The kinetics of glucocorticoid binding to the soluble specific binding protein of mouse fibroblasts
The kinetics of binding of glucocorticoids to the soluble, specific binding protein of mouse fibroblasts has been examined. The rate at which both potent and weak glucocorticoids achieve binding equilibrium is very slow. Second order rate constants of association range from 3 times 10-5 M- minus 1 m...
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| Veröffentlicht in: | The Journal of biological chemistry 1975-06, Vol.250 (12), p.4584-4591 |
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| container_title | The Journal of biological chemistry |
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| creator | Pratt, W B Kaine, J L Pratt, D V |
| description | The kinetics of binding of glucocorticoids to the soluble, specific binding protein of mouse fibroblasts has been examined.
The rate at which both potent and weak glucocorticoids achieve binding equilibrium is very slow. Second order rate constants
of association range from 3 times 10-5 M- minus 1 min- minus 1 for cortisol to 6.7 times 10-5 M- minus 1 min- minus 1 for
triamcinolone acetonide. Studies of the rates of binding at high steroid concentrations suggest that the slow rate of binding
may be explained by a two-step mechanism. Active glucocorticoids, regardless of their potency, bind initially in a rapid manner
to form a weak complex with the binding protein. The dissociation constant for the weak binding reaction is 0.87 times 10-
minus 7 M for triamcinolone acetonide and 2.4 times 10- minus 7 M for cortisol. The weak binding complex becomes converted
slowly to a tight complex. The first order rate constants for this conversion and the rate constants of dissociation from
the tight complex have been determined for cortisol, dexamethasone and triamcinolone acetonide. The binding affinity of steroids
of different biological potency is correlated with their rate of dissociation from this second tight binding state. |
| doi_str_mv | 10.1016/s0021-9258(19)41342-2 |
| format | Article |
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The rate at which both potent and weak glucocorticoids achieve binding equilibrium is very slow. Second order rate constants
of association range from 3 times 10-5 M- minus 1 min- minus 1 for cortisol to 6.7 times 10-5 M- minus 1 min- minus 1 for
triamcinolone acetonide. Studies of the rates of binding at high steroid concentrations suggest that the slow rate of binding
may be explained by a two-step mechanism. Active glucocorticoids, regardless of their potency, bind initially in a rapid manner
to form a weak complex with the binding protein. The dissociation constant for the weak binding reaction is 0.87 times 10-
minus 7 M for triamcinolone acetonide and 2.4 times 10- minus 7 M for cortisol. The weak binding complex becomes converted
slowly to a tight complex. The first order rate constants for this conversion and the rate constants of dissociation from
the tight complex have been determined for cortisol, dexamethasone and triamcinolone acetonide. The binding affinity of steroids
of different biological potency is correlated with their rate of dissociation from this second tight binding state.</description><identifier>ISSN: 0021-9258</identifier><identifier>EISSN: 1083-351X</identifier><identifier>DOI: 10.1016/s0021-9258(19)41342-2</identifier><identifier>PMID: 166997</identifier><language>eng</language><publisher>United States: American Society for Biochemistry and Molecular Biology</publisher><subject>Animals ; Binding Sites ; Cell Line ; Dexamethasone - metabolism ; Fibroblasts - metabolism ; Hydrocortisone - metabolism ; Kinetics ; L Cells - metabolism ; Mathematics ; Mice ; Protein Binding ; Proteins - metabolism ; Receptors, Cell Surface ; Receptors, Drug ; Time Factors ; Triamcinolone Acetonide - metabolism</subject><ispartof>The Journal of biological chemistry, 1975-06, Vol.250 (12), p.4584-4591</ispartof><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c444t-7f576616a140d6160cd5627b175aff5f3063d37d54ad87e77d3941fc6c0922203</citedby><cites>FETCH-LOGICAL-c444t-7f576616a140d6160cd5627b175aff5f3063d37d54ad87e77d3941fc6c0922203</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27924,27925</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/166997$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Pratt, W B</creatorcontrib><creatorcontrib>Kaine, J L</creatorcontrib><creatorcontrib>Pratt, D V</creatorcontrib><title>The kinetics of glucocorticoid binding to the soluble specific binding protein of mouse fibroblasts</title><title>The Journal of biological chemistry</title><addtitle>J Biol Chem</addtitle><description>The kinetics of binding of glucocorticoids to the soluble, specific binding protein of mouse fibroblasts has been examined.
The rate at which both potent and weak glucocorticoids achieve binding equilibrium is very slow. Second order rate constants
of association range from 3 times 10-5 M- minus 1 min- minus 1 for cortisol to 6.7 times 10-5 M- minus 1 min- minus 1 for
triamcinolone acetonide. Studies of the rates of binding at high steroid concentrations suggest that the slow rate of binding
may be explained by a two-step mechanism. Active glucocorticoids, regardless of their potency, bind initially in a rapid manner
to form a weak complex with the binding protein. The dissociation constant for the weak binding reaction is 0.87 times 10-
minus 7 M for triamcinolone acetonide and 2.4 times 10- minus 7 M for cortisol. The weak binding complex becomes converted
slowly to a tight complex. The first order rate constants for this conversion and the rate constants of dissociation from
the tight complex have been determined for cortisol, dexamethasone and triamcinolone acetonide. The binding affinity of steroids
of different biological potency is correlated with their rate of dissociation from this second tight binding state.</description><subject>Animals</subject><subject>Binding Sites</subject><subject>Cell Line</subject><subject>Dexamethasone - metabolism</subject><subject>Fibroblasts - metabolism</subject><subject>Hydrocortisone - metabolism</subject><subject>Kinetics</subject><subject>L Cells - metabolism</subject><subject>Mathematics</subject><subject>Mice</subject><subject>Protein Binding</subject><subject>Proteins - metabolism</subject><subject>Receptors, Cell Surface</subject><subject>Receptors, Drug</subject><subject>Time Factors</subject><subject>Triamcinolone Acetonide - metabolism</subject><issn>0021-9258</issn><issn>1083-351X</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1975</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpFkEtLxDAUhYP4Gkf_gUJBEF1U8067lMEXDLhwBHehzWMabZuxaRH_venMMGZzCOfccy8fABcI3iKI-F2AEKM0xyy7RvkNRYTiFO-BCYIZSQlDH_tgsoscg5MQPmF8NEdH4BBxnudiAtSiMsmXa03vVEi8TZb1oLzyXfx7p5PStdq1y6T3SR-TwddDWUddGeWsUzt_1fneuHZsaPwQTGJd2fmyLkIfTsGBLepgzrY6Be-PD4vZczp_fXqZ3c9TRSntU2GZ4BzxAlGoo0KlGceiRIIV1jJLICeaCM1ooTNhhNAkp8gqrmCOMYZkCq42vfGY78GEXjYuKFPXRWviTTLDWUZhhmOQbYKq8yF0xspV55qi-5UIypGtfBvByRGcRLlcs5Xj3Pl2wVA2Rv9PrWFG-3JjV25Z_bjOyNJ5VZlGYhZ7saQso-QPGfmA2w</recordid><startdate>19750625</startdate><enddate>19750625</enddate><creator>Pratt, W B</creator><creator>Kaine, J L</creator><creator>Pratt, D V</creator><general>American Society for Biochemistry and Molecular Biology</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>19750625</creationdate><title>The kinetics of glucocorticoid binding to the soluble specific binding protein of mouse fibroblasts</title><author>Pratt, W B ; Kaine, J L ; Pratt, D V</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c444t-7f576616a140d6160cd5627b175aff5f3063d37d54ad87e77d3941fc6c0922203</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1975</creationdate><topic>Animals</topic><topic>Binding Sites</topic><topic>Cell Line</topic><topic>Dexamethasone - metabolism</topic><topic>Fibroblasts - metabolism</topic><topic>Hydrocortisone - metabolism</topic><topic>Kinetics</topic><topic>L Cells - metabolism</topic><topic>Mathematics</topic><topic>Mice</topic><topic>Protein Binding</topic><topic>Proteins - metabolism</topic><topic>Receptors, Cell Surface</topic><topic>Receptors, Drug</topic><topic>Time Factors</topic><topic>Triamcinolone Acetonide - metabolism</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Pratt, W B</creatorcontrib><creatorcontrib>Kaine, J L</creatorcontrib><creatorcontrib>Pratt, D V</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>The Journal of biological chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Pratt, W B</au><au>Kaine, J L</au><au>Pratt, D V</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>The kinetics of glucocorticoid binding to the soluble specific binding protein of mouse fibroblasts</atitle><jtitle>The Journal of biological chemistry</jtitle><addtitle>J Biol Chem</addtitle><date>1975-06-25</date><risdate>1975</risdate><volume>250</volume><issue>12</issue><spage>4584</spage><epage>4591</epage><pages>4584-4591</pages><issn>0021-9258</issn><eissn>1083-351X</eissn><abstract>The kinetics of binding of glucocorticoids to the soluble, specific binding protein of mouse fibroblasts has been examined.
The rate at which both potent and weak glucocorticoids achieve binding equilibrium is very slow. Second order rate constants
of association range from 3 times 10-5 M- minus 1 min- minus 1 for cortisol to 6.7 times 10-5 M- minus 1 min- minus 1 for
triamcinolone acetonide. Studies of the rates of binding at high steroid concentrations suggest that the slow rate of binding
may be explained by a two-step mechanism. Active glucocorticoids, regardless of their potency, bind initially in a rapid manner
to form a weak complex with the binding protein. The dissociation constant for the weak binding reaction is 0.87 times 10-
minus 7 M for triamcinolone acetonide and 2.4 times 10- minus 7 M for cortisol. The weak binding complex becomes converted
slowly to a tight complex. The first order rate constants for this conversion and the rate constants of dissociation from
the tight complex have been determined for cortisol, dexamethasone and triamcinolone acetonide. The binding affinity of steroids
of different biological potency is correlated with their rate of dissociation from this second tight binding state.</abstract><cop>United States</cop><pub>American Society for Biochemistry and Molecular Biology</pub><pmid>166997</pmid><doi>10.1016/s0021-9258(19)41342-2</doi><tpages>8</tpages><oa>free_for_read</oa></addata></record> |
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| ispartof | The Journal of biological chemistry, 1975-06, Vol.250 (12), p.4584-4591 |
| issn | 0021-9258 1083-351X |
| language | eng |
| recordid | cdi_proquest_miscellaneous_82884082 |
| source | MEDLINE; EZB-FREE-00999 freely available EZB journals; Alma/SFX Local Collection |
| subjects | Animals Binding Sites Cell Line Dexamethasone - metabolism Fibroblasts - metabolism Hydrocortisone - metabolism Kinetics L Cells - metabolism Mathematics Mice Protein Binding Proteins - metabolism Receptors, Cell Surface Receptors, Drug Time Factors Triamcinolone Acetonide - metabolism |
| title | The kinetics of glucocorticoid binding to the soluble specific binding protein of mouse fibroblasts |
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