Alexander Berchansky at 10:53, 5 February 2023

Alexander Berchansky — Sun, 05 Feb 2023 10:53:31 GMT

←Older revision		Revision as of 10:53, 5 February 2023
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	<StructureSection load='' size='350' side='right' caption='Structure of human FXR ligand-binding domain (magenta) complex with non-steroidal agonist, nuclear receptor coactivator 1 peptide (cyan) and sulfate ions (PDB entry [[3ruu]])' scene='54/545859/Cv/1'>		<StructureSection load='' size='350' side='right' caption='Structure of human FXR ligand-binding domain (magenta) complex with non-steroidal agonist, nuclear receptor coactivator 1 peptide (cyan) and sulfate ions (PDB entry [[3ruu]])' scene='54/545859/Cv/1'>
-	~~'''Under construction!!!'''~~	+
	A ligand that can bind to and alter the function of the receptor that triggers a physiological response is called a receptor '''agonist'''.		A ligand that can bind to and alter the function of the receptor that triggers a physiological response is called a receptor '''agonist'''.

Alexander Berchansky at 13:11, 19 September 2021

Alexander Berchansky — Sun, 19 Sep 2021 13:11:57 GMT

←Older revision		Revision as of 13:11, 19 September 2021
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	<StructureSection load='' size='350' side='right' caption='Structure of human FXR ligand-binding domain (magenta) complex with non-steroidal agonist, nuclear receptor coactivator 1 peptide (cyan) and sulfate ions (PDB entry [[3ruu]])' scene='54/545859/Cv/1'>		<StructureSection load='' size='350' side='right' caption='Structure of human FXR ligand-binding domain (magenta) complex with non-steroidal agonist, nuclear receptor coactivator 1 peptide (cyan) and sulfate ions (PDB entry [[3ruu]])' scene='54/545859/Cv/1'>
	'''Under construction!!!'''		'''Under construction!!!'''
		+	A ligand that can bind to and alter the function of the receptor that triggers a physiological response is called a receptor '''agonist'''.
		+
		+	'''Endogenous agonists:'''
		+	*[[Hormones]]
		+	*[[Neurotransmitters]]
		+	In general, receptors for small molecule neurotransmitters such as serotonin will have only one '''endogenous agonist''', but often have many different receptor subtypes (''e.g.'' 13 [[5-hydroxytryptamine receptor\|different receptors for serotonin]]). On the other hand, neuropeptide receptors (e.g. [[opioid receptors]]) tend to have fewer subtypes, but may have several different endogenous agonists. This allows for a high degree of complexity in the body's signalling system, with different tissues often showing quite distinct responses to a particular ligand.
		+
		+	'''Exogenous agonists''' - [[Drugs]].
		+
		+	'''Full agonists''' bind to and activate a receptor with the maximum response that an agonist can elicit at the receptor. One example of a drug that can act as a full agonist is isoproterenol, which mimics the action of adrenaline at β-adrenoreceptors (see [[UMass Chem 423 Student Projects 2011-1#Beta-1 Adrenergic GPCR\|Beta-1 Adrenergic receptor]]. Another example is morphine, which mimics the actions of endorphins at μ-opioid receptors. See
		+	*[[Mu Opioid Receptor Bound to a Morphinan Antagonist]]
		+	*[[μ Opioid Receptors]]
		+	*[[Mu Opioid Receptor]].
		+
		+	'''Co-agonist''' works with other co-agonists to produce the desired effect together. NMDA receptor (see [[Ionotropic Glutamate Receptors]]) activation requires the binding of both glutamate, glycine and D-serine co-agonists. Calcium can also act as a co-agonist at the [[IP3 receptor]].
		+
		+	'''Selective agonist''' is selective for a specific type of receptor. E.g. buspirone is a selective agonist for serotonin 5-HT1A (see [[5-hydroxytryptamine receptor]].
		+
		+	'''Partial agonists''' (such as buspirone, aripiprazole, buprenorphine, or norclozapine) also bind and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist, even at maximal receptor occupancy. Agents like buprenorphine are used to treat opiate dependence for this reason, as they produce milder effects on the opioid receptor (see [[μ Opioid Receptors]]) with lower dependence and abuse potential. Examples of ligands activating [[PPAR-gamma\|peroxisome proliferator-activated receptor gamma]] as partial agonists are honokiol and falcarindiol.
		+
		+	'''Inverse agonist''' is an agent that binds to the same receptor binding-site as an agonist for that receptor and inhibits the constitutive activity of the receptor. The opioid antagonists naloxone and naltrexone are also partial inverse agonists at [[μ Opioid Receptors]]. Nearly all antihistamines acting at [[Histamine H1 receptor\|H1 receptors]] and H2 receptors have been shown to be inverse agonists. The beta blockers carvedilol and bucindolol have been shown to be low level inverse agonists at [[Beta-2 adrenergic receptor\|beta adrenoreceptors]].
		+
		+	'''Superagonist''' is a term used by some to identify a compound that is capable of producing a greater response than the endogenous agonist for the target receptor. It might be argued that the endogenous agonist is simply a partial agonist in that tissue. <scene name='56/562378/3a3z/1'>The synthetic analogue (20S,23S)-epoxymethano-1alpha,25-dihydroxyvitamin D(3) (2a)</scene> acts as a 1alpha,25(OH)(2)D(3) '''superagonist''' of Vitamin D on [[Vitamin D receptor]] and exhibits both antiproliferative and prodifferentiating properties ''in vitro''.
		+
		+	A '''physiological agonist''' is a substance that creates the same bodily responses but does not bind to the same receptor.
		+
		+	'''Examples of agonists:'''
		+	*<scene name='56/562378/3a3z/1'>The synthetic analogue (20S,23S)-epoxymethano-1alpha,25-dihydroxyvitamin D(3) (2a)</scene> acts as a 1alpha,25(OH)(2)D(3) '''superagonist''' of Vitamin D on [[Vitamin D receptor]] and exhibits both antiproliferative and prodifferentiating properties ''in vitro''.
		+	*<scene name='50/508426/Cvcv/6'>Agonist inositol hexakisphosphate binding site</scene> in [[Transport inhibitor response 1]] ([[3c6o]]). Water molecules are shown as red spheres.
		+	*<scene name='54/545859/Cv/3'>Structure</scene> of human [[Bile acid receptor]] ligand-binding domain (deeppink) complex with non-steroidal agonist, nuclear receptor coactivator 1 peptide (cyan) and sulfate ions (PDB entry [[3ruu]]). <ref>PMID:21890356</ref>

	</StructureSection>		</StructureSection>
	== References ==		== References ==
	<references/>		<references/>

Alexander Berchansky: New page: '''Under construction!!!'''

</StructureSection>
== References ==
<references/>

Agonist - Revision history

Alexander Berchansky at 10:53, 5 February 2023

Alexander Berchansky at 13:11, 19 September 2021

Alexander Berchansky: New page: '''Under construction!!!''' </StructureSection> == References == <references/>

Alexander Berchansky: New page: '''Under construction!!!'''

</StructureSection>
== References ==
<references/>