Sandbox 121: Difference between revisions
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<applet load='3P0G' size=' | <applet load='3P0G' size='300' frame='true' align='right' scene='Sandbox_121/B2ar_struc/1' caption='B₂AR Active'/> | ||
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There are 3 extracellular loops and 3 intracellular loops. The <scene name='Sandbox_121/B2ar_struc/6'>binding pocket</scene> is located to the center of the extracellular surface. | There are 3 extracellular loops and 3 intracellular loops. The <scene name='Sandbox_121/B2ar_struc/6'>binding pocket</scene> is located to the center of the extracellular surface. | ||
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==='''Ligands'''=== | ==='''Ligands'''=== | ||
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A ligand that is an antagonist actually has no effect on the basal activity of the receptor. An antagonist simply sterically blocks the receptor so that no other ligand can bind. Their activity would be considered baseline. Antagonists for the adrenergic receptors are commonly called Beta Blockers. Although Beta Blockers are not prescribed for B₂AR, they are frequently prescribed for Beta-1 Adrenergic Receptors in people with heart conditions. | A ligand that is an antagonist actually has no effect on the basal activity of the receptor. An antagonist simply sterically blocks the receptor so that no other ligand can bind. Their activity would be considered baseline. Antagonists for the adrenergic receptors are commonly called Beta Blockers. Although Beta Blockers are not prescribed for B₂AR, they are frequently prescribed for Beta-1 Adrenergic Receptors in people with heart conditions. | ||
Isoproterenol contains an isopropyl amine group and a catechol group. | {| border="1" cellpadding="2" | ||
! scope="col" width="50" | Name | |||
! scope="col" width="175" | Description | |||
! scope="col" width="350" | Chemical Structure | |||
! scope="col" width="350" | Photo | |||
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| Isoproterenol || Isoproterenol is an agonist that is structurally similar to NE and readily binds to B2AR with high affinity. Isoproterenol contains an isopropyl amine group and a catechol group. || [[Image:B2AR-Isoproterenol-Structure.JPG|thumb|center|alt= Alt text| |350px]] || [[Image:Isoproterenol-Picture.JPG|thumb|center|alt= Alt text| |300px]] | |||
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| BI-167107 || The active state of B2AR was crystallized using BI-1671071 . Although it is not a catecholamine, it is a full agonist. || [[Image:B2AR-BI-167107-Structure.JPG|thumb|center|alt= Alt text| |350px]] || [[Image:B2AR-BI-167107-Picture.JPG|thumb|center|alt= Alt text| |300px]] | |||
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| Carazolol || Carazolol is an inverse agonist designed to inhibit B₂AR. Carazolol contains a propylamine and a carbazole group. || [[Image:B2AR-Carazolol-structure.JPG|thumb|center|alt= Alt text| |300px]] || [[Image:B2AR-Carazolol-Picture.JPG|thumb|center|alt= Alt text| |300px]] | |||
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===='''Comparison of the Inverse Agonist and the Agonist'''==== | ===='''Comparison of the Inverse Agonist and the Agonist'''==== | ||
