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Customizing G Protein-Coupled Receptor Models for Structure-Based Virtual Screening

Chris de Graaf, Didier Rognan
<span title="2009-12-01">2009</span> <i title="Bentham Science Publishers Ltd."> <a target="_blank" rel="noopener" href="https://fatcat.wiki/container/xtiwjcbzsbd35jtqmz56mrpmb4" style="color: black;">Current pharmaceutical design</a> </i> &nbsp;
This review will focus on the construction, refinement, and validation of G Protein-coupled receptor models for the purpose of structure-based virtual screening.  ...  Practical tips and tricks derived from concrete modeling and virtual screening exercises to overcome the problems and pitfalls associated with the different steps of the receptor modeling workflow will  ...  For a set of GPCR targets, the dopamine D2 receptor (DRD2), adenosine A3 receptor (AA3R), and the thromboxane A2 receptor (TA2R), we have evaluated the implication of including ecl2 atomic coordinates  ... 
<span class="external-identifiers"> <a target="_blank" rel="external noopener noreferrer" href="https://doi.org/10.2174/138161209789824786">doi:10.2174/138161209789824786</a> <a target="_blank" rel="external noopener" href="https://www.ncbi.nlm.nih.gov/pubmed/20028320">pmid:20028320</a> <a target="_blank" rel="external noopener" href="https://fatcat.wiki/release/e2j3rcvtenbpne3xbnspjl526a">fatcat:e2j3rcvtenbpne3xbnspjl526a</a> </span>
<a target="_blank" rel="noopener" href="https://web.archive.org/web/20170810173948/http://cheminfo.u-strasbg.fr/labwebsite/publications/paper113.pdf" title="fulltext PDF download" data-goatcounter-click="serp-fulltext" data-goatcounter-title="serp-fulltext"> <button class="ui simple right pointing dropdown compact black labeled icon button serp-button"> <i class="icon ia-icon"></i> Web Archive [PDF] <div class="menu fulltext-thumbnail"> <img src="https://blobs.fatcat.wiki/thumbnail/pdf/d8/a4/d8a44548286dab31232d179ed72f66aed8e0f985.180px.jpg" alt="fulltext thumbnail" loading="lazy"> </div> </button> </a> <a target="_blank" rel="external noopener noreferrer" href="https://doi.org/10.2174/138161209789824786"> <button class="ui left aligned compact blue labeled icon button serp-button"> <i class="external alternate icon"></i> Publisher / doi.org </button> </a>

GPCR Conformations: Implications for Rational Drug Design

Abby L. Parrill, Debra L. Bautista
<span title="2010-12-23">2010</span> <i title="MDPI AG"> <a target="_blank" rel="noopener" href="https://fatcat.wiki/container/lecpmp3vs5hulh3xiqgqnyhrge" style="color: black;">Pharmaceuticals</a> </i> &nbsp;
Key features of GPCR conformations derived from both types of characterization techniques are reviewed.  ...  These critical roles offer targets for therapeutic intervention, as exemplified by the substantial fraction of current pharmaceutical agents that target members of this family.  ...  Acknowledgements Funding for work by the authors related to GPCR structure and ligand discovery from the National Institutes of Health (HL 084007) is gratefully acknowledged.  ... 
<span class="external-identifiers"> <a target="_blank" rel="external noopener noreferrer" href="https://doi.org/10.3390/ph4010007">doi:10.3390/ph4010007</a> <a target="_blank" rel="external noopener" href="https://fatcat.wiki/release/ul2w6e4nzzgdlcxlxwdecwqp6q">fatcat:ul2w6e4nzzgdlcxlxwdecwqp6q</a> </span>
<a target="_blank" rel="noopener" href="https://archive.org/download/pubmed-PMC4052540/PMC4052540-ph4010007.pdf" title="fulltext PDF download" data-goatcounter-click="serp-fulltext" data-goatcounter-title="serp-fulltext"> <button class="ui simple right pointing dropdown compact black labeled icon button serp-button"> <i class="icon ia-icon"></i> File Archive [PDF] <div class="menu fulltext-thumbnail"> <img src="https://blobs.fatcat.wiki/thumbnail/pdf/ee/d2/eed2eedbf810612fe49f00892723961c6bea4df9.180px.jpg" alt="fulltext thumbnail" loading="lazy"> </div> </button> </a> <a target="_blank" rel="external noopener noreferrer" href="https://doi.org/10.3390/ph4010007"> <button class="ui left aligned compact blue labeled icon button serp-button"> <i class="unlock alternate icon" style="background-color: #fb971f;"></i> mdpi.com </button> </a>

The 18th European Symposium on Quantitative Structure–Activity Relationships

Anna Tsantili-Kakoulidou, Dimitris K Agrafiotis
<span title="2011-02-23">2011</span> <i title="Informa Healthcare"> <a target="_blank" rel="noopener" href="https://fatcat.wiki/container/4m2squtugrdvtgjdvfbz5jhmaq" style="color: black;">Expert Opinion on Drug Discovery</a> </i> &nbsp;
Furthermore, the conducted docking studies elucidated the possible alternative binding mode of the ligands into the ATP binding cleft and assigned their physicochemical and structural features which promote  ...  Dr Kontogiorgis Christos is thankful to the Foundation for Education and European Culture, established in Athens for the financial support of this postdoctoral research.  ...  POSTER PRESENTATION IΙ-74 A NEW SERIES OF 2-ARYL-PYRAZOLO-TRIAZOLO-PYRIMIDINES AS POTENT HUMAN A3 ADENOSINE RECEPTOR ANTAGONISTS: QSAR ANALYSIS AND COMFA-GUIDED MODELING OF ANTAGONIST BINDING SITE THROUGH  ... 
<span class="external-identifiers"> <a target="_blank" rel="external noopener noreferrer" href="https://doi.org/10.1517/17460441.2011.560604">doi:10.1517/17460441.2011.560604</a> <a target="_blank" rel="external noopener" href="https://www.ncbi.nlm.nih.gov/pubmed/22646021">pmid:22646021</a> <a target="_blank" rel="external noopener" href="https://fatcat.wiki/release/tb4bhvtnpzahxm4xba7iw4afuy">fatcat:tb4bhvtnpzahxm4xba7iw4afuy</a> </span>
<a target="_blank" rel="noopener" href="https://web.archive.org/web/20190305135714/http://pdfs.semanticscholar.org/ca7c/c586e46f9dc73e2604c8471e4a52df04f51f.pdf" title="fulltext PDF download" data-goatcounter-click="serp-fulltext" data-goatcounter-title="serp-fulltext"> <button class="ui simple right pointing dropdown compact black labeled icon button serp-button"> <i class="icon ia-icon"></i> Web Archive [PDF] <div class="menu fulltext-thumbnail"> <img src="https://blobs.fatcat.wiki/thumbnail/pdf/ca/7c/ca7cc586e46f9dc73e2604c8471e4a52df04f51f.180px.jpg" alt="fulltext thumbnail" loading="lazy"> </div> </button> </a> <a target="_blank" rel="external noopener noreferrer" href="https://doi.org/10.1517/17460441.2011.560604"> <button class="ui left aligned compact blue labeled icon button serp-button"> <i class="external alternate icon"></i> Publisher / doi.org </button> </a>

Recent Advances and Applications of Molecular Docking to G Protein-Coupled Receptors

Damian Bartuzi, Agnieszka Kaczor, Katarzyna Targowska-Duda, Dariusz Matosiuk
<span title="2017-02-22">2017</span> <i title="MDPI AG"> <a target="_blank" rel="noopener" href="https://fatcat.wiki/container/dstyyzbt45gknhqqjsh45p55h4" style="color: black;">Molecules</a> </i> &nbsp;
The growing number of studies on G protein-coupled receptors (GPCRs) family are a source of noticeable improvement in our understanding of the functioning of these proteins.  ...  GPCRs are responsible for a vast part of signaling in vertebrates and, as such, invariably remain in the spotlight of medicinal chemistry.  ...  Conflicts of Interest: The authors declare no conflict of interest.  ... 
<span class="external-identifiers"> <a target="_blank" rel="external noopener noreferrer" href="https://doi.org/10.3390/molecules22020340">doi:10.3390/molecules22020340</a> <a target="_blank" rel="external noopener" href="https://www.ncbi.nlm.nih.gov/pubmed/28241450">pmid:28241450</a> <a target="_blank" rel="external noopener" href="https://fatcat.wiki/release/xyytfxpfcvd43dyoefto4qr5pi">fatcat:xyytfxpfcvd43dyoefto4qr5pi</a> </span>
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Invited Lectures

<span title="">2006</span> <i title="Springer Nature"> <a target="_blank" rel="noopener" href="https://fatcat.wiki/container/jkgqljwebvb2lgsaoj4y6ud6gu" style="color: black;">Purinergic Signalling Purinergic Signalling</a> </i> &nbsp;
The radioligand allowed to set up a fast and efficient screening assay for identifying novel lead structures for the development of P2Y 12 antagonists, which are potent antithrombotic agents.  ...  These findings provide a strong rationale for the exploitation of adenosine receptor antagonist therapies in future treatment of fibrotic diseases.  ...  Understanding the key roles of these ATP receptors may lead to new strategies for the management of intractable chronic pain.  ... 
<span class="external-identifiers"> <a target="_blank" rel="external noopener noreferrer" href="https://doi.org/10.1007/s11302-006-9006-2">doi:10.1007/s11302-006-9006-2</a> <a target="_blank" rel="external noopener" href="https://www.ncbi.nlm.nih.gov/pubmed/18404494">pmid:18404494</a> <a target="_blank" rel="external noopener" href="https://pubmed.ncbi.nlm.nih.gov/PMC2096525/">pmcid:PMC2096525</a> <a target="_blank" rel="external noopener" href="https://fatcat.wiki/release/ul2ea34gmndrfiaaqjq2rdkdhi">fatcat:ul2ea34gmndrfiaaqjq2rdkdhi</a> </span>
<a target="_blank" rel="noopener" href="https://web.archive.org/web/20171013103233/http://publisher-connector.core.ac.uk/resourcesync/data/Springer-OA/pdf/5f4/aHR0cDovL2xpbmsuc3ByaW5nZXIuY29tLzEwLjEwMDcvczExMzAyLTAwNi05MDA2LTIucGRm.pdf" title="fulltext PDF download" data-goatcounter-click="serp-fulltext" data-goatcounter-title="serp-fulltext"> <button class="ui simple right pointing dropdown compact black labeled icon button serp-button"> <i class="icon ia-icon"></i> Web Archive [PDF] </button> </a> <a target="_blank" rel="external noopener noreferrer" href="https://doi.org/10.1007/s11302-006-9006-2"> <button class="ui left aligned compact blue labeled icon button serp-button"> <i class="external alternate icon"></i> springer.com </button> </a> <a target="_blank" rel="external noopener" href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2096525" title="pubmed link"> <button class="ui compact blue labeled icon button serp-button"> <i class="file alternate outline icon"></i> pubmed.gov </button> </a>

Mannich bases in medicinal chemistry and drug design

Gheorghe Roman
<span title="2014-10-30">2015</span> <i title="Elsevier BV"> <a target="_blank" rel="noopener" href="https://fatcat.wiki/container/gzsdtozdnzdfhp5x7vn5vz6a7a" style="color: black;">European Journal of Medicinal Chemistry</a> </i> &nbsp;
The review gives in the end a brief overview of the potential of Mannich bases as inhibitors of various enzymes or ligands for several receptors.  ...  as their use as agents for the treatment of mental disorders have been presented.  ...  Starting from a hit obtained by screening a large library of compounds, and employing subsequent stepwise refinement of structural features, a series of Mannich bases 367 (R ¼ (substituted) phenyl) of  ... 
<span class="external-identifiers"> <a target="_blank" rel="external noopener noreferrer" href="https://doi.org/10.1016/j.ejmech.2014.10.076">doi:10.1016/j.ejmech.2014.10.076</a> <a target="_blank" rel="external noopener" href="https://www.ncbi.nlm.nih.gov/pubmed/25462280">pmid:25462280</a> <a target="_blank" rel="external noopener" href="https://pubmed.ncbi.nlm.nih.gov/PMC7115492/">pmcid:PMC7115492</a> <a target="_blank" rel="external noopener" href="https://fatcat.wiki/release/yhhji2htkjg5rkkex55r7vsfxu">fatcat:yhhji2htkjg5rkkex55r7vsfxu</a> </span>
<a target="_blank" rel="noopener" href="https://web.archive.org/web/20200407071512/http://europepmc.org/backend/ptpmcrender.fcgi?accid=PMC7115492&amp;blobtype=pdf" title="fulltext PDF download" data-goatcounter-click="serp-fulltext" data-goatcounter-title="serp-fulltext"> <button class="ui simple right pointing dropdown compact black labeled icon button serp-button"> <i class="icon ia-icon"></i> Web Archive [PDF] <div class="menu fulltext-thumbnail"> <img src="https://blobs.fatcat.wiki/thumbnail/pdf/39/65/39653fbc28c4914dd863c55b10481d669a9989a1.180px.jpg" alt="fulltext thumbnail" loading="lazy"> </div> </button> </a> <a target="_blank" rel="external noopener noreferrer" href="https://doi.org/10.1016/j.ejmech.2014.10.076"> <button class="ui left aligned compact blue labeled icon button serp-button"> <i class="external alternate icon"></i> elsevier.com </button> </a> <a target="_blank" rel="external noopener" href="https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7115492" title="pubmed link"> <button class="ui compact blue labeled icon button serp-button"> <i class="file alternate outline icon"></i> pubmed.gov </button> </a>

Prediction of competitive CYP450 2C9 inhibitors using 3D-Pharmacophore models

Martin Pramesberger
<span title="">2019</span> <span class="release-stage">unpublished</span>
The program LigandScout (4.4 Expert) was used for processing and filtering compound libraries, 3D-pharmacophore modeling, virtual screening and activity profiling.  ...  The results of this work consist of six ligand-based 3D-pharmacophore models, which can be used for the prediction of competitive inhibitors of CYP450 2C9.  ...  2.4.3 3D-Pharmacophore-based virtual screening ...........................................enzymes are of big relevance in the human body, since they are responsible for the production of endogenous substances  ... 
<span class="external-identifiers"> <a target="_blank" rel="external noopener noreferrer" href="https://doi.org/10.25365/thesis.58003">doi:10.25365/thesis.58003</a> <a target="_blank" rel="external noopener" href="https://fatcat.wiki/release/peoq5rl4xrb4dal3yb3psjogva">fatcat:peoq5rl4xrb4dal3yb3psjogva</a> </span>
<a target="_blank" rel="noopener" href="https://web.archive.org/web/20200811225230/http://othes.univie.ac.at/58003/1/61692.pdf" title="fulltext PDF download" data-goatcounter-click="serp-fulltext" data-goatcounter-title="serp-fulltext"> <button class="ui simple right pointing dropdown compact black labeled icon button serp-button"> <i class="icon ia-icon"></i> Web Archive [PDF] <div class="menu fulltext-thumbnail"> <img src="https://blobs.fatcat.wiki/thumbnail/pdf/8d/45/8d4527b9c1f2e6313b4aa6144033408e5d36d29c.180px.jpg" alt="fulltext thumbnail" loading="lazy"> </div> </button> </a> <a target="_blank" rel="external noopener noreferrer" href="https://doi.org/10.25365/thesis.58003"> <button class="ui left aligned compact blue labeled icon button serp-button"> <i class="external alternate icon"></i> Publisher / doi.org </button> </a>

Nemosis [chapter]

Antti Vaheri
<span title="">2017</span> <i title="Springer Berlin Heidelberg"> Encyclopedia of Cancer </i> &nbsp;
Adebusola Alagbala Ajibade and Christopher Loo for manuscript editing.  ...  Refined models are imperative to unravel specific NK receptor functions, since target cells generally express ligands for several NK receptors.  ...  Numerous other chemical entities of natural origin are under preclinical development and clinical trial, and these have been discovered, largely as a result of the use of refined screening techniques using  ... 
<span class="external-identifiers"> <a target="_blank" rel="external noopener noreferrer" href="https://doi.org/10.1007/978-3-662-46875-3_4002">doi:10.1007/978-3-662-46875-3_4002</a> <a target="_blank" rel="external noopener" href="https://fatcat.wiki/release/xt3vgg7pyjes5hmumo2qkyhlni">fatcat:xt3vgg7pyjes5hmumo2qkyhlni</a> </span>
<a target="_blank" rel="noopener" href="https://web.archive.org/web/20180730121658/https://link.springer.com/content/pdf/10.1007%2F978-3-662-46875-3_4002.pdf" title="fulltext PDF download" data-goatcounter-click="serp-fulltext" data-goatcounter-title="serp-fulltext"> <button class="ui simple right pointing dropdown compact black labeled icon button serp-button"> <i class="icon ia-icon"></i> Web Archive [PDF] <div class="menu fulltext-thumbnail"> <img src="https://blobs.fatcat.wiki/thumbnail/pdf/67/91/679159484b4809b06bc62aaa3d58b0627ef2c66a.180px.jpg" alt="fulltext thumbnail" loading="lazy"> </div> </button> </a> <a target="_blank" rel="external noopener noreferrer" href="https://doi.org/10.1007/978-3-662-46875-3_4002"> <button class="ui left aligned compact blue labeled icon button serp-button"> <i class="external alternate icon"></i> springer.com </button> </a>

CXCR6 Promotes Atherosclerosis by Supporting T-Cell Homing, Interferon- Production, and Macrophage Accumulation in the Aortic Wall

E. Galkina, B. L. Harry, A. Ludwig, E. A. Liehn, J. M. Sanders, A. Bruce, C. Weber, K. Ley
<span title="2007-10-16">2007</span> <i title="Ovid Technologies (Wolters Kluwer Health)"> <a target="_blank" rel="noopener" href="https://fatcat.wiki/container/yp7myvwge5ef7jsub32vmdbdhy" style="color: black;">Circulation</a> </i> &nbsp;
Genetic or pharmacological inhibition of one of these pathways may result in the shunting of arachidonic or linoleic acid down the12-LO pathway.  ...  Therefore, we sought to determine the effect of 12-LO deficiency on AngII-induced AAA formation.  ...  refined, wheat-based or oat ϩ wheat-based foods for 12 weeks.  ... 
<span class="external-identifiers"> <a target="_blank" rel="external noopener noreferrer" href="https://doi.org/10.1161/circulationaha.106.678474">doi:10.1161/circulationaha.106.678474</a> <a target="_blank" rel="external noopener" href="https://www.ncbi.nlm.nih.gov/pubmed/17909108">pmid:17909108</a> <a target="_blank" rel="external noopener" href="https://fatcat.wiki/release/dmlajnutxzfynpn7yok5yo6l6q">fatcat:dmlajnutxzfynpn7yok5yo6l6q</a> </span>
<a target="_blank" rel="noopener" href="https://web.archive.org/web/20171025173754/http://atvb.ahajournals.org/content/atvbaha/27/6/e35.full.pdf" title="fulltext PDF download" data-goatcounter-click="serp-fulltext" data-goatcounter-title="serp-fulltext"> <button class="ui simple right pointing dropdown compact black labeled icon button serp-button"> <i class="icon ia-icon"></i> Web Archive [PDF] </button> </a> <a target="_blank" rel="external noopener noreferrer" href="https://doi.org/10.1161/circulationaha.106.678474"> <button class="ui left aligned compact blue labeled icon button serp-button"> <i class="external alternate icon"></i> Publisher / doi.org </button> </a>

Fortieth Annual Meeting February 17-21, 1996 Baltimore Convention Center Baltimore, Maryland. Wednesday Symposia and Posters, Part III

<span title="">1996</span> <i title="Elsevier BV"> <a target="_blank" rel="noopener" href="https://fatcat.wiki/container/dez2wau7t5aqvklzwrcsreuwq4" style="color: black;">Biophysical Journal</a> </i> &nbsp;
The results show that the single fibre model of eccentric contraction-induced muscle damage is structurally, as well as functionally, akin to the human condition.  ...  It is thus suggested that the inhibition of the formation of "strong-binding" is an important factor in the mechanism for the regulation of smooth muscle contraction. Supp. by grants from RBRF& NIH.  ...  ( PoslOl INHIBITORY EFFECT BY THROMBOXANE A, AGONIST ON Kc, CHANNEL ACTIVITY IN HUMAN CORONARY ARTERY SMOOTH MUSCLE CELLS.  ... 
<span class="external-identifiers"> <a target="_blank" rel="external noopener noreferrer" href="https://doi.org/10.1016/s0006-3495(96)79672-8">doi:10.1016/s0006-3495(96)79672-8</a> <a target="_blank" rel="external noopener" href="https://fatcat.wiki/release/ohs2vrzsxvbppaarefqlgaya5u">fatcat:ohs2vrzsxvbppaarefqlgaya5u</a> </span>
<a target="_blank" rel="noopener" href="https://web.archive.org/web/20170924142719/http://publisher-connector.core.ac.uk/resourcesync/data/elsevier/pdf/168/aHR0cDovL2FwaS5lbHNldmllci5jb20vY29udGVudC9hcnRpY2xlL3BpaS9zMDAwNjM0OTU5Njc5NjcyOA%3D%3D.pdf" title="fulltext PDF download" data-goatcounter-click="serp-fulltext" data-goatcounter-title="serp-fulltext"> <button class="ui simple right pointing dropdown compact black labeled icon button serp-button"> <i class="icon ia-icon"></i> Web Archive [PDF] <div class="menu fulltext-thumbnail"> <img src="https://blobs.fatcat.wiki/thumbnail/pdf/79/53/7953374f3c876647da287ac635761196b21c77d7.180px.jpg" alt="fulltext thumbnail" loading="lazy"> </div> </button> </a> <a target="_blank" rel="external noopener noreferrer" href="https://doi.org/10.1016/s0006-3495(96)79672-8"> <button class="ui left aligned compact blue labeled icon button serp-button"> <i class="external alternate icon"></i> elsevier.com </button> </a>

Nucleotide Excision Repair [chapter]

W. Glenn McGregor
<i title="Springer Berlin Heidelberg"> Encyclopedia of Cancer </i> &nbsp;
Branch for critical reading of the manuscript.  ...  Refined models are imperative to unravel specific NK receptor functions, since target cells generally express ligands for several NK receptors.  ...  Clinical Relevance Interruption of autocrine and paracrine neuropeptide signaling with specific antagonists are considered to be new therapeutic approaches to the treatment of human cancers.  ... 
<span class="external-identifiers"> <a target="_blank" rel="external noopener noreferrer" href="https://doi.org/10.1007/978-3-540-47648-1_4171">doi:10.1007/978-3-540-47648-1_4171</a> <a target="_blank" rel="external noopener" href="https://fatcat.wiki/release/afxc3k5v6rdqrjljpo45alridy">fatcat:afxc3k5v6rdqrjljpo45alridy</a> </span>
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BULGARIAN CHEMICAL COMMUNICATIONS BULGARIAN CHEMICAL COMMUNICATIONS A quarterly published by THE BULGARIAN ACADEMY OF SCIENCES and THE UNION OF CHEMISTS IN BULGARIA ИЗВЕСТИЯ ПО ХИМИЯ Тримесечно издание на БЪЛГАРСКА АКАДЕМИЯ НА НАУКИТЕ и СЪЮЗ НА ХИМИЦИТЕ В БЪЛГАРИЯ

Ch Bonev, P Bontchev, L Boyadzhiev, I Gutzow, I Havezov, E Ivanova, K Petkov, K Petrov, L Petrov, I Pojarlieff, S Rakovsky, D Stoychev (+4 others)
<span title="">2017</span> <i > Hungary) Bulgarian Chemical Communications </i> &nbsp; <span class="release-stage">unpublished</span>
There are two broad categories of computational techniques in virtual screening: 1) a ligand-based screening uses pharmacophore maps and QSAR, which requires knowledge of some ligands that exhibit the  ...  The main feature of the uterus is predominantly expression of AT2 type receptors [25] in myometrium and the uterine artery [26] .  ...  prostaglandin E2 receptor subtype EP3-I (EP3-I), and thromboxane A2 (TP ) [33] .  ... 
<span class="external-identifiers"> <a target="_blank" rel="external noopener" href="https://fatcat.wiki/release/ti6dehpecrghfifkqp2xijtwca">fatcat:ti6dehpecrghfifkqp2xijtwca</a> </span>
<a target="_blank" rel="noopener" href="https://web.archive.org/web/20180410003051/http://www.bcc.bas.bg/BCC_Volumes/Volume_49_Special_E_2017/BCC-49-E-2017-Peptides.pdf" title="fulltext PDF download" data-goatcounter-click="serp-fulltext" data-goatcounter-title="serp-fulltext"> <button class="ui simple right pointing dropdown compact black labeled icon button serp-button"> <i class="icon ia-icon"></i> Web Archive [PDF] </button> </a>

Exploring aspects of allosteric modulation and bias signalling at the glucagon-like peptide-1 receptor

Emilia Elizabeth Savage
<span title="2017-03-01">2017</span>
It is widely accepted that insulin secretion downstream of GLP-1R activation is critically dependent on cAMP formation, but recent evidence is also emerging for an essential role of regulatory proteins  ...  The glucagon-like peptide-1 receptor (GLP-1R) is an important regulator of insulin biosynthesis and secretion, and is one of the key therapeutic targets in the management of type II diabetes mellitus and  ...  Acknowledgements PMS and AC are Principal Research Fellows of the National Health and Medical Research Council of Australia (NHMRC).  ... 
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