Search results for: Maria A. Bednarek

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article

LEAP2 Is an Endogenous Antagonist of the Ghrelin Receptor

Xuecai Ge, Hong Yang, Maria A. Bednarek, Hadas Galon-Tilleman, more

Cell Metabolism > 2018 > 27 > 2 > 461-469.e6

Ghrelin, an appetite-stimulatory hormone secreted by the stomach, was discovered as a ligand for the growth hormone secretagogue receptor (GHSR). Through GHSR, ghrelin stimulates growth hormone (GH) secretion, a function that evolved to protect against starvation-induced hypoglycemia. Though the biology mediated by ghrelin has been described in great detail, regulation of ghrelin action is poorly...

chapter

Potent and selective peptide agonists for human melanocortin receptor 5

Maria A. Bednarek, Tanya MacNeil, Rui Tang, M. Angeles Cabello, more

Advances in Experimental Medicine and Biology > Peptides for Youth > Peptide, Protein, and Peptidomimetic Synthesis honoring Ralph Hirschmann > 95-96

article

Potency optimization of Huwentoxin-IV on hNav1.7: A neurotoxin TTX-S sodium-channel antagonist from the venom of the Chinese bird-eating spider Selenocosmia huwena

Jefferson D. Revell, Per-Eric Lund, John E. Linley, Jacky Metcalfe, more

Peptides > 2013 > 44 > Complete > 40-46

The spider venom peptide Huwentoxin-IV (HwTx-IV) 1 is a potent antagonist of hNa _v 1.7 (IC ₅₀ determined herein as 17±2nM). Na _v 1.7 is a voltage-gated sodium channel involved in the generation and conduction of neuropathic and nociceptive pain signals. We prepared a number of HwTx-IV analogs as part of a structure–function study into Na _v 1.7 antagonism. The inhibitory...

article

MCH receptor peptide agonists and antagonists

Douglas J. MacNeil, Maria A. Bednarek

Peptides > 2009 > 30 > 11 > 2008-2013

Melanin-concentrating hormone (MCH) is an important neuropeptide hormone involved in multiple physiological processes. Peptide derivatives of MCH have been developed as tools to aid research including potent radioligands, receptor selective agonists, and potent antagonists. These tools have been used to further understand the role of MCH in physiology, primarily in rodents. However, the tools could...

article

Cyclic analogs of α-melanocyte-stimulating hormone (αMSH) with high agonist potency and selectivity at human melanocortin receptor 1b

Maria A. Bednarek, Tanya MacNeil, Rui Tang, Tung M. Fong, more

Peptides > 2008 > 29 > 6 > 1010-1017

α-Melanotropin (αMSH), Ac-Ser ¹ -Tyr ² -Ser ³ -Met ⁴ -Glu ⁵ -His ⁶ -Phe ⁷ -Arg ⁸ -Trp ⁹ -Gly ¹⁰ -Lys ¹¹ -Pro ¹² -Val ¹³ -NH ₂ , ¹ 1Throughout this report, the numbering of the amino acid residues in αMSH, Ac-Ser ¹ -Tyr ² -Ser ³ -Met ⁴ -Glu ⁵ ...

article

Potent and Selective Agonists of Human Melanocortin Receptor 5: Cyclic Analogues of α-Melanocyte-Stimulating Hormone ^†

Maria A. Bednarek, Tanya MacNeil, Rui Tang, Tung M. Fong, more

Journal of Medicinal Chemistry > 2007 > 50 > 10 > 2520 - 2526

article

Potent and selective agonists of α-melanotropin (αMSH) action at human melanocortin receptor 5; linear analogs of α-melanotropin

Maria A. Bednarek, Tanya MacNeil, Rui Tang, Tung M. Fong, more

Peptides > 2007 > 28 > 5 > 1020-1028

α-Melanotropin, Ac-Ser ¹ -Tyr-Ser-Met-Glu-His ⁶ -Phe ⁷ -Arg ⁸ -Trp ⁹ -Gly-Lys-Pro-Val ¹³ -NH ₂ ¹ , is a non-selective endogenous agonist for the melanocortin receptor 5; the receptor present in various peripheral tissues and in the brain, cortex and cerebellum. Most of the synthetic analogs of αMSH, including a broadly used and more potent...

article

Characterization of Kir1.1 Channels with the Use of a Radiolabeled Derivative of Tertiapin

John P. Felix, Jessica Liu, William A. Schmalhofer, Timothy Bailey, more

Biochemistry > 2006 > 45 > 33 > 10129 - 10139

article

Chronic MCH-1 receptor modulation alters appetite, body weight and adiposity in rats

Lauren P. Shearman, Ramon E. Camacho, D. Sloan Stribling, Dan Zhou, more

European Journal of Pharmacology > 2003 > 475 > 1-3 > 37-47

Central administration of the neuropeptide melanin-concentrating hormone (MCH) stimulates feeding in rodents. We studied the effects of intracerebroventricular (i.c.v.) administration of an MCH-1 receptor agonist (Compound A) and an MCH-1 receptor antagonist (Compound B) on feeding in satiated rats. Compound B (10 μg, i.c.v.) blocked the acute orexigenic effect of Compound A (5 μg, i.c.v.). In an...

article

''The role of melanocortins in body weight regulation: opportunities for the treatment of obesity''

Douglas J. MacNeil, Andrew D. Howard, Xiaoming Guan, Tung M. Fong, more

European Journal of Pharmacology > 2002 > 450 > 1 > 93-109

Five G-protein-coupled melanocortin receptors (MC ₁ -MC ₅ ) are expressed in mammalian tissues. The melanocortin receptors support diverse physiological functions, including the regulation of hair color, adrenal function, energy homeostasis, feed efficiency, sebaceous gland lipid production and immune and sexual function. The melanocortins (adrenocorticotropic hormone (ACTH), α-melanocyte-stimulating...

article

Synthesis and Biological Evaluation in Vitro of Selective, High Affinity Peptide Antagonists of Human Melanin-Concentrating Hormone Action at Human Melanin-Concentrating Hormone Receptor 1

Maria A. Bednarek, Donna L. Hreniuk, Carina Tan, Oksana C. Palyha, more

Biochemistry > 2002 > 41 > 20 > 6383 - 6390

article

The role of melanocortins in body weight regulation: opportunities for the treatment of obesity

Douglas J. MacNeil, Andrew D. Howard, Xiaoming Guan, Tung M. Fong, more

European Journal of Pharmacology > 2002 > 440 > 2-3 > 141-157

article

Selective, High Affinity Peptide Antagonists of α-Melanotropin Action at Human Melanocortin Receptor 4: Their Synthesis and Biological Evaluation in Vitro ^†

Maria A. Bednarek, Tanya MacNeil, Rubana N. Kalyani, Rui Tang, more

Journal of Medicinal Chemistry > 2001 > 44 > 22 > 3665 - 3672

article

Potent and Selective Peptide Agonists of α-Melanotropin Action at Human Melanocortin Receptor 4: Their Synthesis and Biological Evaluation in Vitro

Maria A. Bednarek, Tanya MacNeil, Rui Tang, Rubana N. Kalyani, more

Biochemical and Biophysical Research Communications > 2001 > 286 > 3 > 641-645

α-Melanotropin (αMSH) and several of its derivatives are potent but not selective agonists at melanocortin receptors 3, 4, and 5 present in the brain (MC3-5R). To differentiate between the physiological role of hMC-4R (believed to be involved in regulation of energy balance) from those of melanocortin receptors 3 and 5, potent and receptor-specific agonists are needed. Therefore, the cyclic derivatives...

article

Short Segment of Human Melanin-Concentrating Hormone That Is Sufficient for Full Activation of Human Melanin-Concentrating Hormone Receptors 1 and 2

Maria A. Bednarek, Scott D. Feighner, Donna L. Hreniuk, Oksana C. Palyha, more

Biochemistry > 2001 > 40 > 31 > 9379 - 9386

article

Analogs of Lactam Derivatives of α-Melanotropin with Basic and Acidic Residues

Maria A. Bednarek, Tanya MacNeil, Rubana N. Kalyani, Rui Tang, more

Biochemical and Biophysical Research Communications > 2000 > 272 > 1 > 23-28

A role of the aromatic and of the basic residues of the potent agonist (MTII) and antagonist (SHU9119) at the human melanocortin receptors 4 in the formation and stabilization of ligand-receptor complexes was examined. Analogs of MTII and SHU9119 with glutamic acid replacing one amino acid at a time were synthesized and tested for their ability to bind to and activate human melanocortin receptors...

article

Analogs of MTII, Lactam Derivatives of α-Melanotropin, Modified at the N-Terminus, and Their Selectivity at Human Melanocortin Receptors 3, 4, and 5

Maria A. Bednarek, Tanya Macneil, Rubana N. Kalyani, Rui Tang, more

Biochemical and Biophysical Research Communications > 1999 > 261 > 1 > 209-213

In search for selective agonists at human melanocortin-4 receptor, proline-substituted analogs of MTII, a potent nonselective agonist at melanocortin receptors, were prepared by solid-phase syntheses and evaluated for their ability to bind and activate human MC-3, MC-4, and MC-5 receptors. Replacement of Nle ⁴ with Pro resulted in [Pro ⁴ ]MTII with affinity to and agonist potency at...

article

Structure-function studies on the cyclic peptide MT-II, lactam derivative of α-melanotropin*

Maria A. Bednarek, Maria V. Silva, Byron Arison, Tanya MacNeil, more

Peptides > 1999 > 20 > 3 > 401-409

The alanine-substituted and the retro, enantio, and retro-enantio analogs of MT-II, a potent agonist at melanocortin (MC) receptors, were prepared by solid-phase synthesis and evaluated for their ability to bind and activate human MC3, MC4, and MC5 receptors. Replacement of His with Ala resulted in [Ala ⁶ ]-MT-II with affinity and agonist potency at human MC3, MC4, and MC5 receptors similar...

article

Development of a Scintillation Proximity Assay for Histone Deacetylase Using a Biotinylated Peptide Derived from Histone-H4

Bakela Nare, John J. Allocco, Richard Kuningas, Stefan Galuska, more

Analytical Biochemistry > 1999 > 267 > 2 > 390-396

Measurement of histone deacetylase activity is usually accomplished by incubation of the enzyme(s) with acetate-radiolabeled histones or synthetic peptides based on histone sequences, followed by extraction and quantification of released radiolabeled acetic acid. Consequently, this assay is both time consuming and extremely limiting when large numbers of samples are involved. We have now developed...

article

Observation of noncovalent complexes between margatoxin and the Kv1.3 peptide ligands: A model investigation using ion-spray mass spectrometry

Ray Bakhtiar, Maria A. Bednarek

Journal of the American Society for Mass Spectrometry > 1996 > 7 > 10 > 1075-1080

Margatoxin (MgTX), a 39 amino acid peptide present in the venom of the new world scorpion Centruroides margaritatus, is a potent inhibitor of the voltage-gated potassium channel (K _v 1.3) in human peripheral T lymphocytes. Peptide analogs corresponding to the amino acid segments that are located at the rat K _v 1.3 putative binding site for the ion channel blockers were synthesized...

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