Identification of a peptide inhibitor against glycosomal phosphoglycerate kinase of Trypanosoma brucei by a synthetic peptide library approach
A synthetic peptide library, composed of 2.5 million l-amino acid pentapeptides anchored on polystyrene beads was prepared with each bead bearing a single pentapeptide sequence. This library was screened for interaction with glycosomal phosphoglycerate kinase (gPGK) of Trypanosoma brucei labelled wi...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry 1995-03, Vol.3 (3), p.257-265 |
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| container_title | Bioorganic & medicinal chemistry |
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| creator | Samson, Isabelle Kerremans, Luc Rozenski, Jef Samyn, Bart Van Beeumen, Jozef Van Aerschot, Arthur Herdewijn, Piet |
| description | A synthetic peptide library, composed of 2.5 million
l-amino acid pentapeptides anchored on polystyrene beads was prepared with each bead bearing a single pentapeptide sequence. This library was screened for interaction with glycosomal phosphoglycerate kinase (gPGK) of
Trypanosoma brucei labelled with fluorescein or with biotin. Affinity beads that bound the enzyme were selected with a pipette or with streptavidin coated magnetic beads. The beads that bound to the enzyme were individually subjected to Edman microsequence analysis to determine the sequence of the corresponding peptide ligands. The corresponding peptide-sequences were synthesised as free peptide acids and evaluated for enzyme activity inhibition. The pentapeptide NWMMF was able to selectively inhibit gPGK with an IC
50 of ≈ 80 μM.
The pentapeptide NH
2-Asn-Trp-Met-Met-Phe-OH was identified as a selective inhibitor of glycosomal phosphoglycerate kinase of
T. brucei using a solid phase synthetic peptide library approach. Isolation of the interacting peptide beads was done with streptavidin coated magnetic beads. |
| doi_str_mv | 10.1016/0968-0896(95)00020-H |
| format | Article |
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l-amino acid pentapeptides anchored on polystyrene beads was prepared with each bead bearing a single pentapeptide sequence. This library was screened for interaction with glycosomal phosphoglycerate kinase (gPGK) of
Trypanosoma brucei labelled with fluorescein or with biotin. Affinity beads that bound the enzyme were selected with a pipette or with streptavidin coated magnetic beads. The beads that bound to the enzyme were individually subjected to Edman microsequence analysis to determine the sequence of the corresponding peptide ligands. The corresponding peptide-sequences were synthesised as free peptide acids and evaluated for enzyme activity inhibition. The pentapeptide NWMMF was able to selectively inhibit gPGK with an IC
50 of ≈ 80 μM.
The pentapeptide NH
2-Asn-Trp-Met-Met-Phe-OH was identified as a selective inhibitor of glycosomal phosphoglycerate kinase of
T. brucei using a solid phase synthetic peptide library approach. Isolation of the interacting peptide beads was done with streptavidin coated magnetic beads.</description><identifier>ISSN: 0968-0896</identifier><identifier>EISSN: 1464-3391</identifier><identifier>DOI: 10.1016/0968-0896(95)00020-H</identifier><identifier>PMID: 7606387</identifier><language>eng</language><publisher>England: Elsevier Ltd</publisher><subject>Affinity Labels ; Amino Acid Sequence ; Animals ; Bacterial Proteins ; Biotin ; Enzyme Inhibitors - chemical synthesis ; Enzyme Inhibitors - chemistry ; Enzyme Inhibitors - isolation & purification ; Fluorescein ; Fluoresceins ; Glycolysis - drug effects ; Molecular Sequence Data ; Oligopeptides - chemical synthesis ; Oligopeptides - chemistry ; Oligopeptides - isolation & purification ; Oligopeptides - pharmacology ; Phosphoglycerate Kinase - antagonists & inhibitors ; Streptavidin ; Trypanosoma brucei brucei - enzymology</subject><ispartof>Bioorganic & medicinal chemistry, 1995-03, Vol.3 (3), p.257-265</ispartof><rights>1995</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c357t-aaa539fafe0b2902e73aac18d6b742c28ee6efc2ec02fe2e4bc5d8ac0ddee2b13</citedby><cites>FETCH-LOGICAL-c357t-aaa539fafe0b2902e73aac18d6b742c28ee6efc2ec02fe2e4bc5d8ac0ddee2b13</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/0968-0896(95)00020-H$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,778,782,3539,27911,27912,45982</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/7606387$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Samson, Isabelle</creatorcontrib><creatorcontrib>Kerremans, Luc</creatorcontrib><creatorcontrib>Rozenski, Jef</creatorcontrib><creatorcontrib>Samyn, Bart</creatorcontrib><creatorcontrib>Van Beeumen, Jozef</creatorcontrib><creatorcontrib>Van Aerschot, Arthur</creatorcontrib><creatorcontrib>Herdewijn, Piet</creatorcontrib><title>Identification of a peptide inhibitor against glycosomal phosphoglycerate kinase of Trypanosoma brucei by a synthetic peptide library approach</title><title>Bioorganic & medicinal chemistry</title><addtitle>Bioorg Med Chem</addtitle><description>A synthetic peptide library, composed of 2.5 million
l-amino acid pentapeptides anchored on polystyrene beads was prepared with each bead bearing a single pentapeptide sequence. This library was screened for interaction with glycosomal phosphoglycerate kinase (gPGK) of
Trypanosoma brucei labelled with fluorescein or with biotin. Affinity beads that bound the enzyme were selected with a pipette or with streptavidin coated magnetic beads. The beads that bound to the enzyme were individually subjected to Edman microsequence analysis to determine the sequence of the corresponding peptide ligands. The corresponding peptide-sequences were synthesised as free peptide acids and evaluated for enzyme activity inhibition. The pentapeptide NWMMF was able to selectively inhibit gPGK with an IC
50 of ≈ 80 μM.
The pentapeptide NH
2-Asn-Trp-Met-Met-Phe-OH was identified as a selective inhibitor of glycosomal phosphoglycerate kinase of
T. brucei using a solid phase synthetic peptide library approach. Isolation of the interacting peptide beads was done with streptavidin coated magnetic beads.</description><subject>Affinity Labels</subject><subject>Amino Acid Sequence</subject><subject>Animals</subject><subject>Bacterial Proteins</subject><subject>Biotin</subject><subject>Enzyme Inhibitors - chemical synthesis</subject><subject>Enzyme Inhibitors - chemistry</subject><subject>Enzyme Inhibitors - isolation & purification</subject><subject>Fluorescein</subject><subject>Fluoresceins</subject><subject>Glycolysis - drug effects</subject><subject>Molecular Sequence Data</subject><subject>Oligopeptides - chemical synthesis</subject><subject>Oligopeptides - chemistry</subject><subject>Oligopeptides - isolation & purification</subject><subject>Oligopeptides - pharmacology</subject><subject>Phosphoglycerate Kinase - antagonists & inhibitors</subject><subject>Streptavidin</subject><subject>Trypanosoma brucei brucei - enzymology</subject><issn>0968-0896</issn><issn>1464-3391</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1995</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9UcGO0zAQtRBoKQt_AJJPCA4B20mc5IKEVkBXWonLcrbG9mQ7kNrBdpH6E3wzybbqkcPI0rw3743fMPZaig9SSP1RDLqvRD_od0P7XgihRLV9wjay0U1V14N8yjYXynP2IuefK6kZ5BW76rTQdd9t2N9bj6HQSA4KxcDjyIHPOBfyyCnsyFKJicMDUMiFP0xHF3Pcw8TnXcxLrR1MUJD_ogAZV4X7dJwhPPK4TQeHxO1x0c3HUHZYyF0cJrIJ0oLNc4rgdi_ZsxGmjK_O7zX78fXL_c22uvv-7fbm813l6rYrFQC09TDCiMKqQSjsagAne69t1yinekSNo1PohBpRYWNd63twwntEZWV9zd6edBfb3wfMxewpO5wmCBgP2XRd3Sst1EJsTkSXYs4JRzMn2i8rGynMegazZmzWjM3QmsczmO0y9uasf7B79Jehc-4L_umE4_LJP4TJZEcYHHpK6Irxkf5v8A-Ie5zk</recordid><startdate>19950301</startdate><enddate>19950301</enddate><creator>Samson, Isabelle</creator><creator>Kerremans, Luc</creator><creator>Rozenski, Jef</creator><creator>Samyn, Bart</creator><creator>Van Beeumen, Jozef</creator><creator>Van Aerschot, Arthur</creator><creator>Herdewijn, Piet</creator><general>Elsevier Ltd</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>19950301</creationdate><title>Identification of a peptide inhibitor against glycosomal phosphoglycerate kinase of Trypanosoma brucei by a synthetic peptide library approach</title><author>Samson, Isabelle ; Kerremans, Luc ; Rozenski, Jef ; Samyn, Bart ; Van Beeumen, Jozef ; Van Aerschot, Arthur ; Herdewijn, Piet</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c357t-aaa539fafe0b2902e73aac18d6b742c28ee6efc2ec02fe2e4bc5d8ac0ddee2b13</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1995</creationdate><topic>Affinity Labels</topic><topic>Amino Acid Sequence</topic><topic>Animals</topic><topic>Bacterial Proteins</topic><topic>Biotin</topic><topic>Enzyme Inhibitors - chemical synthesis</topic><topic>Enzyme Inhibitors - chemistry</topic><topic>Enzyme Inhibitors - isolation & purification</topic><topic>Fluorescein</topic><topic>Fluoresceins</topic><topic>Glycolysis - drug effects</topic><topic>Molecular Sequence Data</topic><topic>Oligopeptides - chemical synthesis</topic><topic>Oligopeptides - chemistry</topic><topic>Oligopeptides - isolation & purification</topic><topic>Oligopeptides - pharmacology</topic><topic>Phosphoglycerate Kinase - antagonists & inhibitors</topic><topic>Streptavidin</topic><topic>Trypanosoma brucei brucei - enzymology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Samson, Isabelle</creatorcontrib><creatorcontrib>Kerremans, Luc</creatorcontrib><creatorcontrib>Rozenski, Jef</creatorcontrib><creatorcontrib>Samyn, Bart</creatorcontrib><creatorcontrib>Van Beeumen, Jozef</creatorcontrib><creatorcontrib>Van Aerschot, Arthur</creatorcontrib><creatorcontrib>Herdewijn, Piet</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>Bioorganic & medicinal chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Samson, Isabelle</au><au>Kerremans, Luc</au><au>Rozenski, Jef</au><au>Samyn, Bart</au><au>Van Beeumen, Jozef</au><au>Van Aerschot, Arthur</au><au>Herdewijn, Piet</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Identification of a peptide inhibitor against glycosomal phosphoglycerate kinase of Trypanosoma brucei by a synthetic peptide library approach</atitle><jtitle>Bioorganic & medicinal chemistry</jtitle><addtitle>Bioorg Med Chem</addtitle><date>1995-03-01</date><risdate>1995</risdate><volume>3</volume><issue>3</issue><spage>257</spage><epage>265</epage><pages>257-265</pages><issn>0968-0896</issn><eissn>1464-3391</eissn><abstract>A synthetic peptide library, composed of 2.5 million
l-amino acid pentapeptides anchored on polystyrene beads was prepared with each bead bearing a single pentapeptide sequence. This library was screened for interaction with glycosomal phosphoglycerate kinase (gPGK) of
Trypanosoma brucei labelled with fluorescein or with biotin. Affinity beads that bound the enzyme were selected with a pipette or with streptavidin coated magnetic beads. The beads that bound to the enzyme were individually subjected to Edman microsequence analysis to determine the sequence of the corresponding peptide ligands. The corresponding peptide-sequences were synthesised as free peptide acids and evaluated for enzyme activity inhibition. The pentapeptide NWMMF was able to selectively inhibit gPGK with an IC
50 of ≈ 80 μM.
The pentapeptide NH
2-Asn-Trp-Met-Met-Phe-OH was identified as a selective inhibitor of glycosomal phosphoglycerate kinase of
T. brucei using a solid phase synthetic peptide library approach. Isolation of the interacting peptide beads was done with streptavidin coated magnetic beads.</abstract><cop>England</cop><pub>Elsevier Ltd</pub><pmid>7606387</pmid><doi>10.1016/0968-0896(95)00020-H</doi><tpages>9</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0968-0896 |
| ispartof | Bioorganic & medicinal chemistry, 1995-03, Vol.3 (3), p.257-265 |
| issn | 0968-0896 1464-3391 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_77382602 |
| source | MEDLINE; ScienceDirect Journals (5 years ago - present) |
| subjects | Affinity Labels Amino Acid Sequence Animals Bacterial Proteins Biotin Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - isolation & purification Fluorescein Fluoresceins Glycolysis - drug effects Molecular Sequence Data Oligopeptides - chemical synthesis Oligopeptides - chemistry Oligopeptides - isolation & purification Oligopeptides - pharmacology Phosphoglycerate Kinase - antagonists & inhibitors Streptavidin Trypanosoma brucei brucei - enzymology |
| title | Identification of a peptide inhibitor against glycosomal phosphoglycerate kinase of Trypanosoma brucei by a synthetic peptide library approach |
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