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Showing 1 to 7 of 7 for “"isoform selectivity"”.
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Identifying Protein Interactors of Voltage-Gated Sodium Channel Nav1.6 in Native Tissue
… targeting Nav channels are available, they lack isoform selectivity, leading to unwanted side effects. Protein-protein interactions regulate Nav channel function and represent a promising target for developing new drugs. Understanding the protein-protein interaction network of Nav channels will …
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Isoform Selective Regulation of Adenylyl Cyclase By Small Molecule Inhibitors and Gbetagamma Protein
<p>The nine membrane-bound isoforms of adenylyl cyclase (AC), via synthesis of the signaling molecule cyclic AMP (cAMP), are involved in many isoform specific physiological functions. All nine isoforms share a similar structural organization; thus, AC isoform differences in physiological function …
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Developing 1,2,3,4-tetrahydro-5H-aryl[1,4]diazepin-5-ones and Related Scaffolds as Poly-(ADP-ribosyl) Polymerase (PARP) Inhibitors and Exploring Their Targeted Polypharmacology with Kinases
… a superfamily of enzymes comprised of 17 known isoforms. PARP inhibitors (PARPi) have shown success in clinical trials for the treatment of homologous recombination-deficient cancers. Though proven effective initially, tumors treated with PARPi eventually develop resistance. Combinatorial …
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Development Of Elisa-Based Hdac Activity Assay For Identification Of Isoform Selective Hdac Inhibitors
… interact with all or most of the eleven HDAC isoforms, leading to possible side-effects. Hence, HDAC inhibitors specific to one HDAC isoforms (Isoform selective HDAC inhibitors) may overcome the potential clinical side effects and be effective anti-cancer drugs. In addition, isoform selective …
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The structural requirements of histone deacetylase (hdac) inhibitors: suberoylanilide hydroxamic acid (saha) analogues modified at c3, c6, and c7 positions enhance selectivity
… requirements of inhibitory potency and isoform selectivity.</p> <p>In previous work, SAHA analogues functionalized at the C2 position (C2-SAHA analogues) near the metal binding hydroxamic acid displayed decreased inhibitory activity compared to the parent compound, SAHA. The lack of …
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Activity-based sensors for reactive aldehydes and their corresponding enzymatic machinery
… stem cell marker. AlDeSense had remarkable selectivity for ALDH1A1, producing a 20-fold increase in fluorescence signal upon oxidation by the enzyme. We confirmed ALDH1A1 activity, as measured by AlDeSense, was a reliable cancer stem cell marker in leukemia, melanoma, and breast cancer …
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Purification of protein phosphatases and 14-3-3-binding proteins and their regulation by the cAMP–PKA pathway
… signalling pathway is activated and study the isoform specificity of PP1. Most protein phosphatases of the PPP family do not exist as free catalytic subunits: instead, they interact with regulatory subunits, which specify, target and/or inhibit their activities. Protein phosphatases of the PPP …