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Optimized Opioid-Neurotensin Multitarget Peptides: From Design to Structure–Activity Relationship Studies

Journal of medicinal chemistry, 2020-11, Vol.63 (21), p.12929-12941

2020

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Novel Cocrystal Structures of Peptide Antagonists Bound to the Human Melanocortin Receptor 4 Unveil Unexplored Grounds for Structure-Based Drug Design

Journal of medicinal chemistry, 2024-02, Vol.67 (4), p.2690-2711

2024

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Hybrid opioid/non-opioid ligands in pain research

Current pharmaceutical design, 2013-12, Vol.19 (42), p.7435

2013

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Structural basis for bifunctional peptide recognition at human δ-opioid receptor

Nature structural & molecular biology, 2015-03, Vol.22 (3), p.265

2015

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Bifunctional Peptide-Based Opioid Agonist–Nociceptin Antagonist Ligands for Dual Treatment of Acute and Neuropathic Pain

Journal of medicinal chemistry, 2016-04, Vol.59 (8), p.3777-3792

2016

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Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure

Journal of medicinal chemistry, 2021-01, Vol.64 (1), p.357-369

2021

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Using conformational constraints at position 6 of Angiotensin II to generate compounds with enhanced AT2R selectivity and proteolytic stability

Bioorganic & medicinal chemistry letters, 2021-07, Vol.43, p.128086-128086, Article 128086

2021

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Analgesic Properties of Opioid/NK1 Multitarget Ligands with Distinct in Vitro Profiles in Naive and Chronic Constriction Injury Mice

ACS chemical neuroscience, 2017-10, Vol.8 (10), p.2315-2324

2017

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Development of potent and proteolytically stable human neuromedin U receptor agonists

European journal of medicinal chemistry, 2018-01, Vol.144, p.887-897

2018

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Trifluoromethylated Proline Surrogates as Part of “Pro–Pro” Turn‐Inducing Templates

Chembiochem : a European journal of chemical biology, 2019-10, Vol.20 (19), p.2513-2518

2019

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Hydrazone Linker as a Useful Tool for Preparing Chimeric Peptide/Nonpeptide Bifunctional Compounds

ACS medicinal chemistry letters, 2017-01, Vol.8 (1), p.73-77

2017

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Variation of the Net Charge, Lipophilicity, and Side Chain Flexibility in Dmt1‑DALDA: Effect on Opioid Activity and Biodistribution

Journal of medicinal chemistry, 2012-11, Vol.55 (22), p.9549-9561

2012

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Design of Novel Neurokinin 1 Receptor Antagonists Based on Conformationally Constrained Aromatic Amino Acids and Discovery of a Potent Chimeric Opioid Agonist-Neurokinin 1 Receptor Antagonist

Journal of medicinal chemistry, 2011-04, Vol.54 (7), p.2467-2476

2011

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Design, Synthesis, Pharmacological Evaluation, and Structure−Activity Study of Novel Endomorphin Analogues with Multiple Structural Modifications

Journal of medicinal chemistry, 2011-03, Vol.54 (5), p.1462-1472

2011

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Synthesis and biological evaluation of compact, conformationally constrained bifunctional opioid agonist – Neurokinin-1 antagonist peptidomimetics

European journal of medicinal chemistry, 2015-03, Vol.92, p.64-77

2015

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Indoloazepinone‐Constrained Oligomers as Cell‐Penetrating and Blood–Brain‐Barrier‐Permeating Compounds

Chembiochem : a European journal of chemical biology, 2018-04, Vol.19 (7), p.696-705

2018

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Side Chain Cyclized Aromatic Amino Acids: Great Tools as Local Constraints in Peptide and Peptidomimetic Design

Journal of medicinal chemistry, 2016-12, Vol.59 (24), p.10865-10890

2016

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Novel Neurotensin Analogues for Radioisotope Targeting to Neurotensin Receptor-Positive Tumors

Bioconjugate chemistry, 2009-08, Vol.20 (8), p.1602-1610

2009

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Superpotent [Dmt1]Dermorphin Tetrapeptides Containing the 4‑Aminotetrahydro-2-benzazepin-3-one Scaffold with Mixed μ/δ Opioid Receptor Agonistic Properties

Journal of medicinal chemistry, 2011-11, Vol.54 (22), p.7848-7859

2011

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Bis(thiosemicarbazones) as bifunctional chelators for the room temperature 64-copper labeling of peptides

Dalton transactions : an international journal of inorganic chemistry, 2010-01, Vol.39 (15), p.3620-3632

2010

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Influence of the Molecular Charge on the Biodistribution of Bombesin Analogues Labeled with the [99mTc(CO)3]-Core

Bioconjugate chemistry, 2008-12, Vol.19 (12), p.2409-2416

2008

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χ‑Space Screening of Dermorphin-Based Tetrapeptides through Use of Constrained Arylazepinone and Quinolinone Scaffolds

ACS medicinal chemistry letters, 2017-11, Vol.8 (11), p.1177-1182

2017

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Dual Alleviation of Acute and Neuropathic Pain by Fused Opioid Agonist-Neurokinin 1 Antagonist Peptidomimetics

ACS medicinal chemistry letters, 2015-12, Vol.6 (12), p.1209-1214

2015

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Opening the amino acid toolbox for peptide‐based NTS2‐selective ligands as promising lead compounds for pain management

Journal of peptide science, 2023-06, Vol.29 (6), p.e3471-n/a

2023

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Neuromedin U and Structural Analogs: An Overview of their Structure, Function and Selectivity

Current medicinal chemistry, 2020-01, Vol.27 (39), p.6744

2020

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Optimized Opioid-Neurotensin Multitarget Peptides: From Design to Structure–Activity Relationship Studies

Novel Cocrystal Structures of Peptide Antagonists Bound to the Human Melanocortin Receptor 4 Unveil Unexplored Grounds for Structure-Based Drug Design

Hybrid opioid/non-opioid ligands in pain research

Structural basis for bifunctional peptide recognition at human δ-opioid receptor

Bifunctional Peptide-Based Opioid Agonist–Nociceptin Antagonist Ligands for Dual Treatment of Acute and Neuropathic Pain

Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure

Using conformational constraints at position 6 of Angiotensin II to generate compounds with enhanced AT2R selectivity and proteolytic stability

Analgesic Properties of Opioid/NK1 Multitarget Ligands with Distinct in Vitro Profiles in Naive and Chronic Constriction Injury Mice

Development of potent and proteolytically stable human neuromedin U receptor agonists

Trifluoromethylated Proline Surrogates as Part of “Pro–Pro” Turn‐Inducing Templates

Hydrazone Linker as a Useful Tool for Preparing Chimeric Peptide/Nonpeptide Bifunctional Compounds

Variation of the Net Charge, Lipophilicity, and Side Chain Flexibility in Dmt1‑DALDA: Effect on Opioid Activity and Biodistribution

Design of Novel Neurokinin 1 Receptor Antagonists Based on Conformationally Constrained Aromatic Amino Acids and Discovery of a Potent Chimeric Opioid Agonist-Neurokinin 1 Receptor Antagonist

Design, Synthesis, Pharmacological Evaluation, and Structure−Activity Study of Novel Endomorphin Analogues with Multiple Structural Modifications

Synthesis and biological evaluation of compact, conformationally constrained bifunctional opioid agonist – Neurokinin-1 antagonist peptidomimetics

Indoloazepinone‐Constrained Oligomers as Cell‐Penetrating and Blood–Brain‐Barrier‐Permeating Compounds

Side Chain Cyclized Aromatic Amino Acids: Great Tools as Local Constraints in Peptide and Peptidomimetic Design

Novel Neurotensin Analogues for Radioisotope Targeting to Neurotensin Receptor-Positive Tumors

Superpotent [Dmt1]Dermorphin Tetrapeptides Containing the 4‑Aminotetrahydro-2-benzazepin-3-one Scaffold with Mixed μ/δ Opioid Receptor Agonistic Properties

Bis(thiosemicarbazones) as bifunctional chelators for the room temperature 64-copper labeling of peptides

Influence of the Molecular Charge on the Biodistribution of Bombesin Analogues Labeled with the [99mTc(CO)3]-Core

χ‑Space Screening of Dermorphin-Based Tetrapeptides through Use of Constrained Arylazepinone and Quinolinone Scaffolds

Dual Alleviation of Acute and Neuropathic Pain by Fused Opioid Agonist-Neurokinin 1 Antagonist Peptidomimetics

Opening the amino acid toolbox for peptide‐based NTS2‐selective ligands as promising lead compounds for pain management

Neuromedin U and Structural Analogs: An Overview of their Structure, Function and Selectivity

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