IUPHAR DATABASE

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Search Facility

The search facility on the sidebar has simple and advanced modes. Simple mode is shown when the page is first loaded; clicking on "Advanced Search" will switch to advanced mode. In simple mode, all types of annotation are searched. In advanced mode, you can choose the types of annotation to search.

Select the database you wish to search using the radio buttons labelled 'GPCR' and 'VGIC'.

In advanced mode:

Select the field from the drop down list that you wish to search.
Type the search term into the text box and press search.

To search more than one field:

Press the control button on your keyboard and select the required fields from the drop down list.
To search the entire database select general. (This is equivalent to selecting all the search fields in the list)

Selecting two fields produces a logical 'OR'.
For example in Figure 1 the search will return all the receptor distributions that contain the word 'Brain' and it will return all the tissue functions that contain the word 'Brain'.

GPCR VGIC

Figure 1

Figure 2

If the search term contains more than one word the following options are available:

Separate the words with spaces: In Figure 2 the search will only return the functional assays that contain both the words 'cAMP' and 'Human'.
Enclose inside speech marks: In Figure 3 the search will only return the functional assays that contain the phase 'cAMP accumulation'.
This can be useful for phases such as 'RT-PCR', 'HEK 293' etc.
Combining the two examples above: In Figure 4 the search will only return the functional assays that contain the phase 'cAMP accumulation' and 'Human'.


GPCR VGIC

GPCR VGIC

Figure 3

Figure 4

GPCR Database

Receptor - The NC-IUPHAR recommended nomenclature for a structurally and operationally distinct receptor in a given family.

Previous Names - Alternative names that exist in the literature, but are no longer the recommended nomenclature.

Database Links - Links to the relevant pages in the Entrez Gene, Homologene, UniGene, Genecard and OMIM databases.

Structural Information - For human, mouse and rat receptors the following data is displayed:

Column	Definition
Transmembrane domains (TM)	The number of times the receptor polypeptide passes through the cell membrane.
Amino acids (AA)	The number of amino acids which make up the receptor protein
Accession number	The UniProtKB/Swiss-Prot accession number which, if highlighted in blue, links to the Swiss-Prot database
Chromosomal location	The genetic location of the receptor.
Gene Name	The name of the gene that codes for the receptor which, if highlighted in blue, links to the HGNC, MGI or RGD database.

Functional Assay - Details of pharmacological test systems (whole tissues or isolated cells) in which a response can be firmly attributed to the function of a defined receptor type

Ligands - Ligands are categorised as agonists, antagonists or allosteric regulators. The column headings or icons in the ligand table are described below:

Icon/Table heading	Definition
	Indicates that the ligand is radioactive.
	Indicates that the ligand is endogenous in the species of the receptor under test.
	Indicates that the ligand also binds to other receptors in the database. Clicking on this icon displays these receptors as well as the ligand's potency at each receptor.
	A link to the PubChem database, where the structure of the ligand can be viewed.
Hs, Mm, Rn	Indicates the species of the receptor and NOT the species of the ligand.
Ligand	The name of the ligand which, if highlighted in blue, can be clicked on to view alternative names for the ligand.
Action	This indicates how the ligand binds to the receptor (see the terms and symbols document for a definition of the terms).
Affinity	A measure of how strongly the ligand binds to the receptor. In cases where no binding data is available functional data may be used.
Units	The units used to measure the ligand's binding to the receptor.

The ligands can be sorted in alphabetical order or by action, affinity or unit by clicking on the column header.

Primary and Secondary Transduction Mechanisms - The preferred primary and secondary receptor signalling pathways or mechanisms, where established.

Receptor Distribution - Central and peripheral distribution of the receptor (and the identifying techniques).

Tissue Function - The physiological response mediated by the receptor if established in whole tissue, preferably in vivo.

Physical Consequences of Altering Gene Expression - Important physiological differences observed as a result of modifying expression levels (e.g. knockouts).

Biologiocally Important Receptor Variants - Details of polymorphisms and post-transcriptional modifications (e.g. splice variation) that influence function.

Ion Channel Database

Voltage-gated ion channels

Receptor - The NC-IUPHAR recommended nomenclature for a structurally and operationally distinct receptor in a given family.

Previous Names - Alternative names that exist in the literature, but are no longer the recommended nomenclature.

Database Links - Links to the relevant pages in the OMIM, GeneCards, Entrez Gene, Homologene and UniGene databases.

Associated and Accessory Proteins - Proteins that interact directly with the receptor either as heteromeric pore-forming subunits, auxiliary subunits or associated proteins.

Structural Information - For human, mouse and rat receptors the following data is displayed:

Column	Definition
Transmembrane domains (TM)	The number of times the receptor polypeptide passes through the cell membrane.
Amino acids (AA)	The number of amino acids which make up the receptor protein
Accession number	The Entrez protein accession number which, if highlighted in blue, links to the Entrez database
Chromosomal location	The genetic location of the receptor.
Gene Name	The name of the gene that codes for the receptor which, if highlighted in blue, links to the HGNC, MGI or RGD database.

If multiple splice variants exist a link to the "Variants" table in the database is displayed rather than the accession number.

Ion Selectivity and Conductance - This table displays relative or absolute conductance data for the receptor on a 'per species' basis.

Voltage Dependence - This table displays the voltages of activation and inactivation and the relevant time constants, where available.

Ligands - Ligands are categorised as activators, pore blockers or gating inhibitors, according to the following definitions:

Activators: Ligands that activate ion channels by binding directly to them, including ligands that cause a change in the voltage dependence of channel gating that favors activation.
Gating Inhibitors: Ligands that inhibit ion channel gating by directly binding to the channels, including ligands that inhibit ion channel activation and those that inhibit ion channel inactivation.
Pore blockers: Ligands that block ion movement through the pore of ion channels.

The column headings or icons in the ligand table are described below:

Icon/Table heading	Definition
	Indicates that the ligand is radioactive.
	Indicates that the ligand is endogenous in the species of the receptor under test.
	Indicates that the ligand also binds to other receptors in the database. Clicking on this icon displays these receptors as well as the ligand's potency at each receptor.
	A link to the PubChem database, where the structure of the ligand can be viewed.
Hs, Mm, Rn	Indicates the species of the receptor and NOT the species of the ligand. '?' indicates that the species was not given in the original publication. Selectivity tables are not shown when the species is unknown.
Ligand	The name of the ligand which, if highlighted in blue, can be clicked on to view alternative names for the ligand.
Affinity	A measure of how strongly the ligand binds to the receptor. In cases where no binding data is available functional data may be used.
Units	The units used to measure the ligand's binding to the receptor.
Concentration range	Where affinity data is not available, the concentration range of ligand used for the study is displayed (in µM).
Holding voltage	The voltage at which the displayed affinity was determined (in mV). 'Physiological' indicates that the experiment was performed in intact cells where voltage could not be determined.

The ligands can be sorted in alphabetical order or by affinity, unit, concentration range or holding voltage by clicking on the column header.

Tissue Distribution - Central and peripheral distribution of the receptor (and the identifying techniques).

Functional Assays - Details of pharmacological test systems (whole tissues or isolated cells) in which a response can be firmly attributed to the function of a defined receptor type

Functions - The physiological response mediated by the receptor if established in whole tissue, preferably in vivo.

Pathophysiology - The pathophysiologies in which the receptor is involved, including, where available, the ligands at the receptor which are of therapeutic use.

Mutations - Details of individual mutations that lead to specific pathophysiology in terms of the change in the amino acid sequence.

Gene Expression and Pathophysiology - The pathophysiology that arises from abnormal gene expression. This may include data from experimental manipulations of gene expression.

Variants - Details of polymorphisms and post-transcriptional modifications (e.g. splice variation) that influence function.

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