Suppressive effect of N-(benzyloxycarbonyl)- l-phenylalanyl- l-tyrosinal on bone resorption in vitro and in vivo
The suppressive effect of N-(benzyloxycarbonyl)- l-phenylalanyl- l-tyrosinal on bone resorption was examined in vitro and in vivo. This synthetic peptidyl aldehyde was found to be a potent and selective cathepsin L inhibitor in our screening for cysteine protease inhibitors. In the pit formation ass...
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| Veröffentlicht in: | European journal of pharmacology 1996-04, Vol.300 (1), p.131-135 |
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| container_title | European journal of pharmacology |
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| creator | Woo, Je-Tae Yamaguchi, Kohji Hayama, Takahiro Kobori, Takeo Sigeizumi, Sanae Sugimoto, Kikuo Kondo, Kiyosi Tsuji, Tomoko Ohba, Yasuo Tagami, Kahori Sumitani, Koji |
| description | The suppressive effect of
N-(benzyloxycarbonyl)-
l-phenylalanyl-
l-tyrosinal on bone resorption was examined in vitro and in vivo. This synthetic peptidyl aldehyde was found to be a potent and selective cathepsin L inhibitor in our screening for cysteine protease inhibitors. In the pit formation assay with unfractionated rat bone cells, 1.5 nM of this compound markedly inhibited parathyroid hormone-stimulated osteoclastic bone resorption. In addition, intraperitoneal administration of this peptidyl aldehyde (2.5–10 mg/kg) for 4 weeks suppressed bone weight loss dose dependently in the ovariectomized mouse, experimental model of osteoporosis. Hydroxyproline measurement of the decalcified femurs from these ovariectomized mice suggested that this compound acts as a bone resorption suppressor through the inhibition of collagen degradation. |
| doi_str_mv | 10.1016/0014-2999(95)00858-6 |
| format | Article |
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N-(benzyloxycarbonyl)-
l-phenylalanyl-
l-tyrosinal on bone resorption was examined in vitro and in vivo. This synthetic peptidyl aldehyde was found to be a potent and selective cathepsin L inhibitor in our screening for cysteine protease inhibitors. In the pit formation assay with unfractionated rat bone cells, 1.5 nM of this compound markedly inhibited parathyroid hormone-stimulated osteoclastic bone resorption. In addition, intraperitoneal administration of this peptidyl aldehyde (2.5–10 mg/kg) for 4 weeks suppressed bone weight loss dose dependently in the ovariectomized mouse, experimental model of osteoporosis. Hydroxyproline measurement of the decalcified femurs from these ovariectomized mice suggested that this compound acts as a bone resorption suppressor through the inhibition of collagen degradation.</description><identifier>ISSN: 0014-2999</identifier><identifier>EISSN: 1879-0712</identifier><identifier>DOI: 10.1016/0014-2999(95)00858-6</identifier><identifier>PMID: 8741178</identifier><identifier>CODEN: EJPHAZ</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>Animals ; Biological and medical sciences ; Bone and Bones - drug effects ; Bone and Bones - metabolism ; Bone resorption ; Bone Resorption - physiopathology ; Bones, joints and connective tissue. Antiinflammatory agents ; Cathepsin L ; Cathepsins - antagonists & inhibitors ; Cysteine Endopeptidases ; Cysteine protease inhibitor ; Cysteine Proteinase Inhibitors - pharmacology ; Dipeptides - pharmacology ; Dipeptidyl aldehyde ; Endopeptidases ; Female ; Humans ; Leucine - analogs & derivatives ; Leucine - pharmacology ; Medical sciences ; Mice ; Ovariectomy ; Pharmacology. Drug treatments ; Rats ; Rats, Sprague-Dawley</subject><ispartof>European journal of pharmacology, 1996-04, Vol.300 (1), p.131-135</ispartof><rights>1996</rights><rights>1996 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c483t-23fc3b66ffa54e12f96baff593a0036173db527702dc3a46f90e9e45fc1672203</citedby><cites>FETCH-LOGICAL-c483t-23fc3b66ffa54e12f96baff593a0036173db527702dc3a46f90e9e45fc1672203</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/0014-2999(95)00858-6$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,778,782,3539,27907,27908,45978</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=3132232$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/8741178$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Woo, Je-Tae</creatorcontrib><creatorcontrib>Yamaguchi, Kohji</creatorcontrib><creatorcontrib>Hayama, Takahiro</creatorcontrib><creatorcontrib>Kobori, Takeo</creatorcontrib><creatorcontrib>Sigeizumi, Sanae</creatorcontrib><creatorcontrib>Sugimoto, Kikuo</creatorcontrib><creatorcontrib>Kondo, Kiyosi</creatorcontrib><creatorcontrib>Tsuji, Tomoko</creatorcontrib><creatorcontrib>Ohba, Yasuo</creatorcontrib><creatorcontrib>Tagami, Kahori</creatorcontrib><creatorcontrib>Sumitani, Koji</creatorcontrib><title>Suppressive effect of N-(benzyloxycarbonyl)- l-phenylalanyl- l-tyrosinal on bone resorption in vitro and in vivo</title><title>European journal of pharmacology</title><addtitle>Eur J Pharmacol</addtitle><description>The suppressive effect of
N-(benzyloxycarbonyl)-
l-phenylalanyl-
l-tyrosinal on bone resorption was examined in vitro and in vivo. This synthetic peptidyl aldehyde was found to be a potent and selective cathepsin L inhibitor in our screening for cysteine protease inhibitors. In the pit formation assay with unfractionated rat bone cells, 1.5 nM of this compound markedly inhibited parathyroid hormone-stimulated osteoclastic bone resorption. In addition, intraperitoneal administration of this peptidyl aldehyde (2.5–10 mg/kg) for 4 weeks suppressed bone weight loss dose dependently in the ovariectomized mouse, experimental model of osteoporosis. Hydroxyproline measurement of the decalcified femurs from these ovariectomized mice suggested that this compound acts as a bone resorption suppressor through the inhibition of collagen degradation.</description><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Bone and Bones - drug effects</subject><subject>Bone and Bones - metabolism</subject><subject>Bone resorption</subject><subject>Bone Resorption - physiopathology</subject><subject>Bones, joints and connective tissue. Antiinflammatory agents</subject><subject>Cathepsin L</subject><subject>Cathepsins - antagonists & inhibitors</subject><subject>Cysteine Endopeptidases</subject><subject>Cysteine protease inhibitor</subject><subject>Cysteine Proteinase Inhibitors - pharmacology</subject><subject>Dipeptides - pharmacology</subject><subject>Dipeptidyl aldehyde</subject><subject>Endopeptidases</subject><subject>Female</subject><subject>Humans</subject><subject>Leucine - analogs & derivatives</subject><subject>Leucine - pharmacology</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>Ovariectomy</subject><subject>Pharmacology. Drug treatments</subject><subject>Rats</subject><subject>Rats, Sprague-Dawley</subject><issn>0014-2999</issn><issn>1879-0712</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1996</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkU1v1DAQhi0EKtvCPwDJB1S1Bxd_xHZ8QUIVBaSqHICz5ThjYZSNg51dkf56HHa1R7jYHs0z74znRegVozeMMvWWUtYQboy5MvKa0la2RD1BG9ZqQ6hm_CnanJDn6LyUn5RSabg8Q2etbhjT7QZNX3fTlKGUuAcMIYCfcQr4gVx1MD4uQ_q9eJe7NC7DNcEDmX5AfbrB1XON5yWnEkc34DTiigGuYilPc6xxHPE-zjlhN_aHYJ9eoGfBDQVeHu8L9P3uw7fbT-T-y8fPt-_viW9aMRMughedUiE42QDjwajOhSCNcJQKxbToO8m1prz3wjUqGAoGGhk8U5pzKi7Q5UF3yunXDspst7F4GOrkkHbF6pZpw7j4L8ikNrWPqmBzAH39cskQ7JTj1uXFMmpXR-y6bruu2xpp_zpi17LXR_1dt4X-VHS0oObfHPOueDeE7EYfywkTTHAueMXeHTCoS9tHyLb4CKOHPuZqmu1T_PccfwDBeKfd</recordid><startdate>19960404</startdate><enddate>19960404</enddate><creator>Woo, Je-Tae</creator><creator>Yamaguchi, Kohji</creator><creator>Hayama, Takahiro</creator><creator>Kobori, Takeo</creator><creator>Sigeizumi, Sanae</creator><creator>Sugimoto, Kikuo</creator><creator>Kondo, Kiyosi</creator><creator>Tsuji, Tomoko</creator><creator>Ohba, Yasuo</creator><creator>Tagami, Kahori</creator><creator>Sumitani, Koji</creator><general>Elsevier B.V</general><general>Elsevier</general><scope>IQODW</scope><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>7QP</scope><scope>7X8</scope></search><sort><creationdate>19960404</creationdate><title>Suppressive effect of N-(benzyloxycarbonyl)- l-phenylalanyl- l-tyrosinal on bone resorption in vitro and in vivo</title><author>Woo, Je-Tae ; Yamaguchi, Kohji ; Hayama, Takahiro ; Kobori, Takeo ; Sigeizumi, Sanae ; Sugimoto, Kikuo ; Kondo, Kiyosi ; Tsuji, Tomoko ; Ohba, Yasuo ; Tagami, Kahori ; Sumitani, Koji</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c483t-23fc3b66ffa54e12f96baff593a0036173db527702dc3a46f90e9e45fc1672203</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1996</creationdate><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Bone and Bones - drug effects</topic><topic>Bone and Bones - metabolism</topic><topic>Bone resorption</topic><topic>Bone Resorption - physiopathology</topic><topic>Bones, joints and connective tissue. Antiinflammatory agents</topic><topic>Cathepsin L</topic><topic>Cathepsins - antagonists & inhibitors</topic><topic>Cysteine Endopeptidases</topic><topic>Cysteine protease inhibitor</topic><topic>Cysteine Proteinase Inhibitors - pharmacology</topic><topic>Dipeptides - pharmacology</topic><topic>Dipeptidyl aldehyde</topic><topic>Endopeptidases</topic><topic>Female</topic><topic>Humans</topic><topic>Leucine - analogs & derivatives</topic><topic>Leucine - pharmacology</topic><topic>Medical sciences</topic><topic>Mice</topic><topic>Ovariectomy</topic><topic>Pharmacology. Drug treatments</topic><topic>Rats</topic><topic>Rats, Sprague-Dawley</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Woo, Je-Tae</creatorcontrib><creatorcontrib>Yamaguchi, Kohji</creatorcontrib><creatorcontrib>Hayama, Takahiro</creatorcontrib><creatorcontrib>Kobori, Takeo</creatorcontrib><creatorcontrib>Sigeizumi, Sanae</creatorcontrib><creatorcontrib>Sugimoto, Kikuo</creatorcontrib><creatorcontrib>Kondo, Kiyosi</creatorcontrib><creatorcontrib>Tsuji, Tomoko</creatorcontrib><creatorcontrib>Ohba, Yasuo</creatorcontrib><creatorcontrib>Tagami, Kahori</creatorcontrib><creatorcontrib>Sumitani, Koji</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Calcium & Calcified Tissue Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>European journal of pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Woo, Je-Tae</au><au>Yamaguchi, Kohji</au><au>Hayama, Takahiro</au><au>Kobori, Takeo</au><au>Sigeizumi, Sanae</au><au>Sugimoto, Kikuo</au><au>Kondo, Kiyosi</au><au>Tsuji, Tomoko</au><au>Ohba, Yasuo</au><au>Tagami, Kahori</au><au>Sumitani, Koji</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Suppressive effect of N-(benzyloxycarbonyl)- l-phenylalanyl- l-tyrosinal on bone resorption in vitro and in vivo</atitle><jtitle>European journal of pharmacology</jtitle><addtitle>Eur J Pharmacol</addtitle><date>1996-04-04</date><risdate>1996</risdate><volume>300</volume><issue>1</issue><spage>131</spage><epage>135</epage><pages>131-135</pages><issn>0014-2999</issn><eissn>1879-0712</eissn><coden>EJPHAZ</coden><abstract>The suppressive effect of
N-(benzyloxycarbonyl)-
l-phenylalanyl-
l-tyrosinal on bone resorption was examined in vitro and in vivo. This synthetic peptidyl aldehyde was found to be a potent and selective cathepsin L inhibitor in our screening for cysteine protease inhibitors. In the pit formation assay with unfractionated rat bone cells, 1.5 nM of this compound markedly inhibited parathyroid hormone-stimulated osteoclastic bone resorption. In addition, intraperitoneal administration of this peptidyl aldehyde (2.5–10 mg/kg) for 4 weeks suppressed bone weight loss dose dependently in the ovariectomized mouse, experimental model of osteoporosis. Hydroxyproline measurement of the decalcified femurs from these ovariectomized mice suggested that this compound acts as a bone resorption suppressor through the inhibition of collagen degradation.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>8741178</pmid><doi>10.1016/0014-2999(95)00858-6</doi><tpages>5</tpages></addata></record> |
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| ispartof | European journal of pharmacology, 1996-04, Vol.300 (1), p.131-135 |
| issn | 0014-2999 1879-0712 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Animals Biological and medical sciences Bone and Bones - drug effects Bone and Bones - metabolism Bone resorption Bone Resorption - physiopathology Bones, joints and connective tissue. Antiinflammatory agents Cathepsin L Cathepsins - antagonists & inhibitors Cysteine Endopeptidases Cysteine protease inhibitor Cysteine Proteinase Inhibitors - pharmacology Dipeptides - pharmacology Dipeptidyl aldehyde Endopeptidases Female Humans Leucine - analogs & derivatives Leucine - pharmacology Medical sciences Mice Ovariectomy Pharmacology. Drug treatments Rats Rats, Sprague-Dawley |
| title | Suppressive effect of N-(benzyloxycarbonyl)- l-phenylalanyl- l-tyrosinal on bone resorption in vitro and in vivo |
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