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Relaxed Substrate Requirements of Sterol 14α-Demethylase from Are Accompanied by Resistance to Inhibition.
Hargrove TY, Wawrzak Z, Rachakonda G, Nes WD, Villalta F, Guengerich FP, Lepesheva GI
(2021) J Med Chem 64: 17511-17522
MeSH Terms: 14-alpha Demethylase Inhibitors, Ligands, Naegleria fowleri, Sterol 14-Demethylase, Substrate Specificity
Added November 30, 2021
0 Communities
1 Members
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5 MeSH Terms
Specificity and affinity of the N-terminal residues in staphylocoagulase in binding to prothrombin.
Maddur AA, Kroh HK, Aschenbrenner ME, Gibson BHY, Panizzi P, Sheehan JH, Meiler J, Bock PE, Verhamme IM
(2020) J Biol Chem 295: 5614-5625
MeSH Terms: Bacterial Proteins, Binding Sites, Coagulase, Humans, Models, Molecular, Protein Binding, Prothrombin, Staphylococcal Infections, Staphylococcus aureus, Substrate Specificity
Added March 21, 2020
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1 Members
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10 MeSH Terms
Engineering cytochrome P450 enzyme systems for biomedical and biotechnological applications.
Li Z, Jiang Y, Guengerich FP, Ma L, Li S, Zhang W
(2020) J Biol Chem 295: 833-849
MeSH Terms: Biocatalysis, Biotechnology, Cytochrome P-450 Enzyme System, Metabolic Engineering, Protein Engineering, Steroids, Substrate Specificity, Xenobiotics
Added March 3, 2020
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8 MeSH Terms
Human cytochrome P450 enzymes bind drugs and other substrates mainly through conformational-selection modes.
Guengerich FP, Wilkey CJ, Phan TTN
(2019) J Biol Chem 294: 10928-10941
MeSH Terms: Catalysis, Cytochrome P-450 CYP2D6, Cytochrome P-450 CYP2E1, Cytochrome P-450 CYP3A, Cytochrome P-450 Enzyme Inhibitors, Cytochrome P-450 Enzyme System, Humans, Kinetics, Lauric Acids, Ligands, Molecular Conformation, Oxidation-Reduction, Palmitic Acid, Protein Binding, Protein Conformation, Spiro Compounds, Substrate Specificity
Added March 3, 2020
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17 MeSH Terms
Conformational selection dominates binding of steroids to human cytochrome P450 17A1.
Guengerich FP, Wilkey CJ, Glass SM, Reddish MJ
(2019) J Biol Chem 294: 10028-10041
MeSH Terms: 17-alpha-Hydroxypregnenolone, 17-alpha-Hydroxyprogesterone, Androstenes, Humans, Kinetics, Protein Conformation, Steroid 17-alpha-Hydroxylase, Substrate Specificity
Added March 3, 2020
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1 Members
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MeSH Terms
A Novel Class of Common Docking Domain Inhibitors That Prevent ERK2 Activation and Substrate Phosphorylation.
Sammons RM, Perry NA, Li Y, Cho EJ, Piserchio A, Zamora-Olivares DP, Ghose R, Kaoud TS, Debevec G, Bartholomeusz C, Gurevich VV, Iverson TM, Giulianotti M, Houghten RA, Dalby KN
(2019) ACS Chem Biol 14: 1183-1194
MeSH Terms: Binding Sites, Crystallography, X-Ray, Dose-Response Relationship, Drug, Enzyme Activation, Guanidine, Humans, Mitogen-Activated Protein Kinase 1, Nuclear Magnetic Resonance, Biomolecular, Phosphorylation, Protein Kinase Inhibitors, Substrate Specificity
Added March 18, 2020
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MeSH Terms
Axonal organization defects in the hippocampus of adult conditional BACE1 knockout mice.
Ou-Yang MH, Kurz JE, Nomura T, Popovic J, Rajapaksha TW, Dong H, Contractor A, Chetkovich DM, Tourtellotte WG, Vassar R
(2018) Sci Transl Med 10:
MeSH Terms: Aging, Amyloid Precursor Protein Secretases, Animals, Animals, Newborn, Apoptosis, Aspartic Acid Endopeptidases, Axons, Cognition, Epilepsy, Gene Deletion, Hippocampus, Long-Term Potentiation, Memory Disorders, Mice, Inbred C57BL, Mice, Knockout, Myelin Sheath, Neurogenesis, Phenotype, Substrate Specificity
Added April 2, 2019
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1 Members
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19 MeSH Terms
VHL substrate transcription factor ZHX2 as an oncogenic driver in clear cell renal cell carcinoma.
Zhang J, Wu T, Simon J, Takada M, Saito R, Fan C, Liu XD, Jonasch E, Xie L, Chen X, Yao X, Teh BT, Tan P, Zheng X, Li M, Lawrence C, Fan J, Geng J, Liu X, Hu L, Wang J, Liao C, Hong K, Zurlo G, Parker JS, Auman JT, Perou CM, Rathmell WK, Kim WY, Kirschner MW, Kaelin WG, Baldwin AS, Zhang Q
(2018) Science 361: 290-295
MeSH Terms: Animals, Carcinoma, Renal Cell, Chromatin Immunoprecipitation, Female, Gene Expression Regulation, Neoplastic, Homeodomain Proteins, Humans, Hydroxylation, Kidney Neoplasms, Mice, Mice, SCID, Molecular Targeted Therapy, Mutation, NF-kappa B, Oncogenes, Substrate Specificity, Transcription Factors, Von Hippel-Lindau Tumor Suppressor Protein
Added October 30, 2019
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MeSH Terms
Discovery, Characterization, and Effects on Renal Fluid and Electrolyte Excretion of the Kir4.1 Potassium Channel Pore Blocker, VU0134992.
Kharade SV, Kurata H, Bender AM, Blobaum AL, Figueroa EE, Duran A, Kramer M, Days E, Vinson P, Flores D, Satlin LM, Meiler J, Weaver CD, Lindsley CW, Hopkins CR, Denton JS
(2018) Mol Pharmacol 94: 926-937
MeSH Terms: Animals, Binding Sites, Diuretics, Electrolytes, HEK293 Cells, Humans, Male, Models, Molecular, Molecular Docking Simulation, Molecular Structure, Mutagenesis, Site-Directed, Potassium Channels, Inwardly Rectifying, Rats, Small Molecule Libraries, Substrate Specificity
Added April 10, 2019
0 Communities
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MeSH Terms
Structural basis of ligand binding modes at the neuropeptide Y Y receptor.
Yang Z, Han S, Keller M, Kaiser A, Bender BJ, Bosse M, Burkert K, Kögler LM, Wifling D, Bernhardt G, Plank N, Littmann T, Schmidt P, Yi C, Li B, Ye S, Zhang R, Xu B, Larhammar D, Stevens RC, Huster D, Meiler J, Zhao Q, Beck-Sickinger AG, Buschauer A, Wu B
(2018) Nature 556: 520-524
MeSH Terms: Arginine, Binding Sites, Crystallography, X-Ray, Dihydropyridines, Diphenylacetic Acids, Humans, Inositol Phosphates, Ligands, Molecular Docking Simulation, Mutant Proteins, Mutation, Neuropeptide Y, Nuclear Magnetic Resonance, Biomolecular, Phenylurea Compounds, Protein Binding, Receptors, Neuropeptide Y, Structure-Activity Relationship, Substrate Specificity
Added March 21, 2020
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MeSH Terms