- The alpha-factor mating pheromone of Saccharomyces cerevisiae: a model for studying the interaction of peptide hormones and G protein-coupled receptors
Department of Chemistry, College of Staten Island and Institute for Macromolecular Assemblies of The City University of New York, Staten Island, NY 10314, USA
Peptides 25:1441-63. 2004
..Many features of this yeast recognition system are relevant to and have counterparts in mammalian cells...
- Neutralization of the aspartic acid residue Asp-367, but not Asp-454, inhibits binding of Na+ to the glutamate-free form and cycling of the glutamate transporter EAAC1
Department of Physiology and Biophysics, University of Miami School of Medicine, 1600 NW 10th Avenue, Miami, FL 33136, USA
J Biol Chem 281:10263-72. 2006
..Our data are consistent with a model in which Asp-367, but not Asp-454, is involved in coordinating the bound Na(+) in the glutamate-free transporter form...
- Nicotinic acetylcholine receptors on basophils and mast cells
P S Sudheer
Department of Anaesthetics and Intensive Care Medicine, University Hospital of Wales, Cardiff, UK
Anaesthesia 61:1170-4. 2006
..The identity of this receptor was confirmed by reverse transcriptase PCR and quantitative PCR...
- Competitive binding of poly- and perfluorinated compounds to the thyroid hormone transport protein transthyretin
Jana M Weiss
Institute for Environmental Studies, Department of Chemistry and Biology, VU University, 1081 HV Amsterdam, The Netherlands
Toxicol Sci 109:206-16. 2009
..b>Competitive binding of PFCs to TTR, as observed for human TTR in the present study, may explain altered thyroid hormone levels ..
- A 26 S protease subunit that binds ubiquitin conjugates
Department of Biochemistry, University of Utah School of Medicine, Salt Lake City 84132
J Biol Chem 269:7059-61. 1994
..Thus, proteins conjugated to polymers of ubiquitin may be selected for degradation by a single subunit of the 26 S protease complex...
- Syntaxin 5 is a common component of the NSF- and p97-mediated reassembly pathways of Golgi cisternae from mitotic Golgi fragments in vitro
Cell Biology Laboratory, Imperial Cancer Research Fund, London, United Kingdom
Cell 92:603-10. 1998
..p47 also mediates the binding of p97 to syntaxin 5 and so plays an analogous role to alpha-SNAP, which mediates the binding of NSF...
- Recombinant transthyretin purification and competitive binding with organohalogen compounds in two gull species (Larus argentatus and Larus hyperboreus)
National Wildlife Research Centre, Carleton University, Ottawa, Ontario, K1A 0H3, Canada
Toxicol Sci 107:440-50. 2009
..the OH-substituted analogs all had lower K(i) and K(d) values, indicating greater affinity and more potent competitive binding to both T(3) and T(4)...
- Changes in conformation and subcellular distribution of alpha4beta2 nicotinic acetylcholine receptors revealed by chronic nicotine treatment and expression of subunit chimeras
Patricia C Harkness
Department of Pharmacology, University College London, London, WC1E 6BT, United Kingdom
J Neurosci 22:10172-81. 2002
..The finding that subunit conformation can be influenced by coassembled subunit partners is in agreement with models of receptor assembly which propose that subunit folding continues after initial subunit-subunit interactions...
- Elucidating the relationship between DISC1, NDEL1 and NDE1 and the risk for schizophrenia: evidence of epistasis and competitive binding
Katherine E Burdick
Department of Psychiatry Research, The Zucker Hillside Hospital, North Shore Long Island Jewish Health System, Glen Oaks, NY 11004, USA
Hum Mol Genet 17:2462-73. 2008
..These data suggest that NDEL1 significantly influences risk for SZ via an interaction with DISC1. We propose a model where NDEL1 and NDE1 compete for binding with DISC1...
- Potent competitive interactions of some brominated flame retardants and related compounds with human transthyretin in vitro
I A Meerts
Toxicology Group, Department of Food Technology and Nutritional Sciences, Wageningen University and Research Center, Tuinlaan 5, 6703 HE Wageningen, The Netherlands
Toxicol Sci 56:95-104. 2000
..the possible interaction of several brominated flame retardants with T(4) binding to TTR in an in vitro competitive binding assay, using human TTR and 125 I-T(4) as the displaceable radioligand...
- Dual interactions of the translational repressor Paip2 with poly(A) binding protein
Department of Biochemistry and McGill Cancer Center, McGill University, Montreal, Quebec, Canada H3G 1Y6
Mol Cell Biol 21:5200-13. 2001
..Significantly, only the central Paip2 fragment, which binds with high affinity to the PABP RRM region, inhibits PABP binding to poly(A) RNA and translation...
- CD4-induced interaction of primary HIV-1 gp120 glycoproteins with the chemokine receptor CCR-5
LeukoSite, Inc, Cambridge, Massachusetts 02142, USA
Nature 384:179-83. 1996
..These results suggest that HIV-1 attachment to CD4 creates a high-affinity binding site for CCR-5, leading to membrane fusion and virus entry...
- RAC-3 is a NF-kappa B coactivator
Deparmento de Cs Biológicas, Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Ciudad Universitaria, Pabellon II, Argentina
FEBS Lett 485:195-9. 2000
..The competition between GR and NF-kappa B for binding to RAC3 may represent a general mechanism by which both transcription factors mutually antagonize their activity...
- Function of sigma1 receptors in Parkinson's disease
The Department of Neurology, Neurological Institute, Nippon Medical School Chiba Hokusoh Hospital, Inba gun, Chiba, Japan
Acta Neurol Scand 112:103-7. 2005
- Inhibition of the transcription of CYP1A1 gene by the upstream stimulatory factor 1 in rabbits. Competitive binding of USF1 with AhR.Arnt complex
Division of Drug Metabolism, Faculty of Pharmaceutical Sciences, Hokkaido University, N12W6, Kita ku, Sapporo, Hokkaido 060, Japan
J Biol Chem 272:30025-31. 1997
..These results indicate that the XRE of the rabbit CYP1A1 gene is recognized by the basic helix-loop-helix proteins to regulate the expression of CYP1A1 in both an agonistic (AhR.Arnt) and an antagonistic (USF1) manner...
- Polyamines regulate the stability of JunD mRNA by modulating the competitive binding of its 3' untranslated region to HuR and AUF1
Department of Surgery, University of Maryland School of Medicine, Baltimore, Maryland 21201, USA
Mol Cell Biol 30:5021-32. 2010
..JunD mRNA is a target of HuR and AUF1 and that polyamines modulate JunD mRNA degradation by altering the competitive binding of HuR and AUF1 to the JunD 3'-UTR...
- Competitive binding exchange between alkali metal ions (K+, Rb+, and Cs+) and Na+ ions bound to the dimeric quadruplex [d(G4T4G4)]2: a 23Na and 1H NMR study
Flaminia Cesare Marincola
Dipartimento di Scienze Chimiche, Universita di Cagliari, Cittadella Universitaria di Monserrato, S S 554 Bivio per Sestu, I 09042, Monserrato, Cagliari, Italy
Magn Reson Chem 47:1036-42. 2009
- ULBP1, 2, 3: novel MHC class I-related molecules that bind to human cytomegalovirus glycoprotein UL16, activate NK cells
Department of Immunobiology, Immunex Corporation, Seattle 98101, USA
Eur J Immunol 31:1428-37. 2001
..Addition of soluble recombinant UL16 protein inhibited the biological activities mediated by ULBP, suggesting the existence of a novel mechanism utilized by CMV to evade elimination by the host immune system...
- Local conformations and competitive binding affinities of single- and double-stranded primer-template DNA at the polymerization and editing active sites of DNA polymerases
Institute of Molecular Biology and Department of Chemistry, University of Oregon, Eugene, Oregon 97403 1229, USA
J Biol Chem 284:17180-93. 2009
..These distributions and the conformational changes in the P/T DNA that occur during template-directed DNA synthesis in solution illuminate some of the mechanisms used by DNA polymerases to assure the fidelity of DNA synthesis...
- Streptococcus gordonii Hsa environmentally constrains competitive binding by Streptococcus sanguinis to saliva-coated hydroxyapatite
Angela H Nobbs
Department of Diagnostic and Biological Sciences, University of Minnesota, 17 164 Moos Tower, 515 Delaware Street, S E, Minneapolis, MN 55455, USA
J Bacteriol 189:3106-14. 2007
..Next, putative S. gordonii adhesins were analyzed for contributions to interspecies competitive binding. Like wild-type S...
- The behavior of mixtures of paralytic shellfish toxins in competitive binding assays
Lyndon E Llewellyn
Australian Institute of Marine Science, PMB 3, Townsville MC, Queensland, 4810, Australia
Chem Res Toxicol 19:661-7. 2006
..This equation has been extended to mixtures of PSTs containing more than three toxins and may be applicable to other natural contaminants and any competitive binding assays used to detect their presence and measure their concentration.
- Development of a competitive binding assay system with recombinant estrogen receptors from multiple species
Cynthia V Rider
Department of Molecular Biomedical Sciences, North Carolina State University, Raleigh, NC 27606, USA
Toxicol Lett 184:85-9. 2009
..This system provides a convenient in vitro approach for directly comparing chemical binding to estrogen receptors across multiple species without the need to sacrifice animals...
- Electrochemical survey of the chain length influence in phytochelatins competitive binding by cadmium
Departament de Quimica Analitica, Universitat de Barcelona, Spain
Anal Biochem 406:61-9. 2010
..with alternating least squares (MCR-ALS) was applied to voltammetric data obtained in the analysis of the competitive binding of glutathione (GSH) and phytochelatins [(gammaGlu-Cys)(n)-Gly, PC(n), n=2-5] by Cd(2+)...
- Collaborative competition mechanism for gene activation in vivo
Joanna A Miller
Department of Biochemistry, Molecular Biology and Cellular Biology, Northwestern University, Evanston, Illinois 60208-3500, USA
Mol Cell Biol 23:1623-32. 2003
..We speculate that initial target site recognition and binding may occur via spontaneous nucleosomal site exposure, with remodeling factor action required downstream to lock in higher levels of regulatory protein occupancy...
- The steroid-responsive hiccup reflex arc: competitive binding to the corticosteroid-receptor?
Rob D Dickerman
Department of Neurosurgery, North Shore University Hospital, New Hyde Park, NY, USA
Neuro Endocrinol Lett 24:167-9. 2003
..This report validates the previous report on anabolic steroids inducing hiccups and exemplifies the ability for steroids as a class, due to there backbone structural homology, to induce function even as competitive inhibitors...
- The CXC chemokine SDF-1 is the ligand for LESTR/fusin and prevents infection by T-cell-line-adapted HIV-1
Unite d Immunologie Virale, Institut Pasteur, Paris, France
Nature 382:833-5. 1996
- A mechanism of translational repression by competition of Paip2 with eIF4G for poly(A) binding protein (PABP) binding
Muhammad M Karim
Department of Biochemistry and McGill Cancer Center, McGill University, Montreal, QC, Canada H3G 1Y6
Proc Natl Acad Sci U S A 103:9494-9. 2006
..Thus, Paip2 can inhibit translation by a previously unrecognized mechanism, which is independent of its ability to disrupt PABP-poly(A) interaction...
- Receptor-mediated effects on ligand availability influence relative mitogenic potencies of epidermal growth factor and transforming growth factor alpha
C C Reddy
Department of Chemical Engineering, University of Illinois at Urbana Champaign, Urbana, Illinois 61801, USA
J Cell Physiol 166:512-22. 1996
..Our results suggest a model of regulation of hormone responsiveness which favors dissociative ligands (such as TGF alpha) in receptor-limited situations and non-dissociative ligands (such as EGF) in the face of high receptor levels...
- Cooperative and competitive binding in synergistic mixtures of Thermobifida fusca cellulases Cel5A, Cel6B, and Cel9A
Department of Biological and Environmental Engineering and Department of Molecular Biology and Genetics, Cornell University, Ithaca, New York 14853, USA
Biotechnol Prog 18:760-9. 2002
- PKCepsilon activation induces dichotomous cardiac phenotypes and modulates PKCepsilon-RACK interactions and RACK expression
J M Pass
Department of Physiology and Biophysics, University of Louisville, Louisville, Kentucky 40292, USA
Am J Physiol Heart Circ Physiol 280:H946-55. 2001
..Our observations demonstrate that RACK expression is dynamically regulated by PKCepsilon and suggest that differential patterns of PKCepsilon-RACK interactions may be important determinants of PKCepsilon-dependent cardiac phenotypes...
- Pesticides interfere with the nongenomic action of a progestogen on meiotic maturation by binding to its plasma membrane receptor on fish oocytes
Department of Internal Medicine, Yale University, School of Medicine, VA Medical Center, West Haven, CT 06516, USA
Endocrinology 140:1953-6. 1999
..The close correspondence between competitive binding of the two pesticides to the 20beta-S membrane receptor and their inhibition of 20beta-S induced FOM ..
- Binding of the G domains of laminin alpha1 and alpha2 chains and perlecan to heparin, sulfatides, alpha-dystroglycan and several extracellular matrix proteins
J F Talts
Max Planck Institut fur Biochemie, Am Klopferspitz 18a, D 82152 Martinsried, Germany
EMBO J 18:863-70. 1999
..This demonstrated similar binding repertoires for the LG modules of three basement membrane proteins involved in cell-matrix interactions and supramolecular assembly...
- Tyrosine 302 in RACK1 is essential for insulin-like growth factor-I-mediated competitive binding of PP2A and beta1 integrin and for tumor cell proliferation and migration
Patrick A Kiely
Department of Biochemistry, Biosciences Institute, University College Cork, Ireland
J Biol Chem 283:22952-61. 2008
..Taken together, the data demonstrate that Tyr-302 in RACK1 is required for interaction with PP2A and beta1 integrin, for regulation of PP2A activity, and for IGF-I-mediated cell migration and proliferation...
- Maintenance of antigen-specific immunological memory through variable regions of heavy and light chains of anti-idiotypic antibody
Department of Microbiology and Cell Biology, Indian Institute of Science, Bangalore, Karnataka, India
Immunology 120:486-96. 2007
..Evidence has been provided for the existence of an antigen-specific B-cell idiotypic network in the body that supports the perpetuation of immunological memory as proposed in the relay hypothesis...
- Block of CaV1.2 channels by Gd3+ reveals preopening transitions in the selectivity filter
Department of Pharmacology and Physiology, University of Medicine and Dentistry of New Jersey, New Jersey Medical School, Newark, NJ 07103, USA
J Gen Physiol 129:461-75. 2007
..Therefore, we propose that at submicromolar concentrations, Gd(3+) binds at the entry to the selectivity locus and that the affinity of the site for permeant ions decreases during preopening transitions of the channel...
- B lymphocyte-induced maturation protein (Blimp)-1, IFN regulatory factor (IRF)-1, and IRF-2 can bind to the same regulatory sites
Tracy C Kuo
Department of Microbiology, College of Physicians and Surgeons, Columbia University, New York, NY 10032, USA
J Immunol 173:5556-63. 2004
..Thus, our data suggest that Blimp-1 competes in vivo with a subset of IRF proteins and help predict the sites and IRF family members that may be affected...
- Competitive binding of AUF1 and TIAR to MYC mRNA controls its translation
Department of Molecular Genetics, Microbiology, and Immunology, Robert Wood Johnson Medical School, University of Medicine and Dentistry of New Jersey, 675 Hoes Lane, Piscataway, New Jersey 08854, USA
Nat Struct Mol Biol 14:511-8. 2007
..Together, these observations suggest a novel regulatory mechanism where tuning the ratios of AUF1 and TIAR bound to MYC mRNA permits dynamic control of MYC translation and cell proliferation...
- In vitro and in vivo binding of neuroactive steroids to the sigma-1 receptor as measured with the positron emission tomography radioligand [18F]FPS
Rikki N Waterhouse
Department of Psychiatry, Columbia University, New York, New York, USA
Synapse 61:540-6. 2007
- Evaluation of novel antimouse VEGFR2 antibodies as potential antiangiogenic or vascular targeting agents for tumor therapy
Simmons Comprehensive Cancer Center, University of Texas Southwestern Medical Center, Dallas, TX 75390-8594, USA
Neoplasia 5:297-307. 2003
..Vascular damage was not observed in normal organs, including kidneys and pancreas. These studies demonstrate that anti-VEGFR2 antibodies have potential for vascular targeting and imaging of tumors in vivo...
- Model of competitive binding of vascular endothelial growth factor and placental growth factor to VEGF receptors on endothelial cells
Feilim Mac Gabhann
Department of Biomedical Engineering, School of Medicine, Johns Hopkins University, Traylor 613, 720 Rutland Ave, Baltimore, MD 21205, USA
Am J Physiol Heart Circ Physiol 286:H153-64. 2004
..These results suggest that VEGFR1 signaling can be functional in adult-derived endothelial cells...
- HEXIM1 is a promiscuous double-stranded RNA-binding protein and interacts with RNAs in addition to 7SK in cultured cells
Department of Biochemistry, University of Iowa, Iowa City, Iowa 52242, USA
Nucleic Acids Res 35:2503-12. 2007
..Our study illuminates novel properties of HEXIM1 both in vitro and in vivo, and suggests that HEXIM1 may be involved in other nuclear and cytoplasmic processes besides controlling P-TEFb...
- Tat competes with HEXIM1 to increase the active pool of P-TEFb for HIV-1 transcription
Department of Medicine, Rosalind Russell Medical Research Center, University of California at San Francisco, San Francisco, CA 94143 0703, USA
Nucleic Acids Res 35:2003-12. 2007
..All these data are consistent with the model that Tat not only recruits but also increases the active pool of P-TEFb for efficient HIV-1 transcription...
- New multifunctional molecular conjugate vector for targeting, imaging, and therapy of tumors
Groupe de Recherche sur le Cancer du Poumon, INSERM U578, Institut Albert Bonniot, La Tronche 38706 Cedex, France
Mol Ther 12:1168-75. 2005
- Antiobesity efficacy of a novel cannabinoid-1 receptor inverse agonist, N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-[[5-(trifluoromethyl)pyridin-2-yl]oxy]propanamide (MK-0364), in rodents
Tung M Fong
Department of Metabolic Disorders, Merck Research Laboratories, R80M 213, P O Box 2000, Rahway, NJ 07065, USA
J Pharmacol Exp Ther 321:1013-22. 2007
..These studies demonstrated that MK-0364 is a highly potent and selective CB1R inverse agonist and that it is orally active in rodent models of obesity...
- Aha1 competes with Hop, p50 and p23 for binding to the molecular chaperone Hsp90 and contributes to kinase and hormone receptor activation
Protein Folding Group, Institute for Genetics, University of Bonn, , D-53117 Bonn, Germany
Biochem J 387:789-96. 2005
- [3H]N-[4-(3,4-dihydro-6,7-dimethoxyisoquinolin-2(1H)-yl)butyl]-2-methoxy-5-methylbenzamide: a novel sigma-2 receptor probe
Department of Radiology, Washington University School of Medicine, 510 S. Kingshighway Blvd, St. Louis, MO 63110, USA
Eur J Pharmacol 525:8-17. 2005
..b>Competitive binding assays were also conducted using a panel of compounds with known affinity for sigma2 receptors...
- Guanine nucleotide exchange factors operate by a simple allosteric competitive mechanism
Department of Structural Biology, Max-Planck Institute of Molecular Physiology, Otto-Hahn-Strasse 11, 44227 Dortmund, Germany
Biochemistry 44:15423-9. 2005
..In addition, we present arguments, which demonstrate how the erroneous conclusions leading to the alternative model were derived...
- Competitive binding of CREB and ATF2 to cAMP/ATF responsive element regulates eNOS gene expression in endothelial cells
Department of Medicine and Biological Science, Gunma University Graduate School of Medicine, Japan
Arterioscler Thromb Vasc Biol 26:1036-42. 2006
..Furthermore, the ability to bind both CREB and ATF2 implicates the CRE/ATF sequence as a potential target for multiple signaling pathways in the regulation of the eNOS gene transcription...
- Structure-activity relationships of new 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric enhancers of the A3 adenosine receptor
Division of Medicinal Chemistry, Leiden Amsterdam Center for Drug Research, Leiden University, P O Box 9502, 2300 RA, Leiden, The Netherlands
J Med Chem 49:3354-61. 2006
..Thus, we have prepared allosteric enhancers of the human A3AR that have an improved allosteric effect in comparison to the inhibition of equilibrium binding at the orthosteric site...
- TIP47 is a key effector for Rab9 localization
Department of Biochemistry, Stanford University School of Medicine, Stanford, CA 94305, USA
J Cell Biol 173:917-26. 2006
..These data confirm the importance of effector interactions for Rab9 localization, and support a model in which effector proteins rely on Rabs as much as Rabs rely on effectors to achieve their correct steady state localizations...
- Glucose sensors based on microcapsules containing an orange/red competitive binding resonance energy transfer assay
Biomedica Engineering Program, Institute for Micromanufacturing, Louisiana Tech University, Ruston, 71272, USA
Diabetes Technol Ther 8:269-78. 2006
..A recent development towards this goal is a highly specific and sensitive competitive binding assay for glucose using apo-glucose oxidase (apo-GOx) as the recognition element and dextran as the ..
- Aptamers targeted to an RNA hairpin show improved specificity compared to that of complementary oligonucleotides
INSERM U386, , 33076 Bordeaux, France
Biochemistry 45:12076-82. 2006
..These results demonstrate the benefit of reading the three-dimensional shape of an RNA target rather than its primary sequence for the design of highly specific oligonucleotides...
- Endocrine disruptor bisphenol A strongly binds to human estrogen-related receptor gamma (ERRgamma) with high constitutive activity
Laboratory of Structure-Function Biochemistry, Department of Chemistry, Faculty and Graduate School of Sciences, Kyushu University, Fukuoka 812-8581, Japan
Toxicol Lett 167:95-105. 2006
..It will now be important to evaluate whether BPA's hitherto reported low dose effects may be mediated through ERRgamma...
- Saturated fat-induced changes in Sf 60-400 particle composition reduces uptake of LDL by HepG2 cells
Kim G Jackson
School of Food Biosciences, University of Reading, Reading, Berkshire, United Kingdom
J Lipid Res 47:393-403. 2006
..008). In conclusion, these findings suggest an alternative or additional mechanism whereby acute fat ingestion can influence LDL clearance via competitive apoE-dependent effects of TRL on the LDL receptor...
- Competitive binding of pentraxins and IgM to newly exposed epitopes on late apoptotic cells
Caroline L F Ciurana
Department of Immunopathology, Sanquin Research at CLB, Plesmanlaan 125, 1066 CX Amsterdam, The Netherlands
Cell Immunol 239:14-21. 2006
..This shared specificity as well as their shared capability to activate complement, suggest that IgM and the pentraxins CRP and SAP exert similar functions in the removal of apoptotic cells...
- Steroid and G protein binding characteristics of the seatrout and human progestin membrane receptor alpha subtypes and their evolutionary origins
University of Texas Marine Science Institute, 750 Channel View Drive, Port Aransas, Texas 78373, USA
Endocrinology 148:705-18. 2007
..Thus, mPRs arose from Eubacteria independently from members of the GPCR superfamily, which arose from Archeabacteria, suggesting convergent evolution of seven-transmembrane hormone receptors coupled to G proteins...
- The anomalous behaviour of exogenous 25-hydroxyvitamin D in competitive binding assays
G D Carter
Department of Clinical Chemistry, Hammersmith Hospitals NHS Trust, London W6 8RF, UK
J Steroid Biochem Mol Biol 103:480-2. 2007
..9, 46.4%, 43.2%, HPLC (n=9); 42.6, 112.2%, 97.1%, LC-MS (n=4); 34.0, 111.5%, 118.1%. The IDS RIA and Nichols assays gave unexpectedly low recoveries. This does not appear to be a calibration problem or the effect of ethanol...
- Satellite DNA binding and cellular localisation of RNA helicase P68
Cell Cultures Department, Institute of Cytology, Tikhoretsky, 4, St Petersburg, 194064, Russia
J Cell Sci 118:611-22. 2005
..Direct interaction of P68/DEAD box RNA helicase with satellite DNAs in vitro has not been demonstrated for any other members of the RNA helicase family...
- Divalent cation sensitivity of BK channel activation supports the existence of three distinct binding sites
Department of Anesthesiology, Washington University School of Medicine, St. Louis, Missouri 63110, USA
J Gen Physiol 125:273-86. 2005
..The major kinetic effect of the E399-related low affinity mechanism is to slow deactivation at mM Mg2+ or Ca2+. The results support the view that three distinct divalent-cation binding sites mediate regulation of BK channels...
- Design and synthesis of an expanded porphyrin that has selectivity for the c-MYC G-quadruplex structure
College of Pharmacy, The University of Arizona, 1703 East Mabel, Tucson, Arizona 85721, USA
J Am Chem Soc 127:2944-59. 2005
..From this study, we have identified an expanded porphyrin that selectively binds with the c-MYC G-quadruplex in the presence of duplex DNA and other G-quadruplexes...
- The breast cell growth inhibitor, estrogen down regulated gene 1, modulates a novel functional interaction between estrogen receptor alpha and transcriptional elongation factor cyclin T1
Bryan M Wittmann
Department of Pharmacology, Case Western Reserve University, Cleveland, OH 44106, USA
Oncogene 24:5576-88. 2005
..Conversely, increased EDG1 expression results in inhibition of cyclin T1 recruitment and ERalpha DNA binding. Our results support a novel functional interaction between ERalpha and cyclin T1 that is modulated by EDG1...
- Nicotine upregulates its own receptors through enhanced intracellular maturation
CNRS URA D2182 Récepteurs et Cognition, Institut Pasteur, Paris, France
Neuron 46:595-607. 2005
- Synthetic cryptolepine inhibits DNA binding of NF-kappaB
Olumayokun A Olajide
Department of Pharmacy, Center of Drug Research, University of Munich, Butenandtstr 5 13, 81377 Munich, Germany
Bioorg Med Chem 15:43-9. 2007
..This indicates that cryptolepine may exhibit its anti-inflammatory action by blocking DNA binding of activated NF-kappaB and thus transcription of NF-kappaB-regulated proinflammatory proteins...
- Ca2+-dependent inactivation of CaV1.2 channels prevents Gd3+ block: does Ca2+ block the pore of inactivated channels?
Department of Pharmacology and Physiology, University of Medicine and Dentistry of New Jersey, New Jersey Medical School, Newark, NJ 07103, USA
J Gen Physiol 129:477-83. 2007
..A minimal model, in which the inactivation "gate" is an increase in affinity of the selectivity filter for permeating ions, successfully simulates the characteristic U-shaped voltage dependence of inactivation in Ca(2+)...
- The Orf18 gene product from conjugative transposon Tn916 is an ArdA antirestriction protein that inhibits type I DNA restriction-modification systems
School of Chemistry, The University of Edinburgh, The King s Buildings, Edinburgh EH9 3JJ, UK
J Mol Biol 383:970-81. 2008
..Our results suggest that ArdA can overcome the restriction barrier following conjugation and so helps increase the spread of antibiotic resistance genes by horizontal gene transfer...
- Small molecule inhibitors of the MDM2-p53 interaction discovered by ensemble-based receptor models
Anna L Bowman
Department of Medicinal Chemistry and the Comprehensive Cancer Center, University of Michigan, Ann Arbor, MI 48109, USA
J Am Chem Soc 129:12809-14. 2007
..Our MPS technique is one of very few ensemble-based techniques to be proven through experimental verification of the discovery of new inhibitors...
- Androgen binding profiles of two distinct nuclear androgen receptors in Atlantic croaker (Micropogonias undulatus)
T S Sperry
Department of Marine Science, The University of Texas Marine Science Institute, The University of Texas at Austin, 78373, USA
J Steroid Biochem Mol Biol 73:93-103. 2000
..Atlantic croaker (Micropogonias undulatus) brain and ovarian tissues, respectively, were determined using competitive binding assays...
- Stimulation of aromatase P450 promoter (II) activity in endometriosis and its inhibition in endometrium are regulated by competitive binding of steroidogenic factor-1 and chicken ovalbumin upstream promoter transcription factor to the same cis-acting elem
Cecil H Ida Green Center for Reproductive Biology Sciences, Department of Obstetrics and Gynecology, The University of Texas Southwestern Medical Center, Dallas 75235 9051, USA
Mol Endocrinol 13:239-53. 1999
- Vitronectin binding to IGF binding protein-5 (IGFBP-5) alters IGFBP-5 modulation of IGF-I actions
Division of Endocrinology, University of North Carolina, Chapel Hill, NC 27599, USA
Endocrinology 143:30-6. 2002
..Synthetic peptides that contained four distinct regions of the IGFBP-5 sequence were used in competitive binding assays to determine the regions of IGFBP-5 that were necessary for vitronectin binding...
- Biotransformation of brominated flame retardants into potentially endocrine-disrupting metabolites, with special attention to 2,2',4,4'-tetrabromodiphenyl ether (BDE-47)
Institute for Environmental Studies IVM, Vrije Universiteit Amsterdam, Amsterdam, The Netherlands
Mol Nutr Food Res 52:284-98. 2008
..In combination with other environmentally relevant hydroxylated organohalogens acting on TTR-binding and E2SULT inhibition, internal exposure to BFR metabolites may significantly contribute to the overall risk of endocrine disruption...
- Competitive binding of xenobiotic oestrogens to rat alpha-fetoprotein and to sex steroid binding proteins in human and rainbow trout (Oncorhynchus mykiss) plasma
S R Milligan
Physiology Group, Biomedical Sciences Division, King s College London, Strand, London, WC2R 2LS, United Kingdom
Gen Comp Endocrinol 112:89-95. 1998
..These results suggest that environmental oestrogenic agents are unlikely to produce biological effects by displacing endogenous steroids from plasma steroid binding proteins unless they are present in very high concentrations...
- Opposing effects of Ndel1 and alpha1 or alpha2 on cytoplasmic dynein through competitive binding to Lis1
Laboratory of Molecular Cell Biology, Institute of Biochemistry and Cell Biology, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai, China
J Cell Sci 122:2820-7. 2009
..They also help to explain why brain development is particularly sensitive to a decrease in Lis1 levels...
- Development of high throughput screening assays using fluorescence polarization: nuclear receptor-ligand-binding and kinase/phosphatase assays
G J Parker
PanVera Corporation, Madison, WI 53711, USA
J Biomol Screen 5:77-88. 2000
..These data show that an FP-based competitive binding assay can be used to screen diverse compounds with a broad range of binding affinities for ERs...
- Influence of surface shape on DNA binding of bimetallo helicates
Jemma C Peberdy
Department of Chemistry, University of Warwick, Coventry CV4 7AL, UK
J Inorg Biochem 101:1937-45. 2007
..b>Competitive binding studies using fluorescent dyes Hoechst 33258 (a minor groove binder), ethidium bromide (an intercalator) ..
- Host-guest chemistry of dendrimer-drug complexes. 3. Competitive binding of multiple drugs by a single dendrimer for combination therapy
Laboratory of Functional Membranes, Department of Chemistry, University of Science and Technology of China, Hefei, Anhui 230026, PR China
J Phys Chem B 113:14172-9. 2009
..The competitive binding of multiple drugs by a single dendrimer in aqueous solutions was investigated by (1)H NMR and 2D-NOESY ..
- Differential binding affinities of PCBs, HO-PCBs, and aroclors with recombinant human, rainbow trout (Onchorhynkiss mykiss), and green anole (Anolis carolinensis) estrogen receptors, using a semi-high throughput competitive binding assay
Department of Biochemistry and National Food Safety and Toxicology Center, Michigan State University, East Lansing 48824 1319, USA
Toxicol Sci 53:326-39. 2000
..These results demonstrate that ERs from different species exhibit differential ligand preferences and relative binding affinities for PCBs, which can be dramatically affected by DMSO concentration...
- Two distinct head-tail interfaces cooperate to suppress activation of vinculin by talin
Daniel M Cohen
Department of Biological Chemistry, The Johns Hopkins School of Medicine, Baltimore, Maryland 21205, USA
J Biol Chem 280:17109-17. 2005
..Together the D1-Vt and D4-Vt interfaces provide the high affinity (approximately 10(-9)) autoinhibition observed in full-length vinculin...
- pH dependency of ligand binding to cellobiohydrolase 1 (Cel7A). Affinity, selectivity and inhibition for designed propranolol analogues
Organic Chemistry, Department of Chemistry, P O Box 124, Lund University, S 221 00 Lund, Sweden
J Chromatogr A 1138:276-83. 2007
..With support of docking computations we propose a hypothesis on the effect of the ligand structure and pH dependency of the binding and selectivity of amino alcohols to Cel7A...
- An unambiguous assay for the cloned human sigma1 receptor reveals high affinity interactions with dopamine D4 receptor selective compounds and a distinct structure-affinity relationship for butyrophenones
Ivan T Lee
Department of Pharmacology and Neuroscience, University of North Texas Health Science Center, Fort Worth, TX 79107, USA
Eur J Pharmacol 578:123-36. 2008
..The antidepressant fluvoxamine, the drug of abuse methamphetamine, and the neurosteroid progesterone were amongst the many ligands whose interactions with the sigma(1) receptor were confirmed with our screening assay...
- Regulatory interactions between the amino terminus of G-protein betagamma subunits and the catalytic domain of phospholipase Cbeta2
Tabetha M Bonacci
Department of Pharmacology and Physiology, University of Rochester School of Medicine and Dentistry, 601 Elmwood Ave, Rochester, New York 14642, USA
J Biol Chem 280:10174-81. 2005
- Subunit structure of a mammalian ER/Golgi SNARE complex
Department of Biology and Program in Biomedical Sciences, University of Michigan, Ann Arbor, Michigan 48109 1048, USA
J Biol Chem 275:39631-9. 2000
..Finally, we demonstrate that the quaternary complex containing sec22b is not an in vitro entity only, but is a bona fide species in living cells...
- Affinity of cyamemazine metabolites for serotonin, histamine and dopamine receptor subtypes
INSERM U669, Hôpital Universitaire Paul Brousse, Villejuif, France
Eur J Pharmacol 578:142-7. 2008
..Further investigation is required to see if the high affinities of cyamemazine sulfoxide for H(1) and 5-HT(2A) receptors are of therapeutic benefit against sleep onset insomnia and/or sleep maintenance insomnia respectively...
- Molecular modeling of human MT2 melatonin receptor: the role of Val204, Leu272 and Tyr298 in ligand binding
Institute of Physiology, Academy of Sciences of the Czech Republic, Prague, Czech Republic
J Neurochem 91:836-42. 2004
..These data suggest that several new amino acid residues within TM V, VI and VII are involved in ligand-MT2 receptor interaction...
- Dynamic associations of heterochromatin protein 1 with the nuclear envelope
Department of Basic Sciences, The University of Crete School of Medicine, 71 110 Heraklion, Crete, Greece
EMBO J 19:6558-68. 2000
..A His(6)-tagged peptide representing this region inhibited recruitment of LAP2beta and B-type lamins around the surfaces of condensed chromosomes, suggesting involvement of HP1 proteins in nuclear envelope reassembly...
- The crystal structure of transthyretin in complex with diethylstilbestrol: a promising template for the design of amyloid inhibitors
Molecular Structure and Molecular Neurobiology, Instituto de Biologia Molecular e Celular, Universidade do Porto, Rua do Campo Alegre, Number 823, 4150 Porto, Portugal
J Biol Chem 279:53483-90. 2004
..The present study gave us further insight in the molecular mechanism by which DES competes with thyroid hormone binding to TTR and highlights key interactions between DES and TTR that oppose amyloid formation...
- Fluorescent pirenzepine derivatives as potential bitopic ligands of the human M1 muscarinic receptor
Laboratoire de Pharmacochimie de la Communication Cellulaire, , UMR CNRS/ULP 7081, IFR 85, 74 route du Rhin, BP 10413, 67412 Illkirch, France
J Med Chem 47:4300-15. 2004
..The data favor the idea that these analogues might interact with both the acetylcholine and the brucine binding domains...
- Allosteric inhibition of protein tyrosine phosphatase 1B
Sunesis Pharmaceuticals, 341 Oyster Point Boulevard, South San Francisco, California 94080, USA
Nat Struct Mol Biol 11:730-7. 2004
..Allosteric inhibition is a promising strategy for targeting PTP1B and constitutes a mechanism that may be applicable to other tyrosine phosphatases...
- Development and validation of opioid ligand-receptor interaction models: the structural basis of mu vs delta selectivity
H I Mosberg
Department of Medicinal Chemistry, College of Pharmacy, University of Michigan, Ann Arbor 48109 1065, USA
J Pept Res 60:329-35. 2002
..Testing this hypothesis by examining the binding of JOM-6 and several of its key analogs with specific micro receptor mutants is described. Our initial results are consistent with the proposed ligand-receptor interaction models...
- Collagen phagocytosis by fibroblasts is regulated by decorin
Vinay M Bhide
Canadian Institutes of Health Research Group in Matrix Dynamics, Faculty of Dentistry, University of Toronto, Ontario
J Biol Chem 280:23103-13. 2005
..Thus a novel collagen binding domain in decorin acts cooperatively with leucine-rich repeat 4 to mask the alpha2beta1 integrin-binding site on collagen, an important sequence for the phagocytosis of collagen fibrils...
- The nociceptin pharmacophore site for opioid receptor binding derived from the NMR structure and bioactivity relationships
Michael J Orsini
Johnson and Johnson Pharmaceutical Research and Development, LLC, Raritan, New Jersey 08869, USA
J Biol Chem 280:8134-42. 2005
..Structure-activity relationships allowed identification of pharmacophore sites that were used in small molecule data base searches, affording hits with demonstrated nociceptin receptor binding affinities...
- Derivatized 2-furoyl-LIGRLO-amide, a versatile and selective probe for proteinase-activated receptor 2: binding and visualization
Morley D Hollenberg
Department of Pharmacology and Therapeutics, University of Calgary Faculty of Medicine, 3330 Hospital Drive NW, Calgary, AB T2N4N1, Canada
J Pharmacol Exp Ther 326:453-62. 2008
..We conclude that ornithine-derivatized 2fLI peptides are conveniently synthesized PAR2 probes that will be of value for future studies of receptor binding and visualization...
- Sigma1 and sigma2 receptor binding affinity and selectivity of SA4503 and fluoroethyl SA4503
John R Lever
Department of Radiology, University of Missouri Columbia, 65211, USA
Synapse 59:350-8. 2006
..The findings have bearing on structure-activity relationships for this active series, and on conclusions that might be drawn from experiments relying upon defined sigma(1)/sigma(2) binding selectivity...
- Diffuse pharmacophoric domains of vasoactive intestinal peptide (VIP) and further insights into the interaction of VIP with the N-terminal ectodomain of human VPAC1 receptor by photoaffinity labeling with [Bpa6]-VIP
Yossan Var Tan
INSERM U410, Neuroendocrinologie et Biologie Cellulaire Digestives, Institut National de la Sante et de la Recherche Medicale, Faculte de Medecine Xavier Bichat, Paris F 75018, France
J Biol Chem 279:38889-94. 2004
..Altogether these data showed that the central part of VIP, at least between Phe(6) and Tyr(22), interacts with the N-terminal ectodomain of the hVPAC1 receptor...
- Saturation analysis of ligand binding using a centrifugation procedure
R T Layer
Cognetix, Salt Lake City, Utah, USA
Curr Protoc Neurosci . 2001
- A urokinase-type plasminogen activator-inhibiting cyclic peptide with an unusual P2 residue and an extended protease binding surface demonstrates new modalities for enzyme inhibition
Department of Molecular Biology, University of Aarhus, Gustav Wied's Vej 10C, 8000 Aarhus C, Denmark
J Biol Chem 280:38424-37. 2005
..Peptide-derived inhibitors such as upain-1 may provide novel mechanistic information about enzyme-inhibitor interactions and alternative methodologies for designing effective protease inhibitors...
- Functional cartography of the ectodomain of the type I interferon receptor subunit ifnar1
Institute of Biochemistry, Johann Wolfgang Goethe University, Frankfurt am Main, Germany
J Mol Biol 350:476-88. 2005
- Saturation assays of radioligand binding to receptors and their allosteric modulatory sites
National Institute of Diabetes, Digestive, and Kidney Diseases, Bethesda, Maryland, USA
Curr Protoc Neurosci . 2001
..A saturation assay is presented to examine ligand binding to the benzodiazepine site on the GABA-A receptor, while a second protocol uses a similar technique to examine the binding site for GABA in this complex...
- New pansomatostatin ligands and their chelated versions: affinity profile, agonist activity, internalization, and tumor targeting
Division of Radiological Chemistry, University Hospital Basel, Basel, Switzerland
Clin Cancer Res 14:2019-27. 2008
..Currently used targeting peptides mainly have sst2 affinity. We aimed at developing (radio)peptides that bind with high affinity to all receptor subtypes...
- Fancy bioisosteres: metallocene-derived G-protein-coupled receptor ligands with subnanomolar binding affinity and novel selectivity profiles
Department of Medicinal Chemistry, Emil Fischer Center, Friedrich Alexander University, Schuhstrasse 19, D-91052 Erlangen, Germany
J Med Chem 48:3696-9. 2005
..50 nM) and dopamine D3 receptor binding (1b, 0.64 nM) and selective D4 agonist properties of the ruthenocene 1c may be a starting point for highly beneficial central nervous system active drugs...
- Successful in silico discovery of novel nonsteroidal ligands for human sex hormone binding globulin
Division of Infectious Diseases, Faculty of Medicine, University of British Columbia, Heather Pavilion, 2733, Heather Street, Vancouver, British Columbia V5Z 3J5, Canada
J Med Chem 48:3203-13. 2005
..Taken together, the in silico strategy we have developed will aid in the discovery of nonsteroidal ligands of SHBG with novel pharmacological properties...
- Structure-affinity relationship studies on arylpiperazine derivatives related to quipazine as serotonin transporter ligands. Molecular basis of the selectivity SERT/5HT3 receptor
Dipartimento Farmaco Chimico Tecnologico and European Research Centre for Drug Discovery and Development, Universita di Siena, Via A Moro, 53100 Siena, Italy
Bioorg Med Chem 13:3455-60. 2005