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Slow conformational...
Slow conformational dynamics of the human A(2A) adenosine receptor are temporally ordered
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- Wei, Shushu (author)
- Univ Tennessee, Coll Arts & Sci, Dept Biochem & Cellular & Mol Biol, 1311 Cumberland Ave, Knoxville, TN 37932 USA.
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- Thakur, Naveen (author)
- Univ Florida, Coll Liberal Arts & Sci, Dept Chem, 126 Sisler Hall, Gainesville, FL 32611 USA.
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- Ray, Arka P. (author)
- Univ Florida, Coll Liberal Arts & Sci, Dept Chem, 126 Sisler Hall, Gainesville, FL 32611 USA.
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- Jin, Beining (author)
- Univ Florida, Coll Liberal Arts & Sci, Dept Chem, 126 Sisler Hall, Gainesville, FL 32611 USA.
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- Obeng, Samuel (author)
- Univ Florida, Coll Pharm, Dept Pharmacodynam, Gainesville, FL 32610 USA.;Univ Florida, Coll Pharm, Dept Med Chem, Gainesville, FL 32610 USA.
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- McCurdy, Christopher R. (author)
- Univ Florida, Coll Pharm, Dept Med Chem, Gainesville, FL 32610 USA.;Univ Florida, Clin & Translat Sci Inst, Translat Drug Dev Core, Gainesville, FL 32610 USA.
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- McMahon, Lance R. (author)
- Univ Florida, Coll Pharm, Dept Pharmacodynam, Gainesville, FL 32610 USA.
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- Gutiérrez-de-Terán, Hugo (author)
- Uppsala universitet,Institutionen för cell- och molekylärbiologi
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- Eddy, Matthew T. (author)
- Univ Florida, Coll Liberal Arts & Sci, Dept Chem, 126 Sisler Hall, Gainesville, FL 32611 USA.
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- Lamichhane, Rajan (author)
- Univ Tennessee, Coll Arts & Sci, Dept Biochem & Cellular & Mol Biol, 1311 Cumberland Ave, Knoxville, TN 37932 USA.
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Univ Tennessee, Coll Arts & Sci, Dept Biochem & Cellular & Mol Biol, 1311 Cumberland Ave, Knoxville, TN 37932 USA Univ Florida, Coll Liberal Arts & Sci, Dept Chem, 126 Sisler Hall, Gainesville, FL 32611 USA. (creator_code:org_t)
- Elsevier, 2022
- 2022
- English.
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In: Structure. - : Elsevier. - 0969-2126 .- 1878-4186. ; 30:3, s. 329-
- Related links:
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http://www.cell.com/...
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Subject headings
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- A more complete depiction of protein energy landscapes includes the identification of different function related conformational states and the determination of the pathways connecting them. We used total internal reflection fluorescence (TIRF) imaging to investigate the conformational dynamics of the human A(2A) adenosine receptor (A(2A)AR), a class A G protein-coupled receptor (GPCR), at the single-molecule level. Slow, reversible conformational exchange was observed among three different fluorescence emission states populated for agonist-bound A(2A)AR. Transitions among these states predominantly occurred in a specific order, and exchange between inactive and active-like conformations proceeded through an intermediate state. Models derived from molecular dynamics simulations with available A(2A)AR structures rationalized the relative fluorescence emission intensities for the highest and lowest emission states but not the transition state. This suggests that the functionally critical intermediate state required to achieve activation is not currently visualized among available A(2A)AR structures.
Subject headings
- NATURVETENSKAP -- Biologi -- Biokemi och molekylärbiologi (hsv//swe)
- NATURAL SCIENCES -- Biological Sciences -- Biochemistry and Molecular Biology (hsv//eng)
- NATURVETENSKAP -- Biologi -- Biofysik (hsv//swe)
- NATURAL SCIENCES -- Biological Sciences -- Biophysics (hsv//eng)
Publication and Content Type
- ref (subject category)
- art (subject category)
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