2om9

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{{STRUCTURE_2om9| PDB=2om9 | SCENE= }}
{{STRUCTURE_2om9| PDB=2om9 | SCENE= }}
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'''Ajulemic acid, a synthetic cannabinoid bound to PPAR gamma'''
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===Ajulemic acid, a synthetic cannabinoid bound to PPAR gamma===
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==Overview==
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Ajulemic acid (AJA) is a synthetic analog of THC-11-oic acid, a metabolite of tetrahydrocannabinol (THC), the major active ingredient of the recreational drug marijuana derived from the plant Cannabis sativa. AJA has potent analgesic and anti-inflammatory activity in vivo, but without the psychotropic action of THC. However, its precise mechanism of action remains unknown. Biochemical studies indicate that AJA binds directly and selectively to the isotype gamma of the peroxisome proliferator-activated receptor (PPARgamma) suggesting that this may be a pharmacologically relevant receptor for this compound and a potential target for drug development in the treatment of pain and inflammation. Here, we report the crystal structure of the ligand binding domain of the gamma isotype of human PPAR in complex with ajulemic acid, determined at 2.8-A resolution. Our results show a binding mode that is compatible with other known partial agonists of PPAR, explaining their moderate activation of the receptor, as well as the structural basis for isotype selectivity, as observed previously in vitro. The structure also provides clues to the understanding of partial agonism itself, suggesting a rational approach to the design of molecules capable of activating the receptor at levels that avoid undesirable side effects.
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(as it appears on PubMed at http://www.pubmed.gov), where 17462987 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17462987}}
==About this Structure==
==About this Structure==
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[[Category: Partial agonist]]
[[Category: Partial agonist]]
[[Category: Ppar gamma]]
[[Category: Ppar gamma]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 11:12:07 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 23:28:36 2008''

Revision as of 20:28, 28 July 2008

Image:2om9.png

Template:STRUCTURE 2om9

Ajulemic acid, a synthetic cannabinoid bound to PPAR gamma

Template:ABSTRACT PUBMED 17462987

About this Structure

2OM9 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Ajulemic acid, a synthetic nonpsychoactive cannabinoid acid, bound to the ligand binding domain of the human peroxisome proliferator-activated receptor gamma., Ambrosio AL, Dias SM, Polikarpov I, Zurier RB, Burstein SH, Garratt RC, J Biol Chem. 2007 Jun 22;282(25):18625-33. Epub 2007 Apr 26. PMID:17462987

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