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Enzyme Inhibitors

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  • 'Reverse' alpha-ketoamide-based p38 map kinase inhibitors  Academic Article
  • (-)-FR182877 is a potent and selective inhibitor of carboxylesterase-1  Academic Article
  • 1-(2-(2,2,2-Trifluoroethoxy)ethyl-1H-pyrazolo 4,3-d pyrimidines as potent phosphodiesterase 5 (PDE5) inhibitors  Academic Article
  • 1-(2-Ethoxyethyl)-1H-pyrazolo 4,3-d pyrimidines as potent phosphodiesterase 5 (PDE5) inhibitors  Academic Article
  • 10-(2-benzoxazolcarbonyl)-5,10-dideaza-acyclic-5,6,7,8-tetrahydrofolic acid: a potential inhibitor of GAR transformylase and AICAR transformylase  Academic Article
  • 10-formyl-5,10-dideaza-acyclic-5,6,7,8-tetrahydrofolic acid (10-formyl-DDACTHF): a potent cytotoxic agent acting by selective inhibition of human GAR Tfase and the de novo purine biosynthetic pathway  Academic Article
  • 10-formyl-5,8,10-trideazafolic acid (10-formyl-TDAF): a potent inhibitor of glycinamide ribonucleotide transformylase  Academic Article
  • 14-3-3 proteins in neuronal development and function  Academic Article
  • 2-(6-Phenyl-1H-indazol-3-yl)-1H-benzo[d]imidazoles: Design and synthesis of a potent and isoform selective PKC-zeta inhibitor  Academic Article
  • 7-alkylidenecephalosporin esters as inhibitors of human leukocyte elastase  Academic Article
  • 7-nitroindazole, nitric oxide synthase inhibitor, attenuates physical dependence on butorphanol in rat  Academic Article
  • 8-Hydroxyquinoline and hydroxamic acid inhibitors of botulinum neurotoxin BoNT/A  Academic Article
  • A FAAH-regulated class of N-acyl taurines that activates TRP ion channels  Academic Article
  • A FluoPol-ABPP PAD2 high-throughput screen identifies the first calcium site inhibitor targeting the PADs  Academic Article
  • A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate  Academic Article
  • A bisubstrate analog induces unexpected conformational changes in phosphoglycerate kinase from trypanosoma brucei  Academic Article
  • A chemical biology approach reveals period shortening of the mammalian circadian clock by specific inhibition of GSK-3β  Academic Article
  • A chemical switch for inhibitor-sensitive alleles of any protein kinase  Academic Article
  • A chemoenzymatic synthesis of UDP-(2-deoxy-2-fluoro)-galactose and evaluation of its interaction with galactosyltransferase  Academic Article
  • A chloroacetamidine-based inactivator of protein arginine methyltransferase 1: Design, synthesis, and in vitro and in vivo evaluation  Academic Article
  • A combinatorial approach to characterize the substrate specificity of protein arginine methyltransferase 1  Academic Article
  • A combinatorial scaffold approach toward kinase-directed heterocycle libraries  Academic Article
  • A comprehensive profile of brain enzymes that hydrolyze the endocannabinoid 2-arachidonoylglycerol  Academic Article
  • A concise and traceless linker strategy toward combinatorial libraries of 2,6,9-substituted purines  Academic Article
  • A conserved XIAP-interaction motif in caspase-9 and Smac/DIABLO regulates caspase activity and apoptosis  Academic Article
  • A cyclic nucleotide-dependent chloride conductance in olfactory receptor neurons  Academic Article
  • A fasting inducible switch modulates gluconeogenesis via activator/coactivator exchange  Academic Article
  • A fluopol-ABPP HTS assay to identify PAD inhibitors  Academic Article
  • A fluorescence-based thiol quantification assay for ultra-high-throughput screening for inhibitors of coenzyme a production  Academic Article
  • A fluoroacetamidine-based inactivator of protein arginine deiminase 4: Design, synthesis, and in vitro and in vivo evaluation  Academic Article
  • A functional proteomic strategy to discover inhibitors for uncharacterized hydrolases  Academic Article
  • A galanin-mastoparan chimeric peptide activates the Na+,K(+)-ATPase and reverses its inhibition by ouabain  Academic Article
  • A glycosidase antibody elicited against a chair-like transition state analog by in vitro immunization  Academic Article
  • A high-throughput screen against pantothenate synthetase (PanC) identifies 3-biphenyl-4-cyanopyrrole-2-carboxylic acids as a new class of inhibitor with activity against Mycobacterium tuberculosis  Academic Article
  • A high-throughput screening compatible assay for activators and inhibitors of methionine sulfoxide reductase a  Academic Article
  • A high-throughput, multiplexed assay for superfamily-wide profiling of enzyme activity  Academic Article
  • A homogeneous resonance energy transfer assay for phosphopantetheinyl transferase  Academic Article
  • A mass spectrometry plate reader: monitoring enzyme activity and inhibition with a desorption/ionization on silicon (DIOS) platform  Academic Article
  • A minor catalytic activity of src family kinases is sufficient for maximal activation of mast cells via the high-affinity ige receptor  Academic Article
  • A myristoylated pseudosubstrate peptide of PKC-ζ induces degranulation in HMC-1 cells independently of PKC-ζ activity  Academic Article
  • A nanostructure-initiator mass spectrometry-based enzyme activity assay  Academic Article
  • A naturally occurring brominated furanone covalently modifies and inactivates LuxS  Academic Article
  • A novel fluorophosphonate inhibitor of the biosynthesis of the endocannabinoid 2-arachidonoylglycerol with potential anti-obesity effects  Academic Article
  • A novel histidine kinase inhibitor regulating development in bacillus subtilis  Academic Article
  • A novel neuroprotective agent with antioxidant and nitric oxide synthase inhibitory action  Academic Article
  • A ph sensitive colorometric assay for the high-throughput screening of enzyme inhibitors and substrates: A case study using kinases  Academic Article
  • A plant-like kinase in plasmodium falciparum regulates parasite egress from erythrocytes  Academic Article
  • A potent and highly selective inhibitor of human α-1,3-fucosyltransferase via click chemistry  Academic Article
  • A potent and highly selective sulfotransferase inhibitor  Academic Article
  • A potent and selective inhibitor for the UBLCP1 proteasome phosphatase  Academic Article
  • A potent mechanism-inspired O-GlcNAcase inhibitor that blocks phosphorylation of tau in vivo  Academic Article
  • A reduced-amide inhibitor of Pin1 binds in a conformation resembling a twisted-amide transition state  Academic Article
  • A reversible S-adenosyl-L-homocysteine hydrolase inhibitor ameliorates experimental autoimmune encephalomyelitis by inhibiting T cell activation  Academic Article
  • A role for I kappa B kinase 2 in bipolar spindle assembly  Academic Article
  • A role for Src kinase in spontaneous epileptiform activity in the CA3 region of the hippocampus  Academic Article
  • A search for pyrophosphate mimics for the development of substrates and inhibitors of glycosyltransferases  Academic Article
  • A selective inhibitor Gal-PUGNAc of human lysosomal beta-hexosaminidases modulates levels of the ganglioside GM2 in neuroblastoma cells  Academic Article
  • A single-subunit nadh-quinone oxidoreductase renders resistance to mammalian nerve cells against complex i inhibition  Academic Article
  • A small interfering RNA screen for modulators of tumor cell motility identifies MAP4K4 as a promigratory kinase  Academic Article
  • A small molecule antagonist of ghrelin O-acyltransferase (GOAT)  Academic Article
  • A small molecule bidentate-binding dual inhibitor probe of the LRRK2 and JNK kinases  Academic Article
  • A small molecule bidentate-binding dual inhibitor probe of the LRRK2 and JNK kinases  Academic Article
  • A small molecule modulates Jumonji histone demethylase activity and selectively inhibits cancer growth  Academic Article
  • A small molecule primes embryonic stem cells for differentiation  Academic Article
  • A strategy to discover inhibitors of Bacillus subtilis surfactin-type phosphopantetheinyl transferase  Academic Article
  • A structural snapshot of CYP2B4 in complex with paroxetine provides insights into ligand binding and clusters of conformational states  Academic Article
  • A substrate mimic allows high-throughput assay of the FabA protein and consequently the identification of a novel inhibitor of pseudomonas aeruginosa FabA  Academic Article
  • A substrate-free activity-based protein profiling screen for the discovery of selective PREPL inhibitors  Academic Article
  • ATM-dependent phosphorylation of MEF2D promotes neuronal survival after DNA damage  Academic Article
  • ATP-competitive, marine derived natural products that target the DEAD box helicase, eIF4A  Academic Article
  • Abenzyl 10-formyl-trideazafolic acid (abenzyl 10-formyl-TDAF): an effective inhibitor of glycinamide ribonucleotide transformylase  Academic Article
  • Aberrant autolysosomal regulation is linked to the induction of embryonic senescence: differential roles of Beclin 1 and p53 in vertebrate Spns1 deficiency  Academic Article
  • Abrogation of complex glycosylation by swainsonine results in strain- and cell-specific inhibition of prion replication  Academic Article
  • Academic cross-fertilization by public screening yields a remarkable class of protein phosphatase methylesterase-1 inhibitors  Academic Article
  • Acceptor specificity and inhibition of the bacterial cell-wall glycosyltransferase murg  Academic Article
  • Acceptor substrate-based selective inhibition of galactosyltransferases  Academic Article
  • Activation of JNK3 alpha 1 requires both MKK4 and MKK7: Kinetic characterization of in vitro phosphorylated JNK3 alpha 1  Academic Article
  • Activation of Rac-1 Rac-2, and Cdc42 by hemopoietic growth factors or cross-linking of the B-lymphocyte receptor for antigen  Academic Article
  • Active and alkylated human agt structures: A novel zinc site, inhibitor and extrahelical base binding  Academic Article
  • Active and inhibited human catalase structures: Ligand and nadph binding and catalytic mechanism  Academic Article
  • Active site residues of cyclophilin A are crucial for its signaling activity via CD147  Academic Article
  • Activity-based protein profiling of protein arginine methyltransferase 1  Academic Article
  • Adaptations for the oxidation of polycyclic aromatic hydrocarbons exhibited by the structure of human P450 1A2  Academic Article
  • Adenosine analogue inhibitors of S-adenosylhomocysteine hydrolase  Academic Article
  • Adenovirus endocytosis requires actin cytoskeleton reorganization mediated by rho family gtpases  Academic Article
  • Advancing biological understanding and therapeutics discovery with small-molecule probes  Academic Article
  • Affinity-based ranking of ligands for DPP-4 from mixtures  Academic Article
  • Agonist-specific coupling of growth hormone secretagogue receptor type 1a to different intracellular signaling systems. Role of adenosine  Academic Article
  • Akt regulates the subcellular localization of the Rab27a-binding protein JFC1 by phosphorylation  Academic Article
  • Aldehyde and phosphinate analogs of glutathione and glutathionylspermidine: potent, selective binding inhibitors of the E. coli bifunctional glutathionylspermidine synthetase/amidase  Academic Article
  • Aldehyde dehydrogenase inhibitors: A comprehensive review of the pharmacology, mechanism of action, substrate specificity, and clinical application  Academic Article
  • All roads lead to PP2A: exploiting the therapeutic potential of this phosphatase  Academic Article
  • Allosteric inhibitors have distinct effects, but also common modes of action, in the HCV polymerase  Academic Article
  • Alpha-Keto heterocycle inhibitors of fatty acid amide hydrolase: carbonyl group modification and alpha-substitution  Academic Article
  • Amino acid residues critical for differential inhibition of CYP2B4, CYP2B5, and CYP2B1 by phenylimidazoles  Academic Article
  • Amino hydroxamic acids as potent inhibitors of leukotriene A4 hydrolase  Academic Article
  • Aminoimidazo[1,2-a]pyridines as a new structural class of cyclin-dependent kinase inhibitors. Part 1: Design, synthesis, and biological evaluation  Academic Article
  • An all-purpose antimalarial drug target  Academic Article
  • An anatomical and temporal portrait of physiological substrates for fatty acid amide hydrolase  Academic Article
  • An endogenous sleep-inducing compound is a novel competitive inhibitor of fatty acid amide hydrolase  Academic Article
  • An enzyme that regulates ether lipid signaling pathways in cancer annotated by multidimensional profiling  Academic Article
  • An epigenetic modifier induces production of (10'S)-verruculide B, an inhibitor of protein tyrosine phosphatases by Phoma sp. nov. LG0217, a fungal endophyte of Parkinsonia microphylla  Academic Article
  • An essential role of phosphatidylinositol 3-kinase in myogenic differentiation  Academic Article
  • An inhibitor of NEDD8-activating enzyme as a new approach to treat cancer  Academic Article
  • An inhibitor of sequence-specific proteolysis that targets the substrate rather than the enzyme  Academic Article
  • Analogs of zanamivir with modified c4-substituents as the inhibitors against the group-1 neuraminidases of influenza viruses  Academic Article
  • Analysis of PUGNAc and NAG-thiazoline as transition state analogues for human O-GlcNAcase: mechanistic and structural insights into inhibitor selectivity and transition state poise  Academic Article
  • Anandamide inhibits metabolism and physiological actions of 2-arachidonoylglycerol in the striatum  Academic Article
  • Anchored plasticity opens doors for selective inhibitor design in nitric oxide synthase  Academic Article
  • Annonacin, a natural mitochondrial complex i inhibitor, causes tau pathology in cultured neurons  Academic Article
  • Anti-tumor promoting effects of palmitoyl: protein thioesterase inhibitors against a human neurotumor cell line  Academic Article
  • Antibacterial agents that inhibit two-component signal transduction systems  Academic Article
  • Antimitotic agents of natural origin  Academic Article
  • Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase  Academic Article
  • Asymmetric synthesis of inhibitors of glycinamide ribonucleotide transformylase  Academic Article
  • Autophagy activation and protection from mitochondrial dysfunction in human chondrocytes  Academic Article
  • Azetidine and piperidine carbamates as efficient, covalent inhibitors of monoacylglycerol lipase  Academic Article
  • BACE1- and BACE2-expressing human cells - characterization of beta-amyloid precursor protein-derived catabolites, design of a novel fluorimetric assay, and identification of new in vitro inhibitors  Academic Article
  • Bacillus subtilis rapa phosphatase domain interaction with its substrate, phosphorylated spo0f, and its inhibitor, the phra peptide  Academic Article
  • Basis for the checkpoint signal specificity that regulates Chk1 and Cds1 protein kinases  Academic Article
  • Behavioral evidence for the interaction of oleamide with multiple neurotransmitter systems  Academic Article
  • Benzothiophene piperazine and piperidine urea inhibitors of fatty acid amide hydrolase (FAAH)  Academic Article
  • Benzylidene rhodanines as novel inhibitors of UDP-N-acetylmuramate/L-alanine ligase  Academic Article
  • Beyond protein binding: recent advances in screening DNA-encoded libraries  Academic Article
  • Bicyclic azetidines target acute and chronic stages of Toxoplasma gondii by inhibiting parasite phenylalanyl t-RNA synthetase  Academic Article
  • Binding and inactivation mechanism of a humanized fatty acid amide hydrolase by alpha-ketoheterocycle inhibitors revealed from cocrystal structures  Academic Article
  • Binding of 3,4,5,6-tetrahydroxyazepanes to the acid-β-glucosidase active site: implications for pharmacological chaperone design for Gaucher disease  Academic Article
  • Binding site for blood coagulation factor Xa involving residues 311-325 in factor Va  Academic Article
  • Binding sites for blood coagulation factor Xa and protein S involving residues 493-506 in factor Va  Academic Article
  • Biochemical characterization of aspartyl phosphate phosphatase interaction with a phosphorylated response regulator and its inhibition by a pentapeptide  Academic Article
  • Biochemical, cellular, and biophysical characterization of a potent inhibitor of mutant isocitrate dehydrogenase IDH1  Academic Article
  • Biological and structural evaluation of 10R- and 10S-methylthio-DDACTHF reveals a new role for sulfur in inhibition of glycinamide ribonucleotide transformylase  Academic Article
  • Biological evaluation of hepatitis C virus helicase inhibitors  Academic Article
  • Bisubstrate analogue structure-activity relationships for p300 histone acetyltransferase inhibitors  Academic Article
  • Blockade of 2-arachidonoylglycerol hydrolysis by selective monoacylglycerol lipase inhibitor 4-nitrophenyl 4-(dibenzo d 1,3 dioxol-5-yl(hydroxy)methyl)piperidine-1-carboxylate (jzl184) enhances retrograde endocannabinoid signaling  Academic Article
  • Blockade of endocannabinoid-degrading enzymes attenuates neuropathic pain  Academic Article
  • Blockade of nitric oxide synthesis reduces responding for cocaine self-administration during extinction and reinstatement  Academic Article
  • Blocking an N-terminal acetylation-dependent protein interaction inhibits an E3 ligase  Academic Article
  • Blocking of fatty acid amide hydrolase activity with PF-04457845 in human brain: a positron emission tomography study with the novel radioligand [(11)C]CURB  Academic Article
  • Bradykinin stimulates phosphoinositide turnover and phospholipase C but not phospholipase D and NADPH oxidase in human neutrophils  Academic Article
  • Brief report: combined chemical treatment enables Oct4-induced reprogramming from mouse embryonic fibroblasts  Academic Article
  • Bromotyrosine-derived natural and synthetic products as inhibitors of mycothiol-S-conjugate amidase  Academic Article
  • C-2-symmetrical tetrahydroxyazepanes as inhibitors of glycosidases and hiv/fiv proteases  Academic Article
  • CDK2/cyclinA inhibitors: Targeting the cyclinA recruitment site with small molecules derived from peptide leads  Academic Article
  • CVT-313, a specific and potent inhibitor of CDK2 that prevents neointimal proliferation  Academic Article
  • Calmodulin regulation of calcium stores in phototransduction of Drosophila  Academic Article
  • Carbon monoxide as a novel central pyrogenic mediator  Academic Article
  • Cardiac glycosides are potent inhibitors of interferon-beta gene expression  Academic Article
  • Caspase cascades in human immunodeficiency virus-associated neurodegeneration  Academic Article
  • Cathepsins X and B can be differentiated through their respective mono- and dipeptidyl carboxypeptidase activities  Academic Article
  • Cathepsins X and B display distinct activity profiles that can be exploited for inhibitor design  Academic Article
  • Cdk1 coordinates cell-surface growth with the cell cycle  Academic Article
  • Cefoxitin is both an inhibitor of class A beta-lactamase of Xanthomonas campestris pv. campestris str. 17 and an inducer of its gene  Academic Article
  • Cell-based optimization of novel benzamides as potential antimalarial leads  Academic Article
  • Cellular applications of a sensitive and selective fiber optic nitric oxide biosensor based on a dye-labeled heme domain of soluble guanylate cyclase  Academic Article
  • Cellular zinc content is a major determinant of iron chelator-induced apoptosis of thymocytes  Academic Article
  • Characterization and manipulation of the acyl chain selectivity of fatty acid amide hydrolase  Academic Article
  • Characterization of H7N9 influenza A viruses isolated from humans  Academic Article
  • Characterization of T-5 N-oxide formation as the first highly selective measure of CYP3A5 activity  Academic Article
  • Characterization of a selective inhibitor of the parkinson's disease kinase lrrk2  Academic Article
  • Characterization of a serine hydrolase targeted by acyl-protein thioesterase inhibitors in Toxoplasma gondii  Academic Article
  • Characterization of dasatinib and its structural analogs as CYP3A4 mechanism-based inactivators and the proposed bioactivation pathways  Academic Article
  • Characterization of monoacylglycerol lipase inhibition reveals differences in central and peripheral endocannabinoid metabolism  Academic Article
  • Characterization of non-nitrocatechol pan and isoform specific catechol-O-methyltransferase inhibitors and substrates  Academic Article
  • Characterization of small RNAs in aplysia reveals a role for miR-124 in constraining synaptic plasticity through CREB  Academic Article
  • Characterization of the 26S proteasome network in Plasmodium falciparum  Academic Article
  • Characterization of the first potent and selective PDE9 inhibitor using a cGMP reporter cell line  Academic Article
  • Chemical and mutagenic investigations of fatty acid amide hydrolase: Evidence for a family of serine hydrolases with distinct catalytic properties  Academic Article
  • Chemical fragments as foundations for understanding target space and activity prediction  Academic Article
  • Chemical genetic modifier screens: Small molecule trichostatin suppressors as probes of intracellular histone and tubulin acetylation  Academic Article
  • Chemical probes identify a role for histone deacetylase 3 in Friedreich's ataxia gene silencing  Academic Article
  • Chemical probes of endocannabinoid metabolism  Academic Article
  • Chemical proteomic probes for profiling cytochrome P450 activities and drug interactions in vivo  Academic Article
  • Chemical strategies for activity-based proteomics  Academic Article
  • Chemical synthesis and biological evaluation of palmerolide a analogues  Academic Article
  • Chemoenzymatic synthesis of iminocyclitol derivatives: A useful library strategy for the development of selective fucosyltransfer enzymes inhibitors  Academic Article
  • Chemoenzymatic synthesis: Application to the study of carbohydrate recognition  Academic Article
  • Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway  Academic Article
  • Chemoproteomic discovery of AADACL1 as a regulator of human platelet activation  Academic Article
  • Chemoproteomics-enabled discovery of a potent and selective inhibitor of the DNA repair protein MGMT  Academic Article
  • Chitinase inhibitors: Extraction of the active framework from natural argifin and use of in situ click chemistry  Academic Article
  • Chk1 suppresses a caspase-2 apoptotic response to DNA damage that bypasses p53, Bcl-2, and caspase-3  Academic Article
  • Chronic interleukin-6 exposure alters metabotropic glutamate receptor-activated calcium signalling in cerebellar Purkinje neurons  Academic Article
  • Chronic monoacylglycerol lipase blockade causes functional antagonism of the endocannabinoid system  Academic Article
  • Chronic morphine treatment alters nmda receptor-mediated synaptic transmission in the nucleus accumbens  Academic Article
  • Cis-Amide isosteric replacement in thienobenzoxepin inhibitors of PI3-kinase  Academic Article
  • Class ipi3k in oncogenic cellular transformation  Academic Article
  • Closing the gate to the active site: Effect of the inhibitor methoxyarachidonyl fluorophosphonate on the conformation and membrane binding of fatty acid amide hydrolase  Academic Article
  • Combinatorial approach to N-substituted aminocyclitol libraries by solution-phase parallel synthesis and preliminary evaluation as glucocerebrosidase inhibitors  Academic Article
  • Combinatorial approach toward synthesis of small molecule libraries as bacterial transglycosylase inhibitors  Academic Article
  • Combinatorial library of five-membered iminocyclitol and the inhibitory activities against glyco-enzymes  Academic Article
  • Combinatorial synthesis of novel and potent inhibitors of NADH:ubiquinone oxidoreductase  Academic Article
  • Combined inhibition of FAAH and COX produces enhanced anti-allodynic effects in mouse neuropathic and inflammatory pain models  Academic Article
  • Combining a PI3K inhibitor with a PARP inhibitor provides an effective therapy for BRCA1-related breast cancer  Academic Article
  • Complete inhibition of cdk/cyclin by one molecule of p21(cip1)  Academic Article
  • Confirming target engagement for reversible inhibitors in vivo by kinetically tuned activity-based probes  Academic Article
  • Conformational flexibility in crystal structures of human 11 β-hydroxysteroid dehydrogenase type I provide insights into glucocorticoid interconversion and enzyme regulation  Academic Article
  • Conformationally-restricted arginine analogues as alternative substrates and inhibitors of nitric oxide syntheses  Academic Article
  • Conserved amino acid residues of the NuoD segment important for structure and function of Escherichia coli NDH-1 (complex I)  Academic Article
  • Control of cortical interneuron migration by neurotrophins and pi3-kinase signaling  Academic Article
  • Control of experimental spasticity by targeting the degradation of endocannabinoids using selective fatty acid amide hydrolase inhibitors  Academic Article
  • Conversion of mouse epiblast stem cells to an earlier pluripotency state by small molecules  Academic Article
  • Covalent inhibitors: an opportunity for rational target selectivity  Academic Article
  • Covalent modification of DNA regulates memory formation  Academic Article
  • Creep of trabecular bone from the human proximal tibia  Academic Article
  • Critical role of integrin alpha 5 beta 1 in urokinase (uPA)/urokinase receptor (uPAR, CD87) signaling  Academic Article
  • Crosstalk between nitric oxide and zinc pathways to neuronal cell death involving mitochondrial dysfunction and p38-activated K+ channels  Academic Article
  • Crystal structure of a cytochrome P450 2B6 genetic variant in complex with the inhibitor 4-(4-chlorophenyl)imidazole at 2.0-A resolution  Academic Article
  • Crystal structure of fatty acid amide hydrolase bound to the carbamate inhibitor urb597: Discovery of a deacylating water molecule and insight into enzyme inactivation  Academic Article
  • Crystal structure of human carboxylesterase 1 complexed with the Alzheimer's drug tacrine: from binding promiscuity to selective inhibition  Academic Article
  • Crystal structure of human cytochrome p450 2d6 with prinomastat bound  Academic Article
  • Crystal structure of the membrane-bound bifunctional transglycosylase pbp1b from escherichia coli  Academic Article
  • Crystal structure of the potent natural product inhibitor balanol in complex with the catalytic subunit of camp-dependent protein kinase  Academic Article
  • Crystal structures of human bifunctional enzyme aminoimidazole-4-carboxamide ribonucleotide transformylase/IMP cyclohydrolase in complex with potent sulfonyl-containing antifolates  Academic Article
  • Crystal structures of leukotriene a(4) hydrolase in complex with captopril and two competitive tight-binding inhibitors  Academic Article
  • Crystal structures of protein phosphatase-1 bound to nodularin-R and tautomycin: a novel scaffold for structure-based drug design of serine/threonine phosphatase inhibitors  Academic Article
  • Cu2+ and zn2+ inhibit nitric-oxide synthase through an interaction with the reductase domain  Academic Article
  • Curing a viral infection by targeting the host: The example of cyclophilin inhibitors  Academic Article
  • Cyclic amidine sugars as transition-state analogue inhibitors of glycosidases: Potent competitive inhibitors of mannosidases  Academic Article
  • Cytomegalovirus activates interferon immediate-early response gene expression and an interferon regulatory factor 3-containing interferon-stimulated response element-binding complex  Academic Article
  • Cytoskeletal breakdown and apoptosis elicited by NO donors in cerebellar granule cells require NMDA receptor activation  Academic Article
  • D-fructose-6-phosphate aldolase-catalyzed one-pot synthesis of iminocyclitols  Academic Article
  • DNA double-strand break repair pathway choice Is directed by distinct MRE11 nuclease activities  Academic Article
  • DNA methylation and histone acetylation work in concert to regulate memory formation and synaptic plasticity  Academic Article
  • DNA-dependent protein kinase inhibitors as drug candidates for the treatment of cancer  Academic Article
  • Dacapo, a cyclin-dependent kinase inhibitor, stops cell proliferation during drosophila development  Academic Article
  • Definition of 2 angiogenic pathways by distinct alpha(v) integrins  Academic Article
  • Dehydratase-specific probes for fatty acid and polyketide synthases  Academic Article
  • Delineation of a fundamental alpha-ketoheterocycle substituent effect for use in the design of enzyme inhibitors  Academic Article
  • Design and characterization of mechanism-based inhibitors for the tyrosine aminomutase sgtam  Academic Article
  • Design and synthesis of 1,2,3-triazole-containing N-acyl zanamivir analogs as potent neuraminidase inhibitors  Academic Article
  • Design and synthesis of 2-substituted-5-(4-trifluoromethylphenyl-sulphonamido)benzoxazole derivatives as human GST P1-1 inhibitors  Academic Article
  • Design and synthesis of dihydrobenzofuran amides as orally bioavailable, centrally active gamma-secretase modulators  Academic Article
  • Design and synthesis of novel hybrid benzamide-peptide histone deacetylase inhibitors  Academic Article
  • Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase  Academic Article
  • Design of allele-specific protein methyltransferase inhibitors  Academic Article
  • Design of molecular logic devices based on a programmable DNA-regulated semisynthetic enzyme  Academic Article
  • Design, synthesis and biological evaluation of 10-CF3CO-DDACTHF analogues and derivatives as inhibitors of GAR Tfase and the de novo purine biosynthetic pathway  Academic Article
  • Design, synthesis and evaluation of Fe-s targeted adenosine 5'-phosphosulfate reductase inhibitors  Academic Article
  • Design, synthesis, and activity of HDAC inhibitors with a N-formyl hydroxylamine head group  Academic Article
  • Design, synthesis, and biochemical evaluation of phosphonate and phosphonamidate analogs of glutathionylspermidine as inhibitors of glutathionylspermidine synthetase/amidase from Escherichia coli  Academic Article
  • Design, synthesis, and biological activities of closantel analogues: structural promiscuity and its impact on Onchocerca volvulus  Academic Article
  • Design, synthesis, and biological activity of substrate competitive SMYD2 inhibitors  Academic Article
  • Design, synthesis, and biological evaluation of 10-methanesulfonyl-DDACTHF, 10-methanesulfonyl-5-DACTHF, and 10-methylthio-DDACTHF as potent inhibitors of GAR Tfase and the de novo purine biosynthetic pathway  Academic Article
  • Design, synthesis, and biological evaluation of fluoronitrophenyl substituted folate analogues as potential inhibitors of GAR transformylase and AICAR transformylase  Academic Article
  • Design, synthesis, and biological evaluation of simplified alpha-keto heterocycle, trifluoromethyl ketone, and formyl substituted folate analogues as potential inhibitors of GAR transformylase and AICAR transformylase  Academic Article
  • Design, synthesis, and evaluation of potential GAR and AICAR transformylase inhibitors  Academic Article
  • Design, synthesis, and kinetic characterization of protein N-terminal acetyltransferase inhibitors  Academic Article
  • Desorption/ionization on silicon (dios): A diverse mass spectrometry platform for protein characterization  Academic Article
  • Developing inhibitors to selectively target two-component and phosphorelay signal transduction systems of pathogenic microorganisms  Academic Article
  • Development and characterization of nonpeptidic small molecule inhibitors of the XIAP/caspase-3 interaction  Academic Article
  • Development and optimization of piperidyl-1,2,3-triazole ureas as selective chemical probes of endocannabinoid biosynthesis  Academic Article
  • Development of 6-substituted indolylquinolinones as potent Chek1 kinase inhibitors  Academic Article
  • Development of GlcNAc-Inspired Iminocyclitiols as Potent and Selective N-Acetyl-beta-Hexosaminidase Inhibitors  Academic Article
  • Development of an HTS-compatible assay for the discovery of ASK1 signalosome inhibitors using alphascreen technology  Academic Article
  • Development of fucosyltransferase and fucosidase inhibitors  Academic Article
  • Development of human cGAS-specific small-molecule inhibitors for repression of dsDNA-triggered interferon expression  Academic Article
  • Development of selective tight-binding inhibitors of leukotriene-a4 hydrolase  Academic Article
  • Differential effects of endocannabinoid catabolic inhibitors on morphine withdrawal in mice  Academic Article
  • Differential effects of synaptic and extrasynaptic NMDA receptors on Aβ-induced nitric oxide production in cerebrocortical neurons  Academic Article
  • Differential mechanisms of morphine antinociceptive tolerance revealed in beta arrestin-2 knock-out mice  Academic Article
  • Differentiation of mouse keratinocytes is accompanied by pkc-dependent changes in ap-1 proteins  Academic Article
  • Dipyridyl amides: Potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists  Academic Article
  • Discovering potent and selective reversible inhibitors of enzymes in complex proteomes  Academic Article
  • Discovery and characterization of a highly selective FAAH inhibitor that reduces inflammatory pain  Academic Article
  • Discovery and optimization of indoles and 7-azaindoles as Rho kinase (ROCK) inhibitors (part-I)  Academic Article
  • Discovery and optimization of piperidyl-1,2,3-triazole ureas as potent, selective, and in vivo-active inhibitors of α/β-hydrolase domain containing 6 (ABHD6)  Academic Article
  • Discovery and optimization of potent and selective benzonaphthyridinone analogs as small molecule mTOR inhibitors with improved mouse microsome stability  Academic Article
  • Discovery of PF-06928215 as a high affinity inhibitor of cGAS enabled by a novel fluorescence polarization assay  Academic Article
  • Discovery of a 3-amino-6-phenyl-pyridazine derivative as a new synthetic antineuroinflammatory compound  Academic Article
  • Discovery of a highly selective CYP3A4 inhibitor suitable for reaction phenotyping studies and differentiation of CYP3A4 and CYP3A5  Academic Article
  • Discovery of a selective covalent inhibitor of lysophospholipase-like 1 (LYPLAL1) as a tool to evaluate the role of this serine hydrolase in metabolism  Academic Article
  • Discovery of a series of efficient, centrally efficacious BACE1 inhibitors through structure-based drug design  Academic Article
  • Discovery of aicar tfase inhibitors that disrupt requisite enzyme dimerization  Academic Article
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  • In vitro biological activity of a novel small-molecule inhibitor of polo-like kinase 1  Academic Article
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  • In vivo characterization of the highly selective monoacylglycerol lipase inhibitor KML29: antinociceptive activity without cannabimimetic side effects  Academic Article
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  • Structure-based design and discovery of potent and selective KDM5 inhibitors  Academic Article
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  • Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (nampt) inhibitors.  Academic Article
  • Structure-based identification of ureas as novel nicotinamide phosphoribosyltransferase (Nampt) inhibitors  Academic Article
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  • Synthesis and activity of largazole analogues with linker and macrocycle modification  Academic Article
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  • Tautomycin suppresses growth and neuroendocrine hormone markers in carcinoid cells through activation of the raf-1 pathway  Academic Article
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  • The development and application of methods for activity-based protein profiling  Academic Article
  • The discovery and development of inhibitors of fatty acid amide hydrolase (FAAH)  Academic Article
  • The discovery of a new structural class of cyclin-dependent kinase inhibitors, aminoimidazo[1,2-a]pyridines  Academic Article
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  • The selective monoacylglycerol lipase inhibitor MJN110 produces opioid-sparing effects in a mouse neuropathic pain model  Academic Article
  • The structure of jnk3 in complex with small molecule inhibitors: Structural basis for potency and selectivity  Academic Article
  • The structure of nitric oxide synthase oxygenase domain and inhibitor complexes  Academic Article
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  • The synthesis and evaluation of 3-substituted-7-(alkylidene)cephalosporin sulfones as β-lactamase inhibitors  Academic Article
  • The synthesis and evaluation of 6-alkylidene-2'β-substituted penam sulfones as β-lactamase inhibitors  Academic Article
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  • Total synthesis and molecular target of largazole, a histone deacetylase inhibitor  Academic Article
  • Total synthesis of (-)-bafilomycin A(1)  Academic Article
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  • Total synthesis of the CP-molecules (CP-263,114 and CP-225,917, phomoidrides B and A). 2. Model studies for the construction of key structural elements and first-generation strategy  Academic Article
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