A covalent small molecule inhibitor of glutamate-oxaloacetate transaminase 1 impairs pancreatic cancer growth
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چکیده
منابع مشابه
Small Molecule Therapeutics A Novel Small-Molecule Inhibitor of Mcl-1 Blocks Pancreatic Cancer Growth In Vitro and In Vivo
Using a high-throughput screening (HTS) approach, we have identified and validated several smallmolecule Mcl-1 inhibitors (SMI). Here, we describe a novel selective Mcl-1 SMI inhibitor, 2 (UMI-77), developed by structure-based chemical modifications of the lead compound 1 (UMI-59). We have characterized the binding of UMI-77 to Mcl-1 by using complementary biochemical, biophysical, and computat...
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AP endonuclease 1 (APE1; also known as REF-1) contains a DNA repair domain and a redox regulation domain. APE1 is overexpressed in several human cancers, and disruption of APE1 function has detrimental effects on cancer cell viability. However, the selective contribution of the redox and the DNA repair domains to maintenance of cellular homeostasis in cancer has not been elucidated. In the pres...
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We have examined a polymorphism for the soluble glutamate oxaloacetate (GOT-1) isozyme system which was found in the Asian mouse Mus castaneus. Variants of GOT-1 segregate as though they are controlled by codominant alleles for a single autosomal locus which we have designated Got-1. No close linkage of genes for soluble and mitochondrial forms of the enzyme, GOT-1 and GOT-2 respectively, was o...
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Using a high-throughput screening (HTS) approach, we have identified and validated several small-molecule Mcl-1 inhibitors (SMI). Here, we describe a novel selective Mcl-1 SMI inhibitor, 2 (UMI-77), developed by structure-based chemical modifications of the lead compound 1 (UMI-59). We have characterized the binding of UMI-77 to Mcl-1 by using complementary biochemical, biophysical, and computa...
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Excessive amounts of extracellular glutamate in brain are excitotoxic and lead to neuronal death. Glutamate pyrovate transamiase (GPT) and glutamate oxaloacetate transaminase (GOT) catalyze transamination of glutamate to alpha ketoglutarate. Because vitamin B6 is essential for the enzymes activities, this study was undertaken to examine the effect of vitamin B6 on age related changes of this en...
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ژورنال
عنوان ژورنال: Biochemical and Biophysical Research Communications
سال: 2020
ISSN: 0006-291X
DOI: 10.1016/j.bbrc.2019.11.130