Beta-2 Adrenergic Receptor: Difference between revisions
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<StructureSection load=' | <StructureSection load='' size='490' side='right' caption='Solved Structure of a Beta 2-Adrenergic Receptor, ([[2rh1]])' scene='Beta-2_Adrenergic_Receptor/Opening/1' > | ||
[[Image:B2ar Image3.png|200px|left]] [[Beta-2 Adrenergic Receptor]]'''s''' (B2ARs) are a type of [[G protein-coupled receptor|G Protein-Coupled Receptor (GPCR)]]. GPCRs are the largest family of integral membrane proteins in the human body with over 1000 unique Isoforms. B2AR is activated by hormone ligands like adrenaline (epinephrine) and noradrenaline and plays a critical role in cardiovascular and pulmonary physiology. Binding of adrenaline by B2AR causes a sympathetic nervous system response like the well-known “fight or flight response”, resulting in an increased heart rate, pupil dilation, rapid energy mobilization and diversion of blood to skeletal muscle. More precisely, upon binding a ligand, B2AR activates [[Adenylyl cyclase]] through interaction with B2ARs C-terminus. Adenylyl cyclase subsequently converts ATP into cAMP, which functions as a downstream signaling molecule activating effectors like cAMP-dependent protein kinases, resulting in various bodily responses.<ref name="Witter"/> | [[Image:B2ar Image3.png|200px|left]] [[Beta-2 Adrenergic Receptor]]'''s''' (B2ARs) are a type of [[G protein-coupled receptor|G Protein-Coupled Receptor (GPCR)]]. GPCRs are the largest family of integral membrane proteins in the human body with over 1000 unique Isoforms. B2AR is activated by hormone ligands like adrenaline (epinephrine) and noradrenaline and plays a critical role in cardiovascular and pulmonary physiology. Binding of adrenaline by B2AR causes a sympathetic nervous system response like the well-known “fight or flight response”, resulting in an increased heart rate, pupil dilation, rapid energy mobilization and diversion of blood to skeletal muscle. More precisely, upon binding a ligand, B2AR activates [[Adenylyl cyclase]] through interaction with B2ARs C-terminus. Adenylyl cyclase subsequently converts ATP into cAMP, which functions as a downstream signaling molecule activating effectors like cAMP-dependent protein kinases, resulting in various bodily responses.<ref name="Witter"/> | ||
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====Pharmaceutical Implications==== | ====Pharmaceutical Implications==== | ||
Although activation of B2AR upon ligand binding is not fully understood, a recently solved structure of Beta 1 Adrenergic Receptors offers clues. Agonists of B1ARs <scene name='Beta-2_Adrenergic_Receptor/Disrupted/1'>disrupt the interaction</scene> ([[2y02]]) between Val 172 and Ser 215, eliminating a key interaction between helices four and five. Since mutation to Val 172 is known to reduce basal activity, it is likely that the agonists interference of Val 172 has a similar affect.<ref>PMID: 21228877</ref> The class of [[Pharmaceutical Drugs|pharmaceutical drugs]] known as the “beta blockers” are antagonists of B2AR. They diminish the effects of adrenaline, slowing the heart rhythm and reducing blood pressure. B2AR Agonists serve a completely different purpose. These molecules which mimic native ligands of B2AR cause smooth muscle relaxation, bronchial passage dilation, vasodilation and rapid release of insulin. These compounds are used to treat asthma, and include the well-known Albuterol and Terbutaline.<ref>PMID: 20692524</ref> | Although activation of B2AR upon ligand binding is not fully understood, a recently solved structure of Beta 1 Adrenergic Receptors offers clues. Agonists of B1ARs <scene name='Beta-2_Adrenergic_Receptor/Disrupted/1'>disrupt the interaction</scene> ([[2y02]]) between Val 172 and Ser 215, eliminating a key interaction between helices four and five. Since mutation to Val 172 is known to reduce basal activity, it is likely that the agonists interference of Val 172 has a similar affect.<ref>PMID: 21228877</ref> The class of [[Pharmaceutical Drugs|pharmaceutical drugs]] known as the “beta blockers” are antagonists of B2AR. They diminish the effects of adrenaline, slowing the heart rhythm and reducing blood pressure. B2AR Agonists serve a completely different purpose. These molecules which mimic native ligands of B2AR cause smooth muscle relaxation, bronchial passage dilation, vasodilation and rapid release of insulin. These compounds are used to treat asthma, and include the well-known Albuterol and Terbutaline.<ref>PMID: 20692524</ref> | ||
See also [[Beta-2 receptors agonists]]. | |||
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==See Also== | ==See Also== | ||
* [[G protein-coupled receptor]] | * [[G protein-coupled receptor]] | ||
*[[Receptor]] | |||
*[[Transmembrane (cell surface) receptors]] | |||
* [[Adrenergic receptor]] | * [[Adrenergic receptor]] | ||
* [[Group:SMART:A Physical Model of the β2-Adrenergic Receptor|The Madison West High School 2008 SMART Team's Page on the β-2 adrenergic receptor]] | * [[Group:SMART:A Physical Model of the β2-Adrenergic Receptor|The Madison West High School 2008 SMART Team's Page on the β-2 adrenergic receptor]] | ||