituent from the Bryostatin Analogue Merle 23 Has Negligible Impact on Its Biological Profile and Potency.Chembiochem : a European journal of chemical biology · 2018Article
- Chemoenzymatic Dissection of Polyketide β-Branching in the Bryostatin Pathway.Methods in enzymology · 2018Article
- Protein kinase C in cancer: The top five unanswered questions.Molecular carcinogenesis · 2017Review
- Evaluation of Chromane-Based Bryostatin Analogues Prepared via Hydrogen-Mediated C-C Bond Formation: Potency Does Not Confer Bryostatin-like Biology.Journal of the American Chemical Society · 2016Article
- Capturing Biological Activity in Natural Product Fragments by Chemical Synthesis.Angewandte Chemie (International ed. in English) · 2016Review
- Capillary nano-immunoassays: advancing quantitative proteomics analysis, biomarker assessment, and molecular diagnostics.Journal of translational medicine · 2015Review
- Toward a biorelevant structure of protein kinase C bound modulators: design, synthesis, and evaluation of labeled bryostatin analogues for analysis with rotational echo double resonance NMR spectroscopy.Journal of the American Chemical Society · 2015Article
- Function through synthesis-informed design.Accounts of chemical research · 2015Article
- Synthesis of seco-B-ring bryostatin analogue WN-1 via C-C bond-forming hydrogenation: critical contribution of the B-ring in determining bryostatin-like and phorbol 12-myristate 13-acetate-like properties.Journal of the American Chemical Society · 2014Article
- Neurotrophic natural products: chemistry and biology.Angewandte Chemie (International ed. in English) · 2014Review
- Real-time nanoscale proteomic analysis of the novel multi-kinase pathway inhibitor rigosertib to measure the response to treatment of cancer.Expert opinion on investigational drugs · 2013Review
- Mechanistic and computational studies of exocyclic stereocontrol in the synthesis of bryostatin-like cis-2,6-disubstituted 4-alkylidenetetrahydropyrans by Prins cyclization.The Journal of organic chemistry · 2013Article
- Designed, synthetically accessible bryostatin analogues potently induce activation of latent HIV reservoirs in vitro.Nature chemistry · 2012Article
- Bryostatin analog: improving on Nature's design.Oncotarget · 2012Article
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
Bryostatin 1 is a naturally occurring complex macrolide with potent anti-neoplastic activity. However, its extremely low natural occurrence has impeded clinical advancement. We developed a strategy directed at the design of simplified and synthetically more accessible bryostatin analogs. Our lead analog, "picolog", can be step-economically produced. Picolog, compared to bryostatin, exhibited superior growth inhibition of MYC-induced lymphoma in vitro. A key mechanism of picolog's (and bryostatin's) activity is activation of PKC. A novel nano-immunoassay (NIA) revealed that picolog treatment increased phospho-MEK2 in the PKC pathway. Moreover, the inhibition of PKC abrogated picolog's activity. Finally, picolog was highly potent at 100 micrograms/kg and well tolerated at doses ranging from 100 micrograms/kg to 1 milligram/kg in vivo for the treatment of our aggressive model of MYC-induced lymphoma. We provide the first in vivo validation that the bryostatin analog, picolog, is a potential therapeutic agent for the treatment of cancer and other diseases.
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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.