Výsledky vyhledávání - "Nicholas W, Griggs"

Novel Dimethyltyrosine–Tetrahydroisoquinoline Peptidomimetics with Aromatic Tetrahydroisoquinoline Substitutions Show in Vitro Kappa and Mu Opioid Receptor Agonism

Autor: Traynor, Deanna Montgomery, Hartman Jg, Henry I. Mosberg, Sánchez-Santiago Aa, Nicholas W. Griggs, Jessica P. Anand, Thomas J Fernandez, Irina D. Pogozheva

Publikováno v: ACS Chemical Neuroscience. 10:3682-3689

The dimethyltyrosine–tetrahydroisoquinoline (Dmt-Tiq) scaffold was originally developed in the production of selective delta opioid receptor (DOR) antagonists. Installation of a 7-benzyl pendant on...

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::179acd152579ad14ee6a988ea61d1c51
https://doi.org/10.1021/acschemneuro.9b00250

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Dual Pharmacophores Explored via Structure–Activity Relationship (SAR) Matrix: Insights into Potent, Bifunctional Opioid Ligand Design

Autor: Aaron M. Bender, Thomas J Fernandez, John R. Traynor, Emily M. Jutkiewicz, Henry I. Mosberg, Nicholas W. Griggs, Jessica P. Anand, Anthony F. Nastase, Deanna Montgomery

Publikováno v: Journal of Medicinal Chemistry. 62:4193-4203

Short-acting μ-opioid receptor (MOR) agonists have long been used for the treatment of severe, breakthrough pain. However, selective MOR agonists including fentanyl and morphine derivatives are limited clinically due to high risks of dependence, tol

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bbfc327b5a0e52c3aca3e632834c3510
https://doi.org/10.1021/acs.jmedchem.9b00378

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In vivoeffects of μ-opioid receptor agonist/δ-opioid receptor antagonist peptidomimetics following acute and repeated administration

Autor: Emily M. Jutkiewicz, Nicholas W. Griggs, Henry I. Mosberg, Jessica P. Anand, Anthony F. Nastase, Deanna Montgomery, Kelsey E Kochan, John R. Traynor

Publikováno v: British Journal of Pharmacology. 175:2013-2027

BACKGROUND AND PURPOSE Agonists at μ-opioid receptors (μ-receptors) are used for pain management but produce adverse effects including tolerance, dependence and euphoria. The co-administration of a μ-receptor agonist with a δ-opioid receptor (δ-

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e5ca42222ac9170fc7afdba2255cc86f
https://doi.org/10.1111/bph.14148

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Synthesis and Pharmacological Evaluation of Novel C-8 Substituted Tetrahydroquinolines as Balanced-Affinity Mu/Delta Opioid Ligands for the Treatment of Pain

Autor: Anthony F. Nastase, Jessica P. Anand, Tyler J. Trask, Henry I. Mosberg, Emily M. Jutkiewicz, Thomas J Fernandez, Nicholas W. Griggs, John R. Traynor, Aubrie A. Harland

Publikováno v: ACS Chem Neurosci

The use of opioids for the treatment of pain, while largely effective, is limited by detrimental side effects including analgesic tolerance, physical dependence, and euphoria, which may lead to opioid abuse. Studies have shown that compounds with a �

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f2aa9cd90a3cb78894dd62220fff74cb
https://doi.org/10.1021/acschemneuro.8b00139

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Placement of Hydroxy Moiety on Pendant of Peptidomimetic Scaffold Modulates Mu and Kappa Opioid Receptor Efficacy

Autor: Henry I. Mosberg, Aubrie A. Harland, Irina D. Pogozheva, Nicholas W. Griggs, John R. Traynor, Tyler J. Trask

Publikováno v: ACS Chemical Neuroscience

In an effort to expand the structure–activity relationship (SAR) studies of a series of mixed-efficacy opioid ligands, peptidomimetics that incorporate methoxy and hydroxy groups around a benzyl or 2-methylindanyl pendant on a tetrahydroquinoline (

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b60a19333a22d3ae99d697cda0dce990
https://doi.org/10.1021/acschemneuro.7b00284

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Structural Simplification of a Tetrahydroquinoline Core Peptidomimetic μ-Opioid Receptor (MOR) Agonist/ δ-Opioid Receptor (DOR) Antagonist Produces Improved Metabolic Stability

Autor: Sean Henry, Nicholas W. Griggs, Thomas J Fernandez, Henry I. Mosberg, John R. Traynor, Jessica P. Anand

We have previously reported a series of μ-opioid receptor (MOR) agonist/δ-opioid receptor (DOR) antagonist ligands to serve as potential nonaddictive opioid analgesics. These ligands have been shown to be active in vivo, do not manifest withdrawal

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1c6689dc3e835c4534fbf08e14ad9bb3
https://europepmc.org/articles/PMC6713576/

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Asymmetric Synthesis and in Vitro and in Vivo Activity of Tetrahydroquinolines Featuring a Diverse Set of Polar Substitutions at the 6 Position as Mixed-Efficacy μ Opioid Receptor/δ Opioid Receptor Ligands

Autor: Jessica P. Anand, John R. Traynor, Nicholas W. Griggs, Aaron M. Bender, Emily M. Jutkiewicz, Henry I. Mosberg

Publikováno v: ACS Chemical Neuroscience. 6:1428-1435

We previously reported a small series of mixed-efficacy μ opioid receptor (MOR) agonist/δ opioid receptor (DOR) antagonist peptidomimetics featuring a tetrahydroquinoline scaffold and showed the promise of this series as effective analgesics after

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d62c7b3413a969382af12a944765015b
https://doi.org/10.1021/acschemneuro.5b00100

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In vivo effects of μ-opioid receptor agonist/δ-opioid receptor antagonist peptidomimetics following acute and repeated administration

Autor: Jessica P, Anand, Kelsey E, Kochan, Anthony F, Nastase, Deanna, Montgomery, Nicholas W, Griggs, John R, Traynor, Henry I, Mosberg, Emily M, Jutkiewicz

Publikováno v: British journal of pharmacology. 175(11)

BACKGROUND AND PURPOSE: Agonists at μ‐opioid receptors (μ‐receptors) are used for pain management but produce adverse effects including tolerance, dependence and euphoria. The co‐administration of a μ‐receptor agonist with a δ‐opioid re

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::28125a02c42cbdd344b119d69c09dd46
https://pubmed.ncbi.nlm.nih.gov/29352503

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Glucose and SIRT2 reciprocally mediate the regulation of keratin 8 by lysine acetylation

Autor: Liangyou Rui, Jessica M. Leonard, Natasha T. Snider, M. Bishr Omary, Raymond Kwan, Nicholas W. Griggs

Publikováno v: The Journal of Cell Biology

Keratin 8 lysine acetylation, which is enhanced by hyperglycemia and reduced by SIRT2, alters filament organization and reduces solubility.
Lysine acetylation is an important posttranslational modification that regulates microtubules and microfi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5c5dfe085a87367a147734cdc1b4dc79
https://doi.org/10.1083/jcb.201209028

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