Reversible Covalent Inhibition of eEF-2K by Carbonitriles
نویسندگان
چکیده
منابع مشابه
Reversible covalent inhibition of eEF-2K by carbonitriles.
eEF-2K is a potential target for treating cancer. However, potent specific inhibitors for this enzyme are lacking. Previously, we identified 2,6-diamino-4-(2-fluorophenyl)-4H-thiopyran-3,5-dicarbonitrile (DFTD) as an inhibitor of eEF-2K. Here we describe its mechanism of action against eEF-2K, on the basis of kinetic, mutational, and docking studies, and use chemoinformatic approaches to identi...
متن کاملEffect reversible inhibition of hippocampal CA1 rehion by lidocaine on amygdala kindling rata in rats
In this study the role of CA1 region of dorsal hippocamus an amygdala kindling rate was investigated by bilateral microinjection of lidocaine into hippocampus.28 rats were divided into four groups.in group I:animals were implanted only with a tripolar electrode into the amygdala but in groups 2-4,two guide cannulaae were also implanted into the CA1 region of the dorsale hippocampus.two monopol...
متن کاملONIOM calculations on serotonin degradation by monoamine oxidase B: insight into the oxidation mechanism and covalent reversible inhibition.
Monoamine oxidase (MAO) is an enzyme which catalyzes the oxidation of neurotransmitter amines and regulates their level. There are two forms of the enzyme with 70% similarity, known as MAO-A and MAO-B. MAO inhibitors are used in the treatment of neurological disorders such as depression, Parkinson's and Alzheimer's diseases. Therefore, understanding the chemical steps of MAO catalyzed amine oxi...
متن کاملA Combinatorial Proof of a Relationship Between Maximal $(2k-1, 2k+1)$-Cores and $(2k-1, 2k, 2k+1)$-Cores
Integer partitions which are simultaneously t–cores for distinct values of t have attracted significant interest in recent years. When s and t are relatively prime, Olsson and Stanton have determined the size of the maximal (s, t)-core κs,t. When k > 2, a conjecture of Amdeberhan on the maximal (2k − 1, 2k, 2k + 1)-core κ2k−1,2k,2k+1 has also recently been verified by numerous authors. In this ...
متن کاملNative chemical ligation in covalent caspase inhibition by p35.
Wide-spectrum caspase inhibition by the baculoviral p35 protein was previously shown to be a consequence of covalent inhibition in which a thioester bond is stably formed between the cleavage residue Asp87 of p35 and the active site Cys360' of caspase-8. Here we show that the N-terminal fragment of cleaved p35 (p35-N) is a circular peptide when dissociated from the caspase. Biochemical and crys...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: ChemBioChem
سال: 2014
ISSN: 1439-4227
DOI: 10.1002/cbic.201402321