Search Results - "Fleck, Beth A."

Binding kinetics redefine the antagonist pharmacology of the corticotropin-releasing factor type 1 receptor by Fleck, Beth A, Hoare, Sam R J, Pick, Rebecca R, Bradbury, Margaret J, Grigoriadis, Dimitri E

“…Corticotropin-releasing factor (CRF) receptor antagonists are under preclinical and clinical investigation for stress-related disorders. In this study the…”
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Allosteric ligands for the corticotropin releasing factor type 1 receptor modulate conformational states involved in receptor activation by Hoare, Sam R J, Fleck, Beth A, Gross, Raymond S, Crowe, Paul D, Williams, John P, Grigoriadis, Dimitri E

“…Allosteric modulators of G-protein-coupled receptors can regulate conformational states involved in receptor activation ( Mol Pharmacol 58: 1412-1423, 2000 )…”
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Studies on the structure–activity relationship of bicifadine analogs as monoamine transporter inhibitors by Zhang, Mingzhu, Jovic, Florence, Vickers, Troy, Dyck, Brian, Tamiya, Junko, Grey, Jonathan, Tran, Joe A., Fleck, Beth A., Pick, Rebecca, Foster, Alan C., Chen, Chen

“…Compounds with various activities and selectivities were discovered through structure–activity relationship studies of bicifadine analogs as monoamine…”
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The importance of target binding kinetics for measuring target binding affinity in drug discovery: a case study from a CRF1 receptor antagonist program by Hoare, Sam R.J., Fleck, Beth A., Williams, John P., Grigoriadis, Dimitri E.

“…[Display omitted] •Knowledge of target binding kinetics is required for accurate measurement of drug affinity.•Incorrect affinity estimates resulting from slow…”
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Identification of 1S,2R-milnacipran analogs as potent norepinephrine and serotonin transporter inhibitors by TAMIYA, Junko, DYCK, Brian, FOSTER, Alan C, CHEN CHEN, MINGZHU ZHANG, PHAN, Kasey, FLECK, Beth A, APARICIO, Anna, JOVIC, Florence, TRAN, Joe A, VICKERS, Troy, GREY, Jonathan

“…A series of milnacipran analogs were synthesized and studied as monoamine transporter inhibitors, and several potent compounds with moderate lipophilicity were…”
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Studies on the SAR and pharmacophore of milnacipran derivatives as monoamine transporter inhibitors by Chen, Chen, Dyck, Brian, Fleck, Beth A., Foster, Alan C., Grey, Jonathan, Jovic, Florence, Mesleh, Michael, Phan, Kasey, Tamiya, Junko, Vickers, Troy, Zhang, Mingzhu

“…Derivatives of milnacipran were synthesized and studied as monoamine transporter inhibitors. Potent analogs were discovered at NET ( 9k) and at both NET and…”
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Studies on a series of milnacipran analogs containing a heteroaromatic group as potent norepinephrine and serotonin transporter inhibitors by Vickers, Troy, Dyck, Brian, Tamiya, Junko, Zhang, Mingzhu, Jovic, Florence, Grey, Jonathan, Fleck, Beth A., Aparicio, Anna, Johns, Michael, Jin, Liping, Tang, Hui, Foster, Alan C., Chen, Chen

“…A series of milnacipran analogs containing a heteroaromatic group were synthesized and studied as monoamine transporter inhibitors. Many compounds exhibited…”
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Design, Synthesis, In Vitro, and In Vivo Characterization of Phenylpiperazines and Pyridinylpiperazines as Potent and Selective Antagonists of the Melanocortin-4 Receptor by Tran, Joe A, Jiang, Wanlong, Tucci, Fabio C, Fleck, Beth A, Wen, Jenny, Sai, Yang, Madan, Ajay, Chen, Ta Kung, Markison, Stacy, Foster, Alan C, Hoare, Sam R, Marks, Daniel, Harman, John, Chen, Caroline W, Arellano, Melissa, Marinkovic, Dragan, Bozigian, Haig, Saunders, John, Chen, Chen

“…Benzylamine and pyridinemethylamine derivatives were synthesized and characterized as potent and selective antagonists of the melanocortin-4 receptor (MC4R)…”
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Potent and orally active non-peptide antagonists of the human melanocortin-4 receptor based on a series of trans-2-disubstituted cyclohexylpiperazines by Tucci, Fabio C., White, Nicole S., Markison, Stacy, Joppa, Margaret, Tran, Joe A., Fleck, Beth A., Madan, Ajay, Dyck, Brian P., Parker, Jessica, Pontillo, Joseph, Melissa Arellano, L., Marinkovic, Dragan, Jiang, Wanlong, Chen, Caroline W., Gogas, Kathleen R., Goodfellow, Val S., Saunders, John, Foster, Alan C., Chen, Chen

“…The melanocortin-4 receptor (MC4R) plays an important role in the regulation of energy homeostasis. Recent studies have shown that blockade of the MC4R…”
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A potent and selective nonpeptide antagonist of the melanocortin-4 receptor induces food intake in satiated mice by Pontillo, Joseph, Tran, Joseph A., Markison, Stacy, Joppa, Margaret, Fleck, Beth A., Marinkovic, Dragan, Arellano, Melissa, Tucci, Fabio C., Lanier, Marion, Nelson, Jodie, Saunders, John, Hoare, Sam R.J., Foster, Alan C., Chen, Chen

“…[Display omitted] Optimization on a series of piperazinebenzylamines resulted in analogues with low nanomolar binding at the human MC4 receptor but weak…”
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The Regulation of Feeding and Metabolic Rate and the Prevention of Murine Cancer Cachexia with a Small-Molecule Melanocortin-4 Receptor Antagonist by Markison, Stacy, Foster, Alan C, Chen, Chen, Brookhart, Gregor B, Hesse, Amy, Hoare, Sam R. J, Fleck, Beth A, Brown, Brock T, Marks, Daniel L

“…Cachexia is metabolic disorder characterized by anorexia, an increased metabolic rate, and loss of lean body mass. It is a relatively common disorder, and is a…”
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Substituted NDP-MSH Peptides Paired with Mutant Melanocortin-4 Receptors Demonstrate the Role of Transmembrane 6 in Receptor Activation by Fleck, Beth A, Ling, Nicholas, Chen

“…The melanocortin-4 receptor (MC4R) is involved in regulating energy homeostasis and is a potential therapeutic target for obesity and cachexia. Molecular…”
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Synthesis and structure–activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with a heterocyclic ring constraint by Hudson, Sarah, Kiankarimi, Mehrak, Eccles, Wendy, Mostofi, Yalda S., Genicot, Marc J., Dwight, Wesley, Fleck, Beth A., Gogas, Kathleen, Wade, Warren S.

“…A series of heterocyclic ring-constrained norepinephrine reuptake inhibitors have activities as racemates equivalent to atomoxetine (IC 50’s < 10 nM). The…”
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Discovery of a potent, selective, and less flexible selective norepinephrine reuptake inhibitor (sNRI) by Wu, Dongpei, Pontillo, Joseph, Ching, Brett, Hudson, Sarah, Gao, Yinghong, Fleck, Beth A., Gogas, Kathleen, Wade, Warren S.

“…A rigid ring-constrained norepinephrine reuptake inhibitor with potent functional activity at the transporter (IC 50 = 8 nM) was used to develop a model for…”
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Pyrrolidines as potent functional agonists of the human melanocortin-4 receptor by Tran, Joe A., Chen, Caroline W., Jiang, Wanlong, Tucci, Fabio C., Fleck, Beth A., Marinkovic, Dragan, Arellano, Melissa, Chen, Chen

“…A series of pyrrolidine derivatives were synthesized and characterized as potent agonists of the human melanocortin-4 receptor. For example, 28c had a K i of…”
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Discovery of 1-{2-[(1S)-(3-Dimethylamino-propionyl)amino-2-methylpropyl]-4-methyl-phenyl}-4-[(2R)-methyl-3-(4-chlorophenyl)-propionyl]piperazine as an Orally Active Antagonist of the Melanocortin-4 Receptor for the Potential Treatment of Cachexia by Chen, Chen, Jiang, Wanlong, Tucci, Fabio, Tran, Joe A, Fleck, Beth A, Hoare, Sam R, Joppa, Margaret, Markison, Stacy, Wen, Jenny, Sai, Yang, Johns, Michael, Madan, Ajay, Chen, Takung, Chen, Caroline W, Marinkovic, Dragan, Arellano, Melissa, Saunders, John, Foster, Alan C

“…A potent and selective antagonist of the melanocortin-4 receptor,…”
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Syntheses of tetrahydrothiophenes and tetrahydrofurans and studies of their derivatives as melanocortin-4 receptor ligands by Tran, Joe A., Chen, Caroline W., Tucci, Fabio C., Jiang, Wanlong, Fleck, Beth A., Chen, Chen

“…Piperazinebenzylamine derivatives from trans-4-(4-chlorophenyl)tetrahydrothiophene-3-carboxylic acid 6 and its S-oxide 7 and sulfone 8, and the tetrahydrofuran…”
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Kinetics of nonpeptide antagonist binding to the human gonadotropin-releasing hormone receptor: Implications for structure–activity relationships and insurmountable antagonism by Sullivan, Susan K., Hoare, Sam R.J., Fleck, Beth A., Zhu, Yun-Fei, Heise, Christopher E., Struthers, R. Scott, Crowe, Paul D.

“…Numerous nonpeptide ligands have been developed for the human gonadotropin-releasing hormone (GnRH) receptor as potential agents for treatment of disorders of…”
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Pharmacological and pharmacokinetic characterization of 2-piperazine-α-isopropyl benzylamine derivatives as melanocortin-4 receptor antagonists by Chen, Chen, Tucci, Fabio C., Jiang, Wanlong, Tran, Joe A., Fleck, Beth A., Hoare, Sam R., Wen, Jenny, Chen, Takung, Johns, Michael, Markison, Stacy, Foster, Alan C., Marinkovic, Dragan, Chen, Caroline W., Arellano, Melissa, Harman, John, Saunders, John, Bozigian, Haig, Marks, Daniel

“…A series of 2-piperazine-α-isopropylbenzylamine derivatives were synthesized and characterized as melanocortin-4 receptor (MC4R) antagonists. Attaching an…”
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4-{(2R)-[3-Aminopropionylamido]-3-(2,4-dichlorophenyl)propionyl}-1-{2-[(2-thienyl)ethylaminomethyl]phenyl}piperazine as a Potent and Selective Melanocortin-4 Receptor AntagonistDesign, Synthesis, and Characterization by Chen, Pontillo, Joseph, Fleck, Beth A, Gao, Yinghong, Wen, Jenny, Tran, Joe A, Tucci, Fabio C, Marinkovic, Dragan, Foster, Alan C, Saunders, John

“…Recent studies have demonstrated that melanocortin-4 receptor (MC4R) antagonists can prevent weight loss in tumor-bearing mice, which indicates clinical usage…”
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