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 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 IC50 of approximately 80 microM.
| Medienart: |
Artikel |
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| Erscheinungsjahr: |
1995 |
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| Erschienen: |
1995 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:3 |
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| Enthalten in: |
Bioorganic & medicinal chemistry - 3(1995), 3 vom: 26. März, Seite 257-65 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Samson, I [VerfasserIn] |
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| Anmerkungen: |
Date Completed 17.08.1995 Date Revised 30.08.2019 published: Print Citation Status MEDLINE |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM075825163 |
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| LEADER | 01000naa a22002652 4500 | ||
|---|---|---|---|
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| 008 | 231222s1995 xx ||||| 00| ||eng c | ||
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| 100 | 1 | |a Samson, I |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Identification of a peptide inhibitor against glycosomal phosphoglycerate kinase of Trypanosoma brucei by a synthetic peptide library approach |
| 264 | 1 | |c 1995 | |
| 336 | |a Text |b txt |2 rdacontent | ||
| 337 | |a ohne Hilfsmittel zu benutzen |b n |2 rdamedia | ||
| 338 | |a Band |b nc |2 rdacarrier | ||
| 500 | |a Date Completed 17.08.1995 | ||
| 500 | |a Date Revised 30.08.2019 | ||
| 500 | |a published: Print | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a 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 IC50 of approximately 80 microM | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Research Support, Non-U.S. Gov't | |
| 650 | 7 | |a Affinity Labels |2 NLM | |
| 650 | 7 | |a Bacterial Proteins |2 NLM | |
| 650 | 7 | |a Enzyme Inhibitors |2 NLM | |
| 650 | 7 | |a Fluoresceins |2 NLM | |
| 650 | 7 | |a Oligopeptides |2 NLM | |
| 650 | 7 | |a Biotin |2 NLM | |
| 650 | 7 | |a 6SO6U10H04 |2 NLM | |
| 650 | 7 | |a Streptavidin |2 NLM | |
| 650 | 7 | |a 9013-20-1 |2 NLM | |
| 650 | 7 | |a Phosphoglycerate Kinase |2 NLM | |
| 650 | 7 | |a EC 2.7.2.3 |2 NLM | |
| 650 | 7 | |a Fluorescein |2 NLM | |
| 650 | 7 | |a TPY09G7XIR |2 NLM | |
| 700 | 1 | |a Kerremans, L |e verfasserin |4 aut | |
| 700 | 1 | |a Rozenski, J |e verfasserin |4 aut | |
| 700 | 1 | |a Samyn, B |e verfasserin |4 aut | |
| 700 | 1 | |a Van Beeumen, J |e verfasserin |4 aut | |
| 700 | 1 | |a Van Aerschot, A |e verfasserin |4 aut | |
| 700 | 1 | |a Herdewijn, P |e verfasserin |4 aut | |
| 773 | 0 | 8 | |i Enthalten in |t Bioorganic & medicinal chemistry |d 1994 |g 3(1995), 3 vom: 26. März, Seite 257-65 |w (DE-627)NLM074978543 |x 1464-3391 |7 nnns |
| 773 | 1 | 8 | |g volume:3 |g year:1995 |g number:3 |g day:26 |g month:03 |g pages:257-65 |
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| 951 | |a AR | ||
| 952 | |d 3 |j 1995 |e 3 |b 26 |c 03 |h 257-65 | ||