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Chemical, Biochemical, Cellular, and Physiological Characterization of Leucettinib-21, a Down Syndrome and Alzheimer's Disease Drug Candidate.
Lindberg MF, Deau E, Miege F, Greverie M, Roche D, George N, George P, Merlet L, Gavard J, Brugman SJT, Aret E, Tinnemans P, de Gelder R, Sadownik J, Verhofstad E, Sleegers D, Santangelo S, Dairou J, Fernandez-Blanco Á, Dierssen M, Krämer A, Knapp S, Meijer L. Lindberg MF, et al. J Med Chem. 2023 Dec 14;66(23):15648-15670. doi: 10.1021/acs.jmedchem.3c01888. Epub 2023 Dec 5. J Med Chem. 2023. PMID: 38051674
Leucettinibs are substituted 2-aminoimidazolin-4-ones (inspired by the marine sponge natural product Leucettamine B) developed as pharmacological inhibitors of DYRK1A (dual-specificity, tyrosine phosphorylation-regulated kinase 1A), a therapeutic target for indicati …
Leucettinibs are substituted 2-aminoimidazolin-4-ones (inspired by the marine sponge natural product Leucettamine B) developed …
Leucettinibs, a Class of DYRK/CLK Kinase Inhibitors Inspired by the Marine Sponge Natural Product Leucettamine B.
Deau E, Lindberg MF, Miege F, Roche D, George N, George P, Krämer A, Knapp S, Meijer L. Deau E, et al. J Med Chem. 2023 Aug 10;66(15):10694-10714. doi: 10.1021/acs.jmedchem.3c00884. Epub 2023 Jul 24. J Med Chem. 2023. PMID: 37487467
We here describe a family of DYRK/CLK inhibitors derived from Leucettines and the marine natural product Leucettamine B. Forty-five N2-functionalized 2-aminoimidazolin-4-ones bearing a fused [6 + 5]-heteroarylmethylene were synthesized. ...
We here describe a family of DYRK/CLK inhibitors derived from Leucettines and the marine natural product Leucettamine B. Forty …
Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors.
Tahtouh T, Durieu E, Villiers B, Bruyère C, Nguyen TL, Fant X, Ahn KH, Khurana L, Deau E, Lindberg MF, Sévère E, Miege F, Roche D, Limanton E, L'Helgoual'ch JM, Burgy G, Guiheneuf S, Herault Y, Kendall DA, Carreaux F, Bazureau JP, Meijer L. Tahtouh T, et al. J Med Chem. 2022 Jan 27;65(2):1396-1417. doi: 10.1021/acs.jmedchem.1c01141. Epub 2021 Dec 20. J Med Chem. 2022. PMID: 34928152
Leucettines, a family of 2-aminoimidazolin-4-ones derived from the marine sponge alkaloid Leucettamine B, have been developed as pharmacological inhibitors of DYRKs (dual specificity, tyrosine phosphorylation regulated kinases) and CLKs (cdc2-like kinases). ...
Leucettines, a family of 2-aminoimidazolin-4-ones derived from the marine sponge alkaloid Leucettamine B, have been developed …
Development of New Meridianin/Leucettine-Derived Hybrid Small Molecules as Nanomolar Multi-Kinase Inhibitors with Antitumor Activity.
Elsherbeny MH, Elkamhawy A, Nada H, Abdellattif MH, Lee K, Roh EJ. Elsherbeny MH, et al. Biomedicines. 2021 Sep 1;9(9):1131. doi: 10.3390/biomedicines9091131. Biomedicines. 2021. PMID: 34572319 Free PMC article.
In a step to develop new marine-inspired potent kinase inhibitors with antiproliferative activities, a new series of hybrid small molecules (5a-5g) was designed and synthesized based on chemical moieties derived from two marine natural products (Meridianin E and Leucettamine …
In a step to develop new marine-inspired potent kinase inhibitors with antiproliferative activities, a new series of hybrid small molecules …
Leucettamine B analogs and their carborane derivative as potential anti-cancer agents: Design, synthesis, and biological evaluation.
Hsu MH, Hsieh CY, Kapoor M, Chang JH, Chu HL, Cheng TM, Hsu KC, Lin TE, Tsai FY, Horng JC. Hsu MH, et al. Bioorg Chem. 2020 May;98:103729. doi: 10.1016/j.bioorg.2020.103729. Epub 2020 Mar 6. Bioorg Chem. 2020. PMID: 32179284
Leucettamine B is a natural product found in marine sponge Leucetta microraphis. Several of analogs of its family, such as aplysinopsine and clathridine, are medicinally active molecules which have applications in many pharmaceuticals and healthcare products; howeve …
Leucettamine B is a natural product found in marine sponge Leucetta microraphis. Several of analogs of its family, such as apl …
Marine-Derived 2-Aminoimidazolone Alkaloids. Leucettamine B-Related Polyandrocarpamines Inhibit Mammalian and Protozoan DYRK & CLK Kinases.
Loaëc N, Attanasio E, Villiers B, Durieu E, Tahtouh T, Cam M, Davis RA, Alencar A, Roué M, Bourguet-Kondracki ML, Proksch P, Limanton E, Guiheneuf S, Carreaux F, Bazureau JP, Klautau M, Meijer L. Loaëc N, et al. Mar Drugs. 2017 Oct 17;15(10):316. doi: 10.3390/md15100316. Mar Drugs. 2017. PMID: 29039762 Free PMC article. Review.
The origin (invertebrate cells, associated microorganisms, or filtered plankton), physiological functions, and natural molecular targets of these alkaloids are largely unknown. Following the identification of leucettamine B as an inhibitor of selected protein kinase …
The origin (invertebrate cells, associated microorganisms, or filtered plankton), physiological functions, and natural molecular targets of …
Unprecedented one-pot chemocontrolled entry to thioxoimidazolidinones and aminoimidazolones: synthesis of kinase inhibitor leucettamine B.
Selvaraju M, Sun CM. Selvaraju M, et al. ACS Comb Sci. 2015 Mar 9;17(3):182-9. doi: 10.1021/co500152s. Epub 2015 Jan 22. ACS Comb Sci. 2015. PMID: 25569559
An attempt to elucidate the observed chemoselectivity is described, and the products were confirmed by X-ray studies. One-pot synthesis toward Leucettamine B, a marine alkaloid, was achieved on the basis of this protocol....
An attempt to elucidate the observed chemoselectivity is described, and the products were confirmed by X-ray studies. One-pot synthesis towa …
Human CDC2-like kinase 1 (CLK1): a novel target for Alzheimer's disease.
Jain P, Karthikeyan C, Moorthy NS, Waiker DK, Jain AK, Trivedi P. Jain P, et al. Curr Drug Targets. 2014 May;15(5):539-50. doi: 10.2174/1389450115666140226112321. Curr Drug Targets. 2014. PMID: 24568585 Review.
Many natural and synthetic molecules are reported to possess CLK1 inhibitory activity. Some specific examples are Marine alkaloid Leucettamine B and KH-CB19. Leucettamine B is a potent inhibitor of CLK1 (15 nM), Dyrk1A (40 nM), and Dyrk2 (35 nM) and a …
Many natural and synthetic molecules are reported to possess CLK1 inhibitory activity. Some specific examples are Marine alkaloid Leucett …
Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B.
Tahtouh T, Elkins JM, Filippakopoulos P, Soundararajan M, Burgy G, Durieu E, Cochet C, Schmid RS, Lo DC, Delhommel F, Oberholzer AE, Pearl LH, Carreaux F, Bazureau JP, Knapp S, Meijer L. Tahtouh T, et al. J Med Chem. 2012 Nov 8;55(21):9312-30. doi: 10.1021/jm301034u. Epub 2012 Oct 8. J Med Chem. 2012. PMID: 22998443
DYRKs (dual specificity, tyrosine phosphorylation regulated kinases) and CLKs (cdc2-like kinases) are implicated in the onset and development of Alzheimer's disease and Down syndrome. The marine sponge alkaloid leucettamine B was recently identified as an inhibitor …
DYRKs (dual specificity, tyrosine phosphorylation regulated kinases) and CLKs (cdc2-like kinases) are implicated in the onset and developmen …
14 results