Search Results - "Debevec, Ginamarie"

Identification of a Novel Polyamine Scaffold With Potent Efflux Pump Inhibition Activity Toward Multi-Drug Resistant Bacterial Pathogens by Fleeman, Renee M, Debevec, Ginamarie, Antonen, Kirsten, Adams, Jessie L, Santos, Radleigh G, Welmaker, Gregory S, Houghten, Richard A, Giulianotti, Marc A, Shaw, Lindsey N

“…We have previously reported the use of combinatorial chemistry to identify broad-spectrum antibacterial agents. Herein, we extend our analysis of this…”
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Identification of Bis-Cyclic Guanidines as Antiplasmodial Compounds from Positional Scanning Mixture-Based Libraries by Perry, Jr, David L, Roberts, Bracken F, Debevec, Ginamarie, Michaels, Heather A, Chakrabarti, Debopam, Nefzi, Adel

“…The screening of more than 30 million compounds derived from 81 small molecule libraries built on 81 distinct scaffolds identified pyrrolidine bis-cyclic…”
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Identification of small molecules by screening a mixture-based scaffold compound library for treatment of alpha-1 antitrypsin deficiency by Zhang, Xiaojuan, Santos, Radleigh, Debevec, Ginamarie, Li, Danmeng, Schutte, Ryan, Pham, Kien, Liu, Chen, Ostrov, David A., Giulianotti, Marc

“…This study aimed to identify small molecules that have the potential to treat alpha1-antitrypsin deficiency (AATD) by screening compounds available from a…”
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Correction to “Discovery of Nanomolar Melanocortin‑3 Receptor (MC3R)-Selective Small Molecule Pyrrolidine Bis-Cyclic Guanidine Agonist Compounds Via a High Throughput ‘Unbiased’ Screening Campaign” by Doering, Skye R., Freeman, Katie, Debevec, Ginamarie, Geer, Phaedra, Santos, Radleigh G., Lavoi, Travis M., Giulianotti, Marc A., Pinilla, Clemencia, Appel, Jon R., Houghten, Richard A., Ericson, Mark D., Haskell-Luevano, Carrie

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Discovery of Nanomolar Melanocortin‑3 Receptor (MC3R)-Selective Small Molecule Pyrrolidine Bis-Cyclic Guanidine Agonist Compounds Via a High-Throughput “Unbiased” Screening Campaign by Doering, Skye R, Freeman, Katie, Debevec, Ginamarie, Geer, Phaedra, Santos, Radleigh G, Lavoi, Travis M, Giulianotti, Marc A, Pinilla, Clemencia, Appel, Jon R, Houghten, Richard A, Ericson, Mark D, Haskell-Luevano, Carrie

“…The central melanocortin-3 and melanocortin-4 receptors (MC3R, MC4R) are key regulators of body weight and energy homeostasis. Herein, the discovery and…”
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Discovery of Polypharmacological Melanocortin-3 and −4 Receptor Probes and Identification of a 100-Fold Selective nM MC3R Agonist versus a µM MC4R Partial Agonist by Fleming, Katlyn A., Freeman, Katie T., Powers, Mike D., Santos, Radleigh G., Debevec, Ginamarie, Giulianotti, Marc A., Houghten, Richard A., Doering, Skye R., Pinilla, Clemencia, Haskell-Luevano, Carrie

“…The centrally expressed melanocortin-3 and melanocortin-4 receptors (MC3R, MC4R) are established targets to treat diseases of positive and negative energy…”
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A Novel Class of Common Docking Domain Inhibitors That Prevent ERK2 Activation and Substrate Phosphorylation by Sammons, Rachel M, Perry, Nicole A, Li, Yangmei, Cho, Eun Jeong, Piserchio, Andrea, Zamora-Olivares, Diana P, Ghose, Ranajeet, Kaoud, Tamer S, Debevec, Ginamarie, Bartholomeusz, Chandra, Gurevich, Vsevolod V, Iverson, Tina M, Giulianotti, Marc, Houghten, Richard A, Dalby, Kevin N

“…Extracellular signal-regulated kinases (ERK1/2) are mitogen-activated protein kinases (MAPKs) that play a pro-tumorigenic role in numerous cancers. ERK1/2…”
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Highly Selective and Potent α4β2 nAChR Antagonist Inhibits Nicotine Self-Administration and Reinstatement in Rats by Wu, Jinhua, Cippitelli, Andrea, Zhang, Yaohong, Debevec, Ginamarie, Schoch, Jennifer, Ozawa, Akihiko, Yu, Yongping, Liu, Huan, Chen, Wenteng, Houghten, Richard A, Welmaker, Gregory S, Giulianotti, Marc A, Toll, Lawrence

“…The α4β2 nAChR is the most predominant subtype in the brain and is a well-known culprit for nicotine addiction. Previously we presented a series of α4β2 nAChR…”
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A key role for the N/OFQ-NOP receptor system in modulating nicotine taking in a model of nicotine and alcohol co-administration by Cippitelli, Andrea, Schoch, Jennifer, Debevec, Ginamarie, Brunori, Gloria, Zaveri, Nurulain T., Toll, Lawrence

“…Alcohol and nicotine are often co-abused. Although the N/OFQ-NOP receptor system is considered a potential target for development of drug abuse…”
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Discovery of Polypharmacological Melanocortin‑3 and -4 Receptor Probes and Identification of a 100-Fold Selective nM MC3R Agonist versus a μM MC4R Partial Agonist by Fleming, Katlyn A, Freeman, Katie T, Powers, Mike D, Santos, Radleigh G, Debevec, Ginamarie, Giulianotti, Marc A, Houghten, Richard A, Doering, Skye R, Pinilla, Clemencia, Haskell-Luevano, Carrie

“…The centrally expressed melanocortin-3 and melanocortin-4 receptors (MC3R and MC4R, respectively) are established targets to treat diseases of positive- and…”
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Identification of a small molecule inhibitor of the aminoglycoside 6'-N-acetyltransferase type Ib [AAC(6')-Ib] using mixture-based combinatorial libraries by Tran, Tung, Chiem, Kevin, Jani, Saumya, Arivett, Brock A., Lin, David L., Lad, Rupali, Jimenez, Verónica, Farone, Mary B., Debevec, Ginamarie, Santos, Radleigh, Giulianotti, Marc, Pinilla, Clemencia, Tolmasky, Marcelo E.

“…•Inhibitors of resistance enzymes can extend the life of existing aminoglycosides.•Identification of novel inhibitors using mixture–based combinatorial…”
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Involvement of α4β2 and α3β4 nicotinic receptor subtypes in alcohol taking and seeking by Cippitelli, Andrea, Wu, Jinhua, Debevec, Ginamarie, Armishaw, Christopher, Welmaker, Greg S, Giulianotti, Marc, Toll, Lawrence

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Identification of a Small Molecule Inhibitor of the Aminoglycoside 6’-NAcetyltransferase Type Ib [AAC(6’)-Ib] Using Mixture-Based Combinatorial Libraries by Tran, Tung, Chiem, Kevin, Jani, Saumya, Arivett, Brock A., Lin, David L., Lad, Rupali, Jimenez, Verónica, Farone, Mary B., Debevec, Ginamarie, Santos, Radleigh, Giulianotti, Marc, Pinilla, Clemencia, Tolmasky, Marcelo E.

“…The aminoglycoside 6′- N -acetyltransferase type Ib [AAC(6’)-Ib] is the most widely distributed enzyme among AAC(6’)-I-producing Gram-negative pathogens and…”
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Identification of Tetrapeptides from a Mixture Based Positional Scanning Library That Can Restore nM Full Agonist Function of the L106P, I69T, I102S, A219V, C271Y, and C271R Human Melanocortin‑4 Polymorphic Receptors (hMC4Rs) by Haslach, Erica M, Huang, Huisuo, Dirain, Marvin, Debevec, Ginamarie, Geer, Phaedra, Santos, Radleigh G, Giulianotti, Marc A, Pinilla, Clemencia, Appel, Jon R, Doering, Skye R, Walters, Michael A, Houghten, Richard A, Haskell-Luevano, Carrie

“…Human obesity has been linked to genetic factors and single nucleotide polymorphisms (SNPs). Melanocortin-4 receptor (MC4R) SNPs have been associated with up…”
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Discovery of Mixed Pharmacology Melanocortin-3 Agonists and Melanocortin-4 Receptor Tetrapeptide Antagonist Compounds (TACOs) Based on the Sequence Ac-Xaa 1 -Arg-(pI)DPhe-Xaa 4 -NH 2 by Doering, Skye R, Freeman, Katie T, Schnell, Sathya M, Haslach, Erica M, Dirain, Marvin, Debevec, Ginamarie, Geer, Phaedra, Santos, Radleigh G, Giulianotti, Marc A, Pinilla, Clemencia, Appel, Jon R, Speth, Robert C, Houghten, Richard A, Haskell-Luevano, Carrie

“…The centrally expressed melanocortin-3 and -4 receptors (MC3R/MC4R) have been studied as possible targets for weight management therapies, with a preponderance…”
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Discovery of Mixed Pharmacology Melanocortin‑3 Agonists and Melanocortin‑4 Receptor Tetrapeptide Antagonist Compounds (TACOs) Based on the Sequence Ac-Xaa1‑Arg-(pI)DPhe-Xaa4‑NH2 by Doering, Skye R, Freeman, Katie T, Schnell, Sathya M, Haslach, Erica M, Dirain, Marvin, Debevec, Ginamarie, Geer, Phaedra, Santos, Radleigh G, Giulianotti, Marc A, Pinilla, Clemencia, Appel, Jon R, Speth, Robert C, Houghten, Richard A, Haskell-Luevano, Carrie

“…The centrally expressed melanocortin-3 and -4 receptors (MC3R/MC4R) have been studied as possible targets for weight management therapies, with a preponderance…”
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Scaffold Ranking and Positional Scanning Identify Novel Neurite Outgrowth Promoters with Nanomolar Potency by Al-Ali, Hassan, Debevec, Ginamarie, Santos, Radleigh G, Houghten, Richard A, Davis, Jennifer C, Nefzi, Adel, Lemmon, Vance P, Bixby, John L, Giulianotti, Marc A

“…Central nervous system (CNS) neurons typically fail to regrow their axons after injury. Injuries or neuropathies that damage CNS axons and disrupt neuronal…”
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Synthesis and biological evaluations of novel endomorphin analogues containing α-hydroxy-β-phenylalanine (AHPBA) displaying mixed μ/δ opioid receptor agonist and δ opioid receptor antagonist activities by Hu, Miao, Giulianotti, Marc A., McLaughlin, Jay P., Shao, Jiaan, Debevec, Ginamarie, Maida, Laura E., Geer, Phaedra, Cazares, Margaret, Misler, Jaime, Li, Ling, Dooley, Colette, Ganno, Michelle L., Eans, Shainnel O., Mizrachi, Elisa, Santos, Radleigh G., Yongye, Austin B., Houghten, Richard A., Yu, Yongping

“…A novel series of endomorphin-1 (EM-1) and endomorphin-2 (EM-2) analogues was synthesized, incorporating chiral α-hydroxy-β-phenylalanine (AHPBA), and/or…”
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Libraries from libraries: a series of sulfonamide linked heterocycles derived from the same scaffold by Debevec, Ginamarie, Chen, Wenteng, Yu, Yongping, Houghten, Richard A., Giulianotti, Marc A.

“…A libraries from libraries approach is described for the synthesis of five different sulfonamide linked scaffolds. Four of the scaffolds are sulfonamides…”
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Fluorescent Mu Selective Opioid Ligands from a Mixture Based Cyclic Peptide Library by Li, Yangmei, Dooley, Colette T, Misler, Jaime A, Debevec, Ginamarie, Giulianotti, Marc A, Cazares, Margaret E, Maida, Laura, Houghten, Richard A

“…A positional scanning cyclic peptide library was generated using a penta-peptide thioester scaffold. Glycine was fixed at position R1. Diaminopropionic acid…”
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