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1.
Nucleic Acids Res ; 2021 Oct 30.
Artigo em Inglês | MEDLINE | ID: mdl-34718737

RESUMO

The IUPHAR/BPS Guide to PHARMACOLOGY (GtoPdb; www.guidetopharmacology.org) is an open-access, expert-curated database of molecular interactions between ligands and their targets. We describe expansion in content over nine database releases made during the last two years, which has focussed on three main areas of infection. The COVID-19 pandemic continues to have a major impact on health worldwide. GtoPdb has sought to support the wider research community to understand the pharmacology of emerging drug targets for SARS-CoV-2 as well as potential targets in the host to block viral entry and reduce the adverse effects of infection in patients with COVID-19. We describe how the database rapidly evolved to include a new family of Coronavirus proteins. Malaria remains a global threat to half the population of the world. Our database content continues to be enhanced through our collaboration with Medicines for Malaria Venture (MMV) on the IUPHAR/MMV Guide to MALARIA PHARMACOLOGY (www.guidetomalariapharmacology.org). Antibiotic resistance is also a growing threat to global health. In response, we have extended our coverage of antibacterials in partnership with AntibioticDB.

3.
Br J Pharmacol ; 178(7): 1507-1523, 2021 04.
Artigo em Inglês | MEDLINE | ID: mdl-33444462

RESUMO

BACKGROUND AND PURPOSE: The enzyme α/ß-hydrolase domain containing 6 (ABHD6), a new member of the endocannabinoid system, is a promising therapeutic target against neuronal-related diseases. However, how ABHD6 activity is regulated is not known. ABHD6 coexists in protein complexes with the brain-specific carnitine palmitoyltransferase 1C (CPT1C). CPT1C is involved in neuro-metabolic functions, depending on brain malonyl-CoA levels. Our aim was to study CPT1C-ABHD6 interaction and determine whether CPT1C is a key regulator of ABHD6 activity depending on nutritional status. EXPERIMENTAL APPROACH: Co-immunoprecipitation and FRET assays were used to explore ABHD6 interaction with CPT1C or modified malonyl-CoA-insensitive or C-terminal truncated CPT1C forms. Cannabinoid CB1 receptor-mediated signalling was investigated by determining cAMP levels. A novel highly sensitive fluorescent method was optimized to measure ABHD6 activity in non-neuronal and neuronal cells and in brain tissues from wild-type (WT) and CPT1C-KO mice. KEY RESULTS: CPT1C interacted with ABHD6 and negatively regulated its hydrolase activity, thereby regulating 2-AG downstream signalling. Accordingly, brain tissues of CPT1C-KO mice showed increased ABHD6 activity. CPT1C malonyl-CoA sensing was key to the regulatory role on ABHD6 activity and CB1 receptor signalling. Fasting, which attenuates brain malonyl-CoA, significantly increased ABHD6 activity in hypothalamus from WT, but not CPT1C-KO, mice. CONCLUSIONS AND IMPLICATIONS: Our finding that negative regulation of ABHD6 activity, particularly in the hypothalamus, is sensitive to nutritional status throws new light on the characterization and the importance of the proteins involved as potential targets against diseases affecting the CNS.


Assuntos
Carnitina O-Palmitoiltransferase , Monoacilglicerol Lipases/metabolismo , Estado Nutricional , Animais , Carnitina O-Palmitoiltransferase/genética , Hidrolases , Malonil Coenzima A , Camundongos
4.
Adv Exp Med Biol ; 1264: 15-28, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33332001

RESUMO

Most of our current understanding of the neuromolecular mechanisms of Cannabis action focusses on two plant cannabinoids, THC and CBD. THC acts primarily through presynaptic CB cannabinoid receptors to regulate neurotransmitter release in the brain, spinal cord and peripheral nerves. CBD action, on the other hand, is probably mediated through multiple molecular targets.


Assuntos
Canabinoides/farmacologia , Cannabis/química , Transmissão Sináptica/efeitos dos fármacos , Canabidiol/farmacologia , Dronabinol/farmacologia , Humanos , Neurotransmissores/metabolismo , Receptores de Canabinoides/metabolismo
6.
Immunology ; 160(1): 10-23, 2020 05.
Artigo em Inglês | MEDLINE | ID: mdl-32020584

RESUMO

Given the critical role that the immune system plays in a multitude of diseases, having a clear understanding of the pharmacology of the immune system is crucial to new drug discovery and development. Here we describe the International Union of Basic and Clinical Pharmacology (IUPHAR) Guide to Immunopharmacology (GtoImmuPdb), which connects expert-curated pharmacology with key immunological concepts and aims to put pharmacological data into the hands of immunologists. In the pursuit of new therapeutics, pharmacological databases are a vital resource to researchers through providing accurate information on the fundamental science underlying drug action. This extension to the existing IUPHAR/British Pharmacological Society Guide to Pharmacology supports research into the development of drugs targeted at modulating immune, inflammatory or infectious components of disease. To provide a deeper context for how the resource can support research we show data in GtoImmuPdb relating to a case study on the targeting of vascular inflammation.


Assuntos
Bases de Dados de Produtos Farmacêuticos , Desenvolvimento de Medicamentos , Descoberta de Drogas , Sistema Imunitário/diagnóstico por imagem , Fatores Imunológicos/farmacologia , Alergia e Imunologia/educação , Anticorpos Monoclonais Humanizados/farmacologia , Anticorpos Monoclonais Humanizados/uso terapêutico , Aterosclerose/tratamento farmacológico , Aterosclerose/imunologia , Aterosclerose/prevenção & controle , Humanos , Fatores Imunológicos/uso terapêutico , Mediadores da Inflamação/metabolismo , Cooperação Internacional , Terapia de Alvo Molecular/métodos , Pesquisa Farmacêutica/educação , Farmacologia Clínica/educação , Ensaios Clínicos Controlados Aleatórios como Assunto , Transdução de Sinais/efeitos dos fármacos , Transdução de Sinais/imunologia , Sociedades Científicas/organização & administração , Resultado do Tratamento
7.
Nucleic Acids Res ; 48(D1): D1006-D1021, 2020 01 08.
Artigo em Inglês | MEDLINE | ID: mdl-31691834

RESUMO

The IUPHAR/BPS Guide to PHARMACOLOGY (www.guidetopharmacology.org) is an open-access, expert-curated database of molecular interactions between ligands and their targets. We describe significant updates made over the seven releases during the last two years. The database is notably enhanced through the continued linking of relevant pharmacology with key immunological data types as part of the IUPHAR Guide to IMMUNOPHARMACOLOGY (www.guidetoimmunopharmacology.org) and by a major new extension, the IUPHAR/MMV Guide to Malaria PHARMACOLOGY (www.guidetomalariapharmacology.org). The latter has been constructed in partnership with the Medicines for Malaria Venture, an organization dedicated to identifying, developing and delivering new antimalarial therapies that are both effective and affordable. This is in response to the global challenge of over 200 million cases of malaria and 400 000 deaths worldwide, with the majority in the WHO Africa Region. It provides new pharmacological content, including molecular targets in the malaria parasite, interaction data for ligands with antimalarial activity, and establishes curation of data from screening assays, used routinely in antimalarial drug discovery, against the whole organism. A dedicated portal has been developed to provide quick and focused access to these new data.


Assuntos
Antimaláricos/farmacologia , Bases de Dados Factuais , Bases de Dados de Produtos Farmacêuticos , Descoberta de Drogas/métodos , Farmacologia , Antimaláricos/uso terapêutico , Humanos , Ligantes , Malária/tratamento farmacológico , Malária/parasitologia , Terapia de Alvo Molecular , Plasmodium/efeitos dos fármacos , Software , Interface Usuário-Computador , Navegador
8.
Br J Pharmacol ; 176 Suppl 1: S397-S493, 2019 12.
Artigo em Inglês | MEDLINE | ID: mdl-31710713

RESUMO

The Concise Guide to PHARMACOLOGY 2019/20 is the fourth in this series of biennial publications. The Concise Guide provides concise overviews of the key properties of nearly 1800 human drug targets with an emphasis on selective pharmacology (where available), plus links to the open access knowledgebase source of drug targets and their ligands (www.guidetopharmacology.org), which provides more detailed views of target and ligand properties. Although the Concise Guide represents approximately 400 pages, the material presented is substantially reduced compared to information and links presented on the website. It provides a permanent, citable, point-in-time record that will survive database updates. The full contents of this section can be found at http://onlinelibrary.wiley.com/doi/10.1111/bph.14753. Transporters are one of the six major pharmacological targets into which the Guide is divided, with the others being: G protein-coupled receptors, ion channels, nuclear hormone receptors, catalytic receptors and enzymes. These are presented with nomenclature guidance and summary information on the best available pharmacological tools, alongside key references and suggestions for further reading. The landscape format of the Concise Guide is designed to facilitate comparison of related targets from material contemporary to mid-2019, and supersedes data presented in the 2017/18, 2015/16 and 2013/14 Concise Guides and previous Guides to Receptors and Channels. It is produced in close conjunction with the International Union of Basic and Clinical Pharmacology Committee on Receptor Nomenclature and Drug Classification (NC-IUPHAR), therefore, providing official IUPHAR classification and nomenclature for human drug targets, where appropriate.


Assuntos
Transportadores de Cassetes de Ligação de ATP/química , Canais Iônicos/química , Preparações Farmacêuticas/química , Receptores de Superfície Celular/química , Receptores Citoplasmáticos e Nucleares/química , Transportadores de Cassetes de Ligação de ATP/agonistas , Transportadores de Cassetes de Ligação de ATP/antagonistas & inibidores , Animais , Bases de Dados de Produtos Farmacêuticos , Humanos , Canais Iônicos/agonistas , Canais Iônicos/antagonistas & inibidores , Ligantes , Receptores de Superfície Celular/agonistas , Receptores de Superfície Celular/antagonistas & inibidores , Receptores Citoplasmáticos e Nucleares/agonistas , Receptores Citoplasmáticos e Nucleares/antagonistas & inibidores
9.
Br J Pharmacol ; 176 Suppl 1: S297-S396, 2019 12.
Artigo em Inglês | MEDLINE | ID: mdl-31710714

RESUMO

The Concise Guide to PHARMACOLOGY 2019/20 is the fourth in this series of biennial publications. The Concise Guide provides concise overviews of the key properties of nearly 1800 human drug targets with an emphasis on selective pharmacology (where available), plus links to the open access knowledgebase source of drug targets and their ligands (www.guidetopharmacology.org), which provides more detailed views of target and ligand properties. Although the Concise Guide represents approximately 400 pages, the material presented is substantially reduced compared to information and links presented on the website. It provides a permanent, citable, point-in-time record that will survive database updates. The full contents of this section can be found at http://onlinelibrary.wiley.com/doi/10.1111/bph.14752. Enzymes are one of the six major pharmacological targets into which the Guide is divided, with the others being: G protein-coupled receptors, ion channels, nuclear hormone receptors, catalytic receptors and transporters. These are presented with nomenclature guidance and summary information on the best available pharmacological tools, alongside key references and suggestions for further reading. The landscape format of the Concise Guide is designed to facilitate comparison of related targets from material contemporary to mid-2019, and supersedes data presented in the 2017/18, 2015/16 and 2013/14 Concise Guides and previous Guides to Receptors and Channels. It is produced in close conjunction with the International Union of Basic and Clinical Pharmacology Committee on Receptor Nomenclature and Drug Classification (NC-IUPHAR), therefore, providing official IUPHAR classification and nomenclature for human drug targets, where appropriate.


Assuntos
Inibidores Enzimáticos/farmacologia , Hidrolases/antagonistas & inibidores , Isomerases/antagonistas & inibidores , Ligases/antagonistas & inibidores , Liases/antagonistas & inibidores , Oxirredutases/antagonistas & inibidores , Transferases/antagonistas & inibidores , Animais , Bases de Dados de Produtos Farmacêuticos , Inibidores Enzimáticos/química , Humanos , Hidrolases/química , Hidrolases/metabolismo , Isomerases/química , Isomerases/metabolismo , Ligantes , Ligases/química , Ligases/metabolismo , Liases/química , Liases/metabolismo , Oxirredutases/química , Oxirredutases/metabolismo , Transferases/química , Transferases/metabolismo
10.
Br J Pharmacol ; 176 Suppl 1: S247-S296, 2019 12.
Artigo em Inglês | MEDLINE | ID: mdl-31710716

RESUMO

The Concise Guide to PHARMACOLOGY 2019/20 is the fourth in this series of biennial publications. The Concise Guide provides concise overviews of the key properties of nearly 1800 human drug targets with an emphasis on selective pharmacology (where available), plus links to the open access knowledgebase source of drug targets and their ligands (www.guidetopharmacology.org), which provides more detailed views of target and ligand properties. Although the Concise Guide represents approximately 400 pages, the material presented is substantially reduced compared to information and links presented on the website. It provides a permanent, citable, point-in-time record that will survive database updates. The full contents of this section can be found at http://onlinelibrary.wiley.com/doi/10.1111/bph.14751. Catalytic receptors are one of the six major pharmacological targets into which the Guide is divided, with the others being: G protein-coupled receptors, ion channels, nuclear hormone receptors, enzymes and transporters. These are presented with nomenclature guidance and summary information on the best available pharmacological tools, alongside key references and suggestions for further reading. The landscape format of the Concise Guide is designed to facilitate comparison of related targets from material contemporary to mid-2019, and supersedes data presented in the 2017/18, 2015/16 and 2013/14 Concise Guides and previous Guides to Receptors and Channels. It is produced in close conjunction with the International Union of Basic and Clinical Pharmacology Committee on Receptor Nomenclature and Drug Classification (NC-IUPHAR), therefore, providing official IUPHAR classification and nomenclature for human drug targets, where appropriate.


Assuntos
Peptídeos/farmacologia , Receptores de Superfície Celular/agonistas , Animais , Bases de Dados de Produtos Farmacêuticos , Humanos , Ligantes , Peptídeos/química , Receptores de Superfície Celular/química
11.
Br J Pharmacol ; 176 Suppl 1: S1-S20, 2019 12.
Artigo em Inglês | MEDLINE | ID: mdl-31710719

RESUMO

The Concise Guide to PHARMACOLOGY 2019/20 is the fourth in this series of biennial publications. The Concise Guide provides concise overviews of the key properties of nearly 1800 human drug targets with an emphasis on selective pharmacology (where available), plus links to the open access knowledgebase source of drug targets and their ligands (www.guidetopharmacology.org), which provides more detailed views of target and ligand properties. Although the Concise Guide represents approximately 400 pages, the material presented is substantially reduced compared to information and links presented on the website. It provides a permanent, citable, point-in-time record that will survive database updates. The full contents of this section can be found at http://onlinelibrary.wiley.com/doi/10.1111/bph.14747. In addition to this overview, in which are identified Other protein targets which fall outside of the subsequent categorisation, there are six areas of focus: G protein-coupled receptors, ion channels, nuclear hormone receptors, catalytic receptors, enzymes and transporters. These are presented with nomenclature guidance and summary information on the best available pharmacological tools, alongside key references and suggestions for further reading. The landscape format of the Concise Guide is designed to facilitate comparison of related targets from material contemporary to mid-2019, and supersedes data presented in the 2017/18, 2015/16 and 2013/14 Concise Guides and previous Guides to Receptors and Channels. It is produced in close conjunction with the International Union of Basic and Clinical Pharmacology Committee on Receptor Nomenclature and Drug Classification (NC-IUPHAR), therefore, providing official IUPHAR classification and nomenclature for human drug targets, where appropriate.


Assuntos
Transportadores de Cassetes de Ligação de ATP/agonistas , Canais Iônicos/agonistas , Preparações Farmacêuticas/química , Proteínas/agonistas , Receptores de Superfície Celular/agonistas , Receptores Citoplasmáticos e Nucleares/agonistas , Transportadores de Cassetes de Ligação de ATP/química , Animais , Bases de Dados de Produtos Farmacêuticos , Humanos , Canais Iônicos/química , Ligantes , Transporte Proteico/efeitos dos fármacos , Proteínas/química , Receptores de Superfície Celular/química , Receptores Citoplasmáticos e Nucleares/química
12.
Br J Pharmacol ; 176 Suppl 1: S229-S246, 2019 12.
Artigo em Inglês | MEDLINE | ID: mdl-31710718

RESUMO

The Concise Guide to PHARMACOLOGY 2019/20 is the fourth in this series of biennial publications. The Concise Guide provides concise overviews of the key properties of nearly 1800 human drug targets with an emphasis on selective pharmacology (where available), plus links to the open access knowledgebase source of drug targets and their ligands (www.guidetopharmacology.org), which provides more detailed views of target and ligand properties. Although the Concise Guide represents approximately 400 pages, the material presented is substantially reduced compared to information and links presented on the website. It provides a permanent, citable, point-in-time record that will survive database updates. The full contents of this section can be found at http://onlinelibrary.wiley.com/doi/10.1111/bph.14750. Nuclear hormone receptors are one of the six major pharmacological targets into which the Guide is divided, with the others being: G protein-coupled receptors, catalytic receptors, enzymes and transporters. These are presented with nomenclature guidance and summary information on the best available pharmacological tools, alongside key references and suggestions for further reading. The landscape format of the Concise Guide is designed to facilitate comparison of related targets from material contemporary to mid-2019, and supersedes data presented in the 2017/18, 2015/16 and 2013/14 Concise Guides and previous Guides to Receptors and Channels. It is produced in close conjunction with the International Union of Basic and Clinical Pharmacology Committee on Receptor Nomenclature and Drug Classification (NC-IUPHAR), therefore, providing official IUPHAR classification and nomenclature for human drug targets, where appropriate.


Assuntos
Preparações Farmacêuticas/química , Receptores Citoplasmáticos e Nucleares/agonistas , Animais , Bases de Dados de Produtos Farmacêuticos , Humanos , Ligantes , Receptores Citoplasmáticos e Nucleares/química , Receptores Citoplasmáticos e Nucleares/genética
13.
Br J Pharmacol ; 176 Suppl 1: S142-S228, 2019 12.
Artigo em Inglês | MEDLINE | ID: mdl-31710715

RESUMO

The Concise Guide to PHARMACOLOGY 2019/20 is the fourth in this series of biennial publications. The Concise Guide provides concise overviews of the key properties of nearly 1800 human drug targets with an emphasis on selective pharmacology (where available), plus links to the open access knowledgebase source of drug targets and their ligands (www.guidetopharmacology.org), which provides more detailed views of target and ligand properties. Although the Concise Guide represents approximately 400 pages, the material presented is substantially reduced compared to information and links presented on the website. It provides a permanent, citable, point-in-time record that will survive database updates. The full contents of this section can be found at http://onlinelibrary.wiley.com/doi/10.1111/bph.14749. Ion channels are one of the six major pharmacological targets into which the Guide is divided, with the others being: G protein-coupled receptors, nuclear hormone receptors, catalytic receptors, enzymes and transporters. These are presented with nomenclature guidance and summary information on the best available pharmacological tools, alongside key references and suggestions for further reading. The landscape format of the Concise Guide is designed to facilitate comparison of related targets from material contemporary to mid-2019, and supersedes data presented in the 2017/18, 2015/16 and 2013/14 Concise Guides and previous Guides to Receptors and Channels. It is produced in close conjunction with the International Union of Basic and Clinical Pharmacology Committee on Receptor Nomenclature and Drug Classification (NC-IUPHAR), therefore, providing official IUPHAR classification and nomenclature for human drug targets, where appropriate.


Assuntos
Canais Iônicos/agonistas , Preparações Farmacêuticas/química , Animais , Bases de Dados de Produtos Farmacêuticos , Humanos , Canais Iônicos/química , Ligantes
14.
Br J Pharmacol ; 176 Suppl 1: S21-S141, 2019 12.
Artigo em Inglês | MEDLINE | ID: mdl-31710717

RESUMO

The Concise Guide to PHARMACOLOGY 2019/20 is the fourth in this series of biennial publications. The Concise Guide provides concise overviews of the key properties of nearly 1800 human drug targets with an emphasis on selective pharmacology (where available), plus links to the open access knowledgebase source of drug targets and their ligands (www.guidetopharmacology.org), which provides more detailed views of target and ligand properties. Although the Concise Guide represents approximately 400 pages, the material presented is substantially reduced compared to information and links presented on the website. It provides a permanent, citable, point-in-time record that will survive database updates. The full contents of this section can be found at http://onlinelibrary.wiley.com/doi/10.1111/bph.14748. G protein-coupled receptors are one of the six major pharmacological targets into which the Guide is divided, with the others being: ion channels, nuclear hormone receptors, catalytic receptors, enzymes and transporters. These are presented with nomenclature guidance and summary information on the best available pharmacological tools, alongside key references and suggestions for further reading. The landscape format of the Concise Guide is designed to facilitate comparison of related targets from material contemporary to mid-2019, and supersedes data presented in the 2017/18, 2015/16 and 2013/14 Concise Guides and previous Guides to Receptors and Channels. It is produced in close conjunction with the International Union of Basic and Clinical Pharmacology Committee on Receptor Nomenclature and Drug Classification (NC-IUPHAR), therefore, providing official IUPHAR classification and nomenclature for human drug targets, where appropriate.


Assuntos
Preparações Farmacêuticas/química , Receptores Acoplados a Proteínas G/agonistas , Animais , Bases de Dados de Produtos Farmacêuticos , Humanos , Ligantes , Receptores Acoplados a Proteínas G/química , Receptores Acoplados a Proteínas G/metabolismo
15.
Br J Pharmacol ; 176(10): 1359-1360, 2019 05.
Artigo em Inglês | MEDLINE | ID: mdl-31032895

RESUMO

LINKED ARTICLES: This article is part of a themed section on 8th European Workshop on Cannabinoid Research. To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v176.10/issuetoc.


Assuntos
Canabinoides/farmacologia , Animais , Humanos , Camundongos
17.
Biochim Biophys Acta Mol Cell Biol Lipids ; 1863(11): 1433-1440, 2018 11.
Artigo em Inglês | MEDLINE | ID: mdl-30591150

RESUMO

Anandamide, the first identified endogenous cannabinoid and TRPV1 agonist, is one of a series of endogenous N-acylethanolamines, NAEs. We have generated novel assays to quantify the levels of multiple NAEs in biological tissues and their rates of hydrolysis through fatty acid amide hydrolase. This range of NAEs was also tested in rapid response assays of CB1, CB2 cannabinoid and TRPV1 receptors. The data indicate that PEA, SEA and OEA are not endocannabinoids or endovanilloids, and that the higher endogenous levels of these metabolites compared to polyunsaturated analogues are a correlate of their slow rates of hydrolysis. The n-6 NAEs (AEA, docosatetraenoyl and docosapentaenoyl derivatives) activated both CB1 and CB2 receptors, as well as TRPV1 channels, suggesting them to be 'genuine' endocannabinoids and 'endovanilloids'. The n-3 NAEs (eicosapentaenoyl, docosapentaenoyl and docosahexaenoyl derivatives) activated CB2 receptors and some n-3 NAEs (docosapentaenoyl and docosahexaenoyl derivatives) also activated TRPV1 channels, but failed to activate the CB1 receptor. We hypothesise that the preferential activation of CB2 receptors by n-3 PUFA NAEs contributes, at least in some part, to their broad anti-inflammatory profile.


Assuntos
Etanolaminas/metabolismo , Fígado/metabolismo , Mesencéfalo/metabolismo , Receptor CB2 de Canabinoide/metabolismo , Animais , Endocanabinoides/metabolismo , Ácidos Graxos Ômega-3/metabolismo , Humanos , Hidrólise , Espectrometria de Massas , Ratos , Ratos Sprague-Dawley , Receptor CB1 de Canabinoide/metabolismo , Canais de Cátion TRPV/metabolismo
18.
Nucleic Acids Res ; 46(D1): D1091-D1106, 2018 01 04.
Artigo em Inglês | MEDLINE | ID: mdl-29149325

RESUMO

The IUPHAR/BPS Guide to PHARMACOLOGY (GtoPdb, www.guidetopharmacology.org) and its precursor IUPHAR-DB, have captured expert-curated interactions between targets and ligands from selected papers in pharmacology and drug discovery since 2003. This resource continues to be developed in conjunction with the International Union of Basic and Clinical Pharmacology (IUPHAR) and the British Pharmacological Society (BPS). As previously described, our unique model of content selection and quality control is based on 96 target-class subcommittees comprising 512 scientists collaborating with in-house curators. This update describes content expansion, new features and interoperability improvements introduced in the 10 releases since August 2015. Our relationship matrix now describes ∼9000 ligands, ∼15 000 binding constants, ∼6000 papers and ∼1700 human proteins. As an important addition, we also introduce our newly funded project for the Guide to IMMUNOPHARMACOLOGY (GtoImmuPdb, www.guidetoimmunopharmacology.org). This has been 'forked' from the well-established GtoPdb data model and expanded into new types of data related to the immune system and inflammatory processes. This includes new ligands, targets, pathways, cell types and diseases for which we are recruiting new IUPHAR expert committees. Designed as an immunopharmacological gateway, it also has an emphasis on potential therapeutic interventions.


Assuntos
Bases de Dados de Produtos Farmacêuticos , Fenômenos do Sistema Imunológico/efeitos dos fármacos , Sistema Imunitário/efeitos dos fármacos , Animais , Humanos , Doenças do Sistema Imunitário/tratamento farmacológico , Ligantes , Farmacologia , Proteínas/efeitos dos fármacos
19.
Brain Neurosci Adv ; 2: 2398212818783908, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-32166144

RESUMO

Endocannabinoids have been identified to have roles in numerous physiological and pathological processes. Largely due to the association of the effects of Cannabis administration on mental states, the CNS impact of the endocannabinoid system has been the most intensively studied. Here, we provide a brief summary of the endocannabinoid system, comprising the receptors and the multiple endogenous lipid derivatives which activate them, as well as the enzymes which control the levels of these lipid derivatives. We identify pharmacological tools which may be used to interrogate the endocannabinoid system, as well as current and future options to exploit the system in the clinic.

20.
Adv Pharmacol ; 80: 223-247, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-28826536

RESUMO

Of the druggable group of G protein-coupled receptors in the human genome, a number remain which have yet to be paired with an endogenous ligand-orphan GPCRs. Among these 100 or so entities, 3 have been linked to the cannabinoid system. GPR18, GPR55, and GPR119 exhibit limited sequence homology with the established CB1 and CB2 cannabinoid receptors. However, the pharmacology of these orphan receptors displays overlap with CB1 and CB2 receptors, particularly for GPR18 and GPR55. The linking of GPR119 to the cannabinoid receptors is less convincing and emanates from structural similarities of endogenous ligands active at these GPCRs, but which do not cross-react. This review describes the evidence for describing these orphan GPCRs as cannabinoid receptor-like receptors.


Assuntos
Receptores Nucleares Órfãos/metabolismo , Receptores de Canabinoides/metabolismo , Animais , Canabinoides/química , Canabinoides/metabolismo , Humanos , Ligantes , Filogenia , Receptores de Canabinoides/genética , Transdução de Sinais
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