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Biochemical and pharmacological characterization of three opioid-nociceptin hybrid peptide ligands reveals substantially differing modes of their actions
2018
Peptides
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These chimeric molecules consist of YGGF sequence, a crucial motif in the N-terminus of natural opioid peptides, and Ac-RYYRIK-NH2, which was isolated from a combinatorial peptide library as an antagonist ...
The designed chimeric peptide ligands presented in this study accommodate well into a group of multitarget opioid compounds that include opioid-non-opioid peptide dimer analogues, dual non-peptide dimers ...
Hybrid or bifunctional peptide or non-peptide ligands developed recently, bearing two pharmacophores, represent novel biochemical tools in investigating GPCRs and their interacting complexes. ...
doi:10.1016/j.peptides.2017.10.005
pmid:29038035
fatcat:xhoqxuvmxbeelohf3iktjgi33u
A combined ligand-based and target-based drug design approach for G-protein coupled receptors: application to salvinorin A, a selective kappa opioid receptor agonist
2006
Journal of Computer-Aided Molecular Design
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Utilizing a set of recently reported derivatives of salvinorin A, a structurally unique KOP receptor agonist, a pharmacophore model was developed that consisted of two hydrogen bond acceptor and three ...
Therefore, we set out to develop a powerful virtual screening model to identify novel molecular scaffolds as potential leads for the human KOP (hKOP) receptor employing a combined approach. ...
Acknowledgements Support for this work was provided by NIDA grant DA017360. ...
doi:10.1007/s10822-006-9067-x
pmid:17009091
fatcat:aoeqek44cber3pp2uvcoo5evba
Computational Studies for Structure-Based Drug Designing Against Transmembrane Receptors: pLGICs and Class A GPCRs
2018
Frontiers in Physics
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The plasma membrane, a phospholipid bilayer consisting of two asymmetric leaflets, defines its existence by separating the interior from the exterior. ...
Present review considers the members of two important protein superfamilies that provided the major pharmaceutical drug-targets, viz., Cys-loop pentameric ligand gated ion channels (pLGICs) and class A ...
All authors listed have made a substantial, direct and intellectual contribution to the work, and approved it for publication.
ACKNOWLEDGMENTS ...
doi:10.3389/fphy.2018.00052
fatcat:fuu4aqb6avbcpp6n26yb5qkaxm
Predicted Ligands for the Human Urotensin-II G Protein-Coupled Receptor with Some Experimental Validation
2014
ChemMedChem
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Acknowledgements Funding for this project was provided by the Korea Research Institute of Chemical Technology (South Korea). ...
Keywords: computational chemistry · docking · GPCRs · Rgroup screening · urotensin II · virtual screening ...
Our efforts identified a new scaffold as a potential new lead structure for the development of novel hUT 2 R antagonists, and the computational methods used could find more general applicability to other ...
doi:10.1002/cmdc.201402087
pmid:24989481
fatcat:mhuwqjuctbhujmfsg2kxls5m3i
Discovery of new GPCR ligands to illuminate new biology
2017
Nature Chemical Biology
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Although a plurality of drugs target G-protein-coupled receptors (GPCRs), most have emerged from classical medicinal chemistry and pharmacology programs and resemble one another structurally and functionally ...
Structural determination of almost 40 GPCRs in the last decade has revealed them to be well suited for small-molecule recognition -a post hoc explanation for their preponderance among drug targets. ...
Acknowledgments Support was given by NIH grants U01104974, and R35GM122481, and the NIMH-PDSP. We thank T. Kenakin for discussions of allostery, J. Pottel and A. ...
doi:10.1038/nchembio.2490
pmid:29045379
pmcid:PMC5835362
fatcat:fmig24qavzfhfkn3a5ywetrctm
Customizing G Protein-Coupled Receptor Models for Structure-Based Virtual Screening
2009
Current pharmaceutical design
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This review will focus on the construction, refinement, and validation of G Protein-coupled receptor models for the purpose of structure-based virtual screening. ...
Finally, an overview of several successful structure-based screening shows that receptor models, despite structural inaccuracies, can be efficiently used to find novel ligands. ...
First a pharmacophore was derived from a set of known DRD3 ligands (antagonists and partial agonists (Fig. (8) ) and used as a query for retrieving a first hit list of 6 727 compounds from an initial ...
doi:10.2174/138161209789824786
pmid:20028320
fatcat:e2j3rcvtenbpne3xbnspjl526a
The Spicy Story of Cannabimimetic Indoles
2021
Molecules
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and a high potential for abuse. ...
The sale of these alleged "herbal products" evades FDA consumer protections for proper labeling and safety as a medicine, as well as DEA scheduling as compounds having no currently accepted medical use ...
Acknowledgments: The authors would like to thank Andrew England for preparing the images of the compounds. ...
doi:10.3390/molecules26206190
pmid:34684770
pmcid:PMC8538531
fatcat:wxzymnmiuvf73awtnivejagsgm
GPCR structure, function, drug discovery and crystallography: report from Academia-Industry International Conference (UK Royal Society) Chicheley Hall, 1–2 September 2014
2015
Naunyn-Schmiedeberg's Archives of Pharmacology
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The UniProt database has records for about 800 proteins classified as GPCRs, but drugs have only been developed against 50 of these. ...
Therefore, an international conference, sponsored by the Royal Society, with world-renowned researchers from industry and academia was recently held to discuss recent progress and highlight key areas of ...
Open Access This article is distributed under the terms of the Creative Commons Attribution License which permits any use, distribution, and reproduction in any medium, provided the original author(s) ...
doi:10.1007/s00210-015-1111-8
pmid:25772061
pmcid:PMC4495723
fatcat:bpqwfda4p5hili35sspnltqjxy
13th EBSA congress, July 24–28, 2021, Vienna, Austria
2021
European Biophysics Journal
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Welcome from the President of EBSA The world is dealing with one of its greatest challenges, and thanks to the amazing contribution of science and the development, in record time, of vaccines against SARS-CoV ...
Elena Pohl, from University of Veterinary Medicine Vienna, and her team, for taking the lead to assemble an attractive scientific programme, in the tradition of the spectacular past European Congresses ...
of prenatal exposure to delta-opioid receptor (DOR) agonist SNC80 on hippocampal excitability of offsprings. ...
doi:10.1007/s00249-021-01558-w
pmid:34245338
pmcid:PMC8272448
fatcat:z2svytd4kbamrmvarle4lxwtxm
Abstracts of the Tenth Annual Meeting of the Israel Society for Neurosciences
2001
Neural Plasticity
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Gan; 3Ben-Gurion University of the Negev, Beer Sheva We investigated the co.upling between response selection and execution in a Stroop tas.k witti handwritten resp.onses. ...
According to the model, the conflicting intirmatign arriving from the intended processing of color and the (unintended) automatic reading finds, its expression.either in an incorrect response or in an ...
The finding that cognitive development is affected by the apoE genotype provides a novel link between the developmental and neurodegenerative functions of apoE and suggests that the latter may be mediated ...
doi:10.1155/np.2001.157
pmid:11783444
pmcid:PMC2565376
fatcat:ybrait32srfhbaddpozdxlwvcu
Other Radiopharmaceuticals for Imaging GEP-NET
[chapter]
2015
Somatostatin Analogues
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completeness of the contents of this book and specifically disclaim any implied warranties of merchantability or fitness for a particular purpose. ...
Limit of Liability/Disclaimer of Warranty: While the publisher and author have used their best efforts in preparing this book, they make no representations or warranties with respect to the accuracy or ...
Acknowledgments We would like to thank E. de Blois for supplying the figures with radiochemical structures of the various chelators and peptide-chelator complexes. reFerences ...
doi:10.1002/9781119031659.ch7
fatcat:jyxrrzso3jhttmgryudojq7mry
Somatostatin Receptor Scintigraphy in Medullary Thyroid Cancer
[chapter]
2015
Somatostatin Analogues
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completeness of the contents of this book and specifically disclaim any implied warranties of merchantability or fitness for a particular purpose. ...
Limit of Liability/Disclaimer of Warranty: While the publisher and author have used their best efforts in preparing this book, they make no representations or warranties with respect to the accuracy or ...
Acknowledgments We would like to thank E. de Blois for supplying the figures with radiochemical structures of the various chelators and peptide-chelator complexes. reFerences ...
doi:10.1002/9781119031659.ch11
fatcat:5apxxosx3vhrrjq7wzxylxn56u
Abstracts of the 13th Annual Meeting of Israel Society for Neuroscience
2005
Neural Plasticity
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These dma demonstrate a L.B_M. ph.eno.type resulting from the absence of central IL-1RI sig.almg. ...
For IM_s, the distance th.at the bend .point moved and the time or movement tor the regenerative arm was half of those of the normal arms. ...
We checked proinflammatory cytokines profile at 2 and 4h after CHI using RT-PCR. b-actin served as ...
doi:10.1155/np.2005.1
pmid:15940829
pmcid:PMC2565472
fatcat:6yiorqangzffpo5b3mdytg5xhy
Gli1/DNA interaction is a druggable target for Hedgehog-dependent tumors
2016
European Journal of Cancer
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Hedgehog signaling is essential for tissue development and stemness, and its deregulation has been observed in many tumors. ...
For this reason, understanding the poorly elucidated mechanism of Gli1-mediated transcription allows to identify novel molecules blocking the pathway at a downstream level, representing a critical goal ...
Scott for the gift of Ptch1 À/À MEF cells, R. Toftgard for SuFu À/À
MEF and Smo ...
doi:10.1016/s0959-8049(16)61456-9
fatcat:7kqfzx4jfvfkxkylcumexgbnpu
Gli1/DNA interaction is a druggable target for Hedgehog-dependent tumors
2014
EMBO Journal
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Hedgehog signaling is essential for tissue development and stemness, and its deregulation has been observed in many tumors. ...
For this reason, understanding the poorly elucidated mechanism of Gli1-mediated transcription allows to identify novel molecules blocking the pathway at a downstream level, representing a critical goal ...
Scott for the gift of Ptch1 À/À MEF cells, R. Toftgard for SuFu À/À
MEF and Smo ...
doi:10.15252/embj.201489213
pmid:25476449
pmcid:PMC4298015
fatcat:yby64djkkffjxhvroaccrifcea
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