67023-53-4Relevant academic research and scientific papers
Targeting nuclear protein TDP-43 by cell division cycle kinase 7 inhibitors: A new therapeutic approach for amyotrophic lateral sclerosis
Rojas-Prats, Elisa,Martinez-Gonzalez, Loreto,Gonzalo-Consuegra, Claudia,Liachko, Nicole F.,Perez, Concepción,Ramírez, David,Kraemer, Brian C.,Martin-Requero, ángeles,Perez, Daniel I.,Gil, Carmen,de Lago, Eva,Martinez, Ana
supporting information, (2020/11/12)
Amyotrophic lateral sclerosis (ALS) is a fatal neurodegenerative disease with no known cure. Aggregates of the nuclear protein TDP-43 have been recognized as a hallmark of proteinopathy in both familial and sporadic cases of ALS. Post-translational modifications of this protein, include hyperphosphorylation, cause disruption of TDP-43 homeostasis and as a consequence, promotion of its neurotoxicity. Among the kinases involved in these changes, cell division cycle kinase 7 (CDC7) plays an important role by directly phosphorylating TDP-43. In the present manuscript the discovery, synthesis, and optimization of a new family of selective and ATP-competitive CDC7 inhibitors based on 6-mercaptopurine scaffold are described. Moreover, we demonstrate the ability of these inhibitors to reduce TDP-43 phosphorylation in both cell cultures and transgenic animal models such as C. elegans and Prp-hTDP43 (A315T) mice. Altogether, the compounds described here may be useful as versatile tools to explore the role of CDC7 in TDP-43 phosphorylation and also as new drug candidates for the future development of ALS therapies.
Method for treating disease or condition susceptible to amelioration by AMPK activators and compounds of formula which are useful to activate AMP-activated protein kinase (AMPK)
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Paragraph 0051-0052, (2014/10/16)
The present invention relates to a method for treating disease or condition susceptible to amelioration by AMPK activators and compounds of formula which are useful to activate AMP-activated protein kinase (AMPK) and the use of the compounds in the prevention or treatment of disease, including pre-diabetes, type 2 diabetes, syndrome X, metabolic syndrome and obesity.
Diverse in vitro and in vivo anti-inflammatory effects of trichlorido-gold(III) complexes with N6-benzyladenine derivatives
K?ikavová, Radka,Ho?ek, Jan,Suchy, Pavel,Van?o, Ján,Trávní?ek, Zdeněk
, p. 92 - 99 (2014/03/21)
A series of gold(III) complexes involving differently substituted derivatives of a plant hormone N6-benzyladenine (HL1-5) is reported. The complexes have the general formula [Au(HL1-5)Cl3] a?nH2O (n = 0 for 1, 3-5; and n = 1 for 2),
Preparation and biological activity of 6-benzylaminopurine derivatives in plants and human cancer cells
Dolezal, Karel,Popa, Igor,Krystof, Vladimir,Spichal, Lukas,Fojtikova, Martina,Holub, Jan,Lenobel, Rene,Schmuelling, Thomas,Strnad, Miroslav
, p. 875 - 884 (2007/10/03)
To study the structure-activity relationships of aromatic cytokinins, the cytokinin activity at both the receptor and cellular levels, as well as CDK inhibitory and anticancer properties of 38 6-benzylaminopurine (BAP) derivatives were compared in various
