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Literature summary for 3.4.25.1 extracted from

  • Yoo, E.; Stokes, B.H.; de Jong, H.; Vanaerschot, M.; Kumar, T.; Lawrence, N.; Njoroge, M.; Garcia, A.; Van der Westhuyzen, R.; Momper, J.D.; Ng, C.L.; Fidock, D.A.; Bogyo, M.
    Defining the determinants of specificity of Plasmodium proteasome inhibitors (2018), J. Am. Chem. Soc., 140, 11424-11437 .
    View publication on PubMedView publication on EuropePMC
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Inhibitors

Inhibitors Comment Organism Structure
N-(2-methyl-1,3-thiazole-5-carbonyl)-5-phenyl-L-norvalyl-N-[(1E,3S)-1-(methanesulfonyl)-5-methylhex-1-en-3-yl]-L-homoserinamide compound has low nanomolar activity at killing parasite in the 72 h treatment with exceptionally low toxicity against human foreskin fibroblast resulting in greatly enhanced selectivity ratio. Compound has no toxicity to HepG2 cells even after 72 h treatment with doses as high as 10 microM Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum
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Plasmodium falciparum W2
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Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information enzyme has a preference for aromatic residues at P1 such as Phe, Tyr, Trp, and His. Aliphatic side chains (propyl, butyl) are well tolerated in the P2 position. The S3 pocket accommodates bulky and hydrophobic residues Plasmodium falciparum ?
-
 ?
additional information enzyme has a preference for aromatic residues at P1 such as Phe, Tyr, Trp, and His. Aliphatic side chains (propyl, butyl) are well tolerated in the P2 position. The S3 pocket accommodates bulky and hydrophobic residues Plasmodium falciparum W2 ?
-
 ?
morpholinoacetyl-homophenylalanyl-methylseryl-thienylalanyl-7-amido-4-carbamoylmethylcoumarin + H2O most optimal combination of substrate residues identified Plasmodium falciparum morpholinoacetyl-homophenylalanine-methylserine-thienylalanine + 7-amino-4-carbamoylmethylcoumarin
-
 ?
morpholinoacetyl-homophenylalanyl-methylseryl-thienylalanyl-7-amido-4-carbamoylmethylcoumarin + H2O most optimal combination of substrate residues identified Plasmodium falciparum W2 morpholinoacetyl-homophenylalanine-methylserine-thienylalanine + 7-amino-4-carbamoylmethylcoumarin
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 ?