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Identification of s...
Identification of small molecules blocking the Pseudomonas aeruginosa type III secretion system protein PcrV
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- Sundin, Charlotta (författare)
- Umeå universitet,Kemiska institutionen
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- Saleeb, Michael (författare)
- Umeå universitet,Kemiska institutionen
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- Spjut, Sara, 1978- (författare)
- Umeå universitet,Kemiska institutionen
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- Qin, Liena (författare)
- Umeå universitet,Kemiska institutionen
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- Elofsson, Mikael (författare)
- Umeå universitet,Kemiska institutionen
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(creator_code:org_t)
- 2021-01-04
- 2021
- Engelska.
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Ingår i: Biomolecules. - : MDPI. - 2218-273X. ; 11:1
- Relaterad länk:
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https://doi.org/10.3...
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https://umu.diva-por... (primary) (Raw object)
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https://www.mdpi.com...
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https://urn.kb.se/re...
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https://doi.org/10.3...
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Abstract
Ämnesord
Stäng
- Pseudomonas aeruginosa is an opportunistic bacterial pathogen that employs its type III secretion system (T3SS) during the acute phase of infection to translocate cytotoxins into the host cell cytoplasm to evade the immune system. The PcrV protein is located at the tip of the T3SS, facilitates the integration of pore-forming proteins into the eukaryotic cell membrane, and is required for translocation of cytotoxins into the host cell. In this study, we used surface plasmon resonance screening to identify small molecule binders of PcrV. A follow-up structure-activity relationship analysis resulted in PcrV binders that protect macrophages in a P. aeruginosa cell-based infection assay. Treatment of P. aeruginosa infections is challenging due to acquired, intrinsic, and adaptive resistance in addition to a broad arsenal of virulence systems such as the T3SS. Virulence blocking molecules targeting PcrV constitute valuable starting points for development of next generation antibacterials to treat infections caused by P. aeruginosa.
Ämnesord
- NATURVETENSKAP -- Kemi -- Organisk kemi (hsv//swe)
- NATURAL SCIENCES -- Chemical Sciences -- Organic Chemistry (hsv//eng)
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Mikrobiologi inom det medicinska området (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Microbiology in the medical area (hsv//eng)
Nyckelord
- Pseudomonas aeruginosa
- type III secretion
- PcrV
- surface plasmon resonance
- screening
- small molecules
- macrophages
- virulence inhibitors
- infection
- organisk kemi
- Organic Chemistry
- biology
- biologi
Publikations- och innehållstyp
- ref (ämneskategori)
- art (ämneskategori)
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