871807-58-8Relevant academic research and scientific papers
TRICYCLIC PROTEASOME ACTIVITY ENHANCING COMPOUNDS
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, (2012/02/05)
Proteinopathies result from the proteasome not acting efficiently enough to eliminate harmful proteins and prevent the formation of the pathogenic aggregates. As described herein, inhibition of proteasome-associated deubiquitinase Usp14 results in increased proteasome efficiency. The present invention therefore provides novel compositions and methods for inhibition of Usp14, enhancement of proteasome activity and treatment of proteinopathies.
Identification of 5,6-substituted 4-aminothieno[2,3-d]pyrimidines as LIMK1 inhibitors
Sleebs, Brad E.,Nikolakopoulos, George,Street, Ian P.,Falk, Hendrik,Baell, Jonathan B.
supporting information; experimental part, p. 5992 - 5994 (2011/10/18)
4-Aminobenzothieno[3,2-d]pyrimidines were previously identified in a high throughput screening campaign as LIMK1 inhibitors. Scaffold reversal led to the identification of a series of simple 5,6-substituted 4-aminothieno[2,3-d] pyrimidines with low micromolar inhibition of LIMK1.
Synthesis and study of antiproliferative activity of novel thienopyrimidines on glioblastoma cells
Pédeboscq, Stéphane,Gravier, Denis,Casadebaig, Fran?oise,Hou, Geneviève,Gissot, Arnaud,De Giorgi, Francesca,Ichas, Fran?ois,Cambar, Jean,Pometan, Jean-Paul
experimental part, p. 2473 - 2479 (2010/07/08)
The receptor tyrosine kinases (for example EGFR, PDGFR, VEGFR) are a transmembrane protein family which plays a crucial role in tumor growth, survival, metastasis dissemination and angiogenesis. During the past 10 years, many tyrosine kinase inhibitors (T
