Matches in SemOpenAlex for { <https://semopenalex.org/work/W2948559700> ?p ?o ?g. }
- W2948559700 endingPage "6145" @default.
- W2948559700 startingPage "6137" @default.
- W2948559700 abstract "The Plasmodium proteasome (Pf20S) emerged as a target for antimalarials. Pf20S inhibitors are active at multiple stages of the parasite life cycle and synergize with artemisinins, suggesting that Pf20S inhibitors have potential to be prophylactic, therapeutic, and transmission blocking as well as are useful for combination therapy. We recently reported asparagine ethylenediamines (AsnEDAs) as immunoproteasome inhibitors and modified AsnEDAs as selective Pf20S inhibitors. Here, we report further a structure-activity relationship study of AsnEDAs for selective inhibition of Pf20S over human proteasomes. Additionally, we show new mutation that conferred resistance to AsnEDAs and collateral sensitivity to an inhibitor of the Pf20S β2 subunit, the same as previously identified resistant mutation. This resistance could be overcome through the use of the structure-guided inhibitor design. Collateral sensitivity to inhibitors among respective proteasome subunits underscores the potential value of treating malaria with combinations of inhibitors of different proteasome subunits to minimize the emergence of drug resistance." @default.
- W2948559700 created "2019-06-14" @default.
- W2948559700 creator A5000986048 @default.
- W2948559700 creator A5004483141 @default.
- W2948559700 creator A5007066567 @default.
- W2948559700 creator A5011515834 @default.
- W2948559700 creator A5032012451 @default.
- W2948559700 creator A5036666565 @default.
- W2948559700 creator A5037689453 @default.
- W2948559700 creator A5040091657 @default.
- W2948559700 creator A5043882333 @default.
- W2948559700 creator A5047847814 @default.
- W2948559700 creator A5050207383 @default.
- W2948559700 creator A5068972754 @default.
- W2948559700 creator A5070982391 @default.
- W2948559700 creator A5075525907 @default.
- W2948559700 creator A5076363473 @default.
- W2948559700 creator A5077631479 @default.
- W2948559700 creator A5078708996 @default.
- W2948559700 creator A5086017109 @default.
- W2948559700 creator A5087903668 @default.
- W2948559700 date "2019-06-09" @default.
- W2948559700 modified "2023-10-15" @default.
- W2948559700 title "Improvement of Asparagine Ethylenediamines as Anti-malarial <i>Plasmodium</i>-Selective Proteasome Inhibitors" @default.
- W2948559700 cites W1965575777 @default.
- W2948559700 cites W1974010669 @default.
- W2948559700 cites W1975396841 @default.
- W2948559700 cites W1999119754 @default.
- W2948559700 cites W1999353132 @default.
- W2948559700 cites W2007703161 @default.
- W2948559700 cites W2010163650 @default.
- W2948559700 cites W2014404730 @default.
- W2948559700 cites W2035992308 @default.
- W2948559700 cites W2055465577 @default.
- W2948559700 cites W2076682168 @default.
- W2948559700 cites W2088245562 @default.
- W2948559700 cites W2107324383 @default.
- W2948559700 cites W2108981909 @default.
- W2948559700 cites W2114818342 @default.
- W2948559700 cites W2133913001 @default.
- W2948559700 cites W2171102256 @default.
- W2948559700 cites W2256548132 @default.
- W2948559700 cites W2322436739 @default.
- W2948559700 cites W2478575915 @default.
- W2948559700 cites W2518116639 @default.
- W2948559700 cites W2562526830 @default.
- W2948559700 cites W2734549968 @default.
- W2948559700 cites W2755002668 @default.
- W2948559700 cites W2768357100 @default.
- W2948559700 cites W2799282155 @default.
- W2948559700 cites W2800834635 @default.
- W2948559700 cites W2810656554 @default.
- W2948559700 cites W2886849711 @default.
- W2948559700 cites W2899174839 @default.
- W2948559700 doi "https://doi.org/10.1021/acs.jmedchem.9b00363" @default.
- W2948559700 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/7104388" @default.
- W2948559700 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/31177777" @default.
- W2948559700 hasPublicationYear "2019" @default.
- W2948559700 type Work @default.
- W2948559700 sameAs 2948559700 @default.
- W2948559700 citedByCount "27" @default.
- W2948559700 countsByYear W29485597002019 @default.
- W2948559700 countsByYear W29485597002020 @default.
- W2948559700 countsByYear W29485597002021 @default.
- W2948559700 countsByYear W29485597002022 @default.
- W2948559700 countsByYear W29485597002023 @default.
- W2948559700 crossrefType "journal-article" @default.
- W2948559700 hasAuthorship W2948559700A5000986048 @default.
- W2948559700 hasAuthorship W2948559700A5004483141 @default.
- W2948559700 hasAuthorship W2948559700A5007066567 @default.
- W2948559700 hasAuthorship W2948559700A5011515834 @default.
- W2948559700 hasAuthorship W2948559700A5032012451 @default.
- W2948559700 hasAuthorship W2948559700A5036666565 @default.
- W2948559700 hasAuthorship W2948559700A5037689453 @default.
- W2948559700 hasAuthorship W2948559700A5040091657 @default.
- W2948559700 hasAuthorship W2948559700A5043882333 @default.
- W2948559700 hasAuthorship W2948559700A5047847814 @default.
- W2948559700 hasAuthorship W2948559700A5050207383 @default.
- W2948559700 hasAuthorship W2948559700A5068972754 @default.
- W2948559700 hasAuthorship W2948559700A5070982391 @default.
- W2948559700 hasAuthorship W2948559700A5075525907 @default.
- W2948559700 hasAuthorship W2948559700A5076363473 @default.
- W2948559700 hasAuthorship W2948559700A5077631479 @default.
- W2948559700 hasAuthorship W2948559700A5078708996 @default.
- W2948559700 hasAuthorship W2948559700A5086017109 @default.
- W2948559700 hasAuthorship W2948559700A5087903668 @default.
- W2948559700 hasBestOaLocation W29485597002 @default.
- W2948559700 hasConcept C114851261 @default.
- W2948559700 hasConcept C166342909 @default.
- W2948559700 hasConcept C181199279 @default.
- W2948559700 hasConcept C185592680 @default.
- W2948559700 hasConcept C203014093 @default.
- W2948559700 hasConcept C27740335 @default.
- W2948559700 hasConcept C2775895851 @default.
- W2948559700 hasConcept C2778048844 @default.
- W2948559700 hasConcept C2778371730 @default.
- W2948559700 hasConcept C55493867 @default.
- W2948559700 hasConcept C86803240 @default.