subject area of

• 3-Aryl-5-phenoxymethyl-1,3-oxazolidin-2-ones as positive allosteric modulators of mGluR2 for the treatment of schizophrenia: Hit-to-lead efforts  Academic Article
• A conformational switch in human immunodeficiency virus gp41 revealed by the structures of overlapping epitopes recognized by neutralizing antibodies  Academic Article
• A critical role of the C-terminal segment for allosteric inhibitor-induced aberrant multimerization of HIV-1 integrase  Academic Article
• A detergent-activated tyrosinase from xenopus-laevis .1. Purification and partial characterization  Academic Article
• A heteroaryldihydropyrimidine activates and can misdirect hepatitis b virus capsid assembly  Academic Article
• A metal-binding motif implicated in RNA recognition by an aminoacyl-tRNA synthetase and by a retroviral gene product  Academic Article
• A new mechanism of allostery in a G protein-coupled receptor dimer  Academic Article
• A novel loop-loop recognition motif in the yeast ribosomal protein L30 autoregulatory RNA complex  Academic Article
• A novel α2/α4 subtype-selective positive allosteric modulator of nicotinic acetylcholine receptors acting from the C-tail of an α subunit  Academic Article
• A sphingosine 1-phosphate receptor 2 selective allosteric agonist  Academic Article
• A steady-state-kinetic model for formaldehyde dehydrogenase from human liver. A mechanism involving NAD+ and the hemimercaptal adduct of glutathione and formaldehyde as substrates and free glutathione as an allosteric activator of the enzyme  Academic Article
• ATP sulfurylase from filamentous fungi: which sulfonucleotide is the true allosteric effector?  Academic Article
• Activation of AMP-activated protein kinase revealed by hydrogen/deuterium exchange mass spectrometry  Academic Article
• Active site mutants of Escherichia coli citrate synthase. Effects of mutations on catalytic and allosteric properties  Academic Article
• Activity-enhancing mutations in an E3 ubiquitin ligase identified by high-throughput mutagenesis  Academic Article
• Allosteric activators of glucokinase: potential role in diabetes therapy  Academic Article
• Allosteric communication in the dynein motor domain  Academic Article
• Allosteric control of ligand selectivity between estrogen receptors alpha and beta: Implications for other nuclear receptors  Academic Article
• Allosteric control of quaternary states in escherichia-coli aspartate-transcarbamylase  Academic Article
• Allosteric inhibition of human ribonucleotide reductase by dATP entails the stabilization of a hexamer  Academic Article
• Allosteric inhibition of hypoxia inducible factor-2 with small molecules  Academic Article
• Allosteric inhibition via R-state destabilization in ATP sulfurylase from Penicillium chrysogenum  Academic Article
• Allosteric inhibitors have distinct effects, but also common modes of action, in the HCV polymerase  Academic Article
• Allosteric modulation of ampa-type glutamate receptors increases activity of the promoter for the neural cell adhesion molecule, n-cam  Academic Article
• Allosteric regulation by oleamide of the binding properties of 5-hydroxytryptamine(7) receptors  Academic Article
• Allosteric regulation of DNA cleavage and sequence-specificity through run-on oligomerization  Academic Article
• Allosteric regulation of the 16-alpha-hydroxylation of progesterone as catalyzed by rabbit microsomal cytochrome-p-450-3b  Academic Article
• Allosteric sodium in class A GPCR signaling  Academic Article
• An allosteric mechanism for drug block of the human cardiac potassium channel KCNQ1  Academic Article
• Application of parallel multiparametric cell-based FLIPR detection assays for the identification of modulators of the muscarinic acetylcholine receptor 4 (M-4)  Academic Article
• Bacterial chemoreceptor dynamics correlate with activity state and are coupled over long distances  Academic Article
• Benzazoles as allosteric potentiators of metabotropic glutamate receptor 2 (mGluR2): Efficacy in an animal model for schizophrenia  Academic Article
• Bifacial peptide nucleic acid as an allosteric switch for aptamer and ribozyme function  Academic Article
• Biphenyl-indanones: Allosteric potentiators of the metabotropic glutamate subtype 2 receptor  Academic Article
• Broadly neutralizing antibody PGT121 allosterically modulates CD4 binding via recognition of the HIV-1 gp120 V3 base and multiple surrounding glycans  Academic Article
• CD44 receptor unfolding enhances binding by freeing basic amino acids to contact carbohydrate ligand  Academic Article
• Calmodulin stabilizes an amphiphilic alpha-helix within rc3/neurogranin and gap-43/neuromodulin only when ca2+ is absent  Academic Article
• Carbamyl phosphate binding to aspartate transcarbamylase. Partial saturation and its alteration by succinate  Academic Article
• Characterization of two different five-coordinate soluble guanylate cyclase ferrous-nitrosyl complexes  Academic Article
• Cofactor-mediated conformational dynamics promote product release from Escherichia coli dihydrofolate reductase via an allosteric pathway  Academic Article
• Conditional RNA interference mediated by allosteric ribozyme  Academic Article
• Conformational changes in aspartate trancarbamylase. I. Studies of ligand binding and of subunit interactions by circular dichroism spectroscopy  Academic Article
• Conformational changes in aspartate transcarbamylase. II. Circular dichroism evidence for the involvement of metal ions in allosteric interactions  Academic Article
• Congenital disease snps target lineage specific structural elements in protein kinases  Academic Article
• Constitutive forms of rabbit-liver microsomal cytochrome-P-450 - enzymatic diversity, polymorphism and allosteric regulation  Academic Article
• Coupling of agonist binding to channel gating in an ACh-binding protein linked to an ion channel  Academic Article
• Coupling of receptor conformation and ligand orientation determine graded activity  Academic Article
• Crystal structure of atp sulfurylase from penicillium chrysogenum: Insights into the allosteric regulation of sulfate assimilation  Academic Article
• Crystal structure of hsiuv complexed with a vinyl sulfone inhibitor: Corroboration of a proposed mechanism of allosteric activation of hsiv by hsiu  Academic Article
• Crystal structure of the lactose operon repressor and its complexes with DNA and inducer  Academic Article
• Crystallographic fragment-based drug discovery: use of a brominated fragment library targeting HIV protease  Academic Article
• Cysteine modifiers suggest an allosteric inhibitory site on the CAL PDZ domain  Academic Article
• Designing allosteric control into enzymes by chemical rescue of structure  Academic Article
• Development of a highly potent, novel M(5) positive allosteric modulator (PAM) demonstrating CNS exposure: 1-((1H-indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)pipe ridine-4-carboxamide (ML380)  Academic Article
• Discovery and SAR of muscarinic receptor subtype 1 (M-1) allosteric activators from a molecular libraries high throughput screen. Part 1: 2,5-Dibenzyl-2H-pyrazolo 4,3-c quinolin-3(5H)-ones as positive allosteric modulators  Academic Article
• Discovery and characterization of novel allosteric FAK inhibitors  Academic Article
• Discovery of 5-aryl-1,3-dihydro-2H-imidazo 4,5-b pyridin-2-ones as positive allosteric modulators of metabotropic glutamate subtype-2 (mGlu2) receptors with efficacy in a preclinical model of psychosis  Academic Article
• Discovery of a distinct chemical and mechanistic class of allosteric HIV-1 integrase inhibitors with antiretroviral activity  Academic Article
• Discovery of a novel class of negative allosteric modulator of the dopamine D-2 receptor through fragmentation of a bitopic ligand  Academic Article
• Discovery of allosteric inhibitors of kinesin spindle protein (KSP) for the treatment of taxane-refractory cancer: MK-0731 and analogs  Academic Article
• Discovery of an intravenous hepatoselective glucokinase activator for the treatment of inpatient hyperglycemia  Academic Article
• Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators  Academic Article
• Discovery of the first M5-selective and CNS penetrant negative allosteric modulator (NAM) of a muscarinic acetylcholine receptor: (S)-9b-(4-chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-one (ML375)  Academic Article
• Distal substitutions drive divergent DNA specificity among paralogous transcription factors through subdivision of conformational space  Academic Article
• Dual allosteric inhibitors jointly modulate protein structure and dynamics in the hepatitis C virus polymerase  Academic Article
• GalR2-positive allosteric modulator exhibits anticonvulsant effects in animal models  Academic Article
• Gating movement of acetylcholine receptor caught by plunge-freezing  Academic Article
• Girk channel modulation by assembly with allosterically regulated RGS proteins  Academic Article
• Hidden allostery in human glutathione transferase p1-1 unveiled by unnatural amino acid substitutions and inhibition studies  Academic Article
• High-throughput FRET assay yields allosteric SERCA activators  Academic Article
• High-throughput assay and engineering of self-cleaving ribozymes by sequencing  Academic Article
• Human GLP-1 receptor transmembrane domain structure in complex with allosteric modulators  Academic Article
• Identification of coumarin derivatives as a novel class of allosteric MEK1 inhibitors  Academic Article
• Importance of a conserved residue, aspartate-162, for the function of escherichia-coli aspartate transcarbamoylase  Academic Article
• In vitro selection of nucleic acids and proteins: what are we learning?  Academic Article
• Induction of positive cooperativity by amino acid replacements within the C-terminal domain of penicillium chrysogenum ATP sulfurylase  Academic Article
• Influence of cofactor binding and active site occupancy on the conformation of the macromolecular substrate exosite of factor viia  Academic Article
• Inhibition of acetyl-CoA carboxylase suppresses fatty acid synthesis and tumor growth of non-small-cell lung cancer in preclinical models  Academic Article
• Interaction between beta-adrenergic receptors and guanine-nucleotide sites in turkey erythrocyte-membranes  Academic Article
• Intraspecies individuality for the metabolism of steroids  Academic Article
• Ligand-binding dynamics rewire cellular signaling via estrogen receptor-alpha  Academic Article
• Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers  Academic Article
• Mechanisms for zinc and proton inhibition of the GluN1/GluN2A NMDA receptor  Academic Article
• Metabolic flux responses to pyruvate kinase knockout in escherichia coli  Academic Article
• Mode of action for linear peptide inhibitors of hiv-1 gp120 interactions  Academic Article
• Modulation of allostery by protein intrinsic disorder  Academic Article
• Modulation of glucokinase by glucose, small-molecule activator and glucokinase regulatory protein: steady-state kinetic and cell-based analysis  Academic Article
• Modulation of rabbit and human hepatic cytochrome P-450-catalyzed steroid hydroxylations by alpha-naphthoflavone  Academic Article
• Molecular architecture of human polycomb repressive complex 2  Academic Article
• Molecular control of delta-opioid receptor signalling  Academic Article
• Molecular mechanism of the sweet taste enhancers  Academic Article
• Nitric-oxide synthase forms N-NO-pterin and S-NO-cys: implications for activity, allostery, and regulation  Academic Article
• Nucleotide regulation of soluble guanylate cyclase substrate specificity  Academic Article
• P53 latency - out of the blind alley  Academic Article
• Parallel synthesis of N-biaryl quinolone carboxylic acids as selective M(1) positive allosteric modulators  Academic Article
• Positive allosteric modulators to peptide GPCRs: A promising class of drugs  Academic Article
• Potent mechanism-based inactivation of cytochrome p450 2b4 by 9-ethynylphenanthrene: Implications for allosteric modulation of cytochrome p450 catalysis  Academic Article
• Probing protein disorder and complexity at single-molecule resolution  Academic Article
• Progress towards validating the NMDA receptor hypofunction hypothesis of schizophrenia  Academic Article
• Protein arginine methyltransferase 5 catalyzes substrate dimethylation in a distributive fashion  Academic Article
• Protein-protein interactions involved in the recognition of p27 by e3 ubiquitin ligase  Academic Article
• Proton uptake accompanies formation of the ternary complex of citrate synthase, oxaloacetate, and the transition-state analog inhibitor, carboxymethyl-CoA. Evidence that a neutral enol is the activated form of acetyl-CoA in the citrate synthase reaction  Academic Article
• Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif  Academic Article
• Regulation of tissue factor cytoplasmic domain phosphorylation by palmitoylation  Academic Article
• Retinoid x receptor is a nonsilent major contributor to vitamin d receptor-mediated transcriptional activation  Academic Article
• Reversible activation of non-steroid binding oestrogen receptor  Academic Article
• Role of residue phe(225) in the cofactor-mediated, allosteric regulation of the serine protease coagulation factor viia  Academic Article
• Sodium ion binding pocket mutations and adenosine A2A receptor function  Academic Article
• Soluble guanylate cyclase is activated differently by excess no and by yc-1: Resonance raman spectroscopic evidence  Academic Article
• Stable expression of recombinant ampa receptor subunits: Binding affinities and effects of allosteric modulators  Academic Article
• Structural basis for allosteric regulation of GPCRs by sodium ions  Academic Article
• Structural basis for the root effect in haemoglobin  Academic Article
• Structural basis of autoregulation of phenylalanine hydroxylase  Academic Article
• Structural interconversions modulate activity of escherichia coli ribonucleotide reductase  Academic Article
• Structural mechanisms of allostery and autoinhibition in JNK family kinases  Academic Article
• Structure of a class C GPCR metabotropic glutamate receptor 1 bound to an allosteric modulator  Academic Article
• Structure of the intact ppar-gamma-rxr-alpha nuclear receptor complex on DNA  Academic Article
• Structure, distribution, and functional expression of the phosphofructokinase-c isozyme  Academic Article
• Structure-function of the G protein-coupled receptor superfamily  Academic Article
• Synthesis and activity of substituted heteroaromatics as positive allosteric modulators for α4β2α5 nicotinic acetylcholine receptors  Academic Article
• Target of γ-secretase modulators, presenilin marks the spot  Academic Article
• Temperature effects on the allosteric transition of atp sulfurylase from penicillium chrysogenum  Academic Article
• The 5' leader of the mRNA encoding the Marek's disease virus serotype 1 pp14 protein contains an intronic internal ribosome entry site with allosteric properties  Academic Article
• The E-2.65 A mutation disrupts dynamic binding poses of SB269652 at the dopamine D2 and D3 receptors  Academic Article
• The design and synthesis of potent and cell-active allosteric dual Akt 1 and 2 inhibitors devoid of hERG activity  Academic Article
• The expanding view of RNA and DNA function  Academic Article
• The interaction of activated factor vii with tissue factor: Insight into the mechanism of cofactor-mediated activation of activated factor vii  Academic Article
• The role of a sodium ion binding site in the allosteric modulation of the A2A adenosine G protein-coupled receptor  Academic Article
• The role of cysteine 206 in allosteric inhibition of Escherichia coli citrate synthase. Studies by chemical modification, site-directed mutagenesis, and 19-F NMR  Academic Article
• The structural basis of function of the TF. VIIa complex in the cellular initiation of coagulation  Academic Article
• The structure of apo human glutamate dehydrogenase details subunit communication and allostery  Academic Article
• Thumb inhibitor binding eliminates functionally important dynamics in the hepatitis C virus RNA polymerase  Academic Article
• Transposition of three amino acids transforms the human metabotropic glutamate receptor (mGluR)-3-positive allosteric modulation site to mGluR2, and additional characterization of the mGluR2-positive allosteric modulation site  Academic Article
• Turning a protein kinase on or off from a single allosteric site via disulfide trapping  Academic Article
• Unique allosteric regulation of 5-hydroxytryptamine receptor-mediated signal transduction by oleamide  Academic Article
• Volatile anesthetic modulation of oligomerization equilibria in a hexameric model peptide  Academic Article