101258-16-6Relevant articles and documents
Hitting a Moving Target: Simulation and Crystallography Study of ATAD2 Bromodomain Blockers
Dolbois, Aymeric,Batiste, Laurent,Wiedmer, Lars,Dong, Jing,Brütsch, Manuela,Huang, Danzhi,Deerain, Nicholas M.,Spiliotopoulos, Dimitrios,Cheng-Sánchez, Iván,Laul, Eleen,Nevado, Cristina,?led?, Pawe?,Caflisch, Amedeo
supporting information, p. 1573 - 1580 (2020/09/16)
Small molecule ligand binding to the ATAD2 bromodomain is investigated here through the synergistic combination of molecular dynamics and protein crystallography. A previously unexplored conformation of the binding pocket upon rearrangement of the gatekeeper residue Ile1074 has been found. Further, our investigations reveal how minor structural differences in the ligands result in binding with different plasticity of the ZA loop for this difficult-to-drug bromodomain.
Substituted hydantoins
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Page/Page column 61, (2008/06/13)
The present invention relates to compounds of the formula which are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as, cancer, cognative and CNS disorders and inflammatory/autoimmune diseases.
NOVEL 2-PYRIDINECARBOXAMIDE DERIVATIVES
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Page/Page column 127, (2008/06/13)
The present invention relates to a compound which has a glucokinase-activating effect and is useful as a therapeutic agent for diabetes mellitus, being represented by a formula (I): [wherein X1 represents a nitrogen atom, sulfur atom, oxygen at