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Literature summary for 3.5.1.99 extracted from

  • Lodola, A.; Mor, M.; Hermann, J.C.; Tarzia, G.; Piomelli, D.; Mulholland, A.J.
    QM/MM modelling of oleamide hydrolysis in fatty acid amide hydrolase (FAAH) reveals a new mechanism of nucleophile activation (2005), Chem. Commun. (Camb. ), 35, 4399-401.
    View publication on PubMed

Application

Application Comment Organism
medicine FAAH is a promising target for the treatment of several central and peripheral nervous system disorders, such as anxiety, pain and hypertension Rattus norvegicus

Protein Variants

Protein Variants Comment Organism
K142A the greater reduction of Ser241 labelling rate in the K142A/S217A double mutant, compared to the K142A and S217A single mutants, suggests that Lys142 and Ser217 cooperate to deprotonate Ser241 Rattus norvegicus
K142A/S217A the greater reduction of Ser241 labelling rate in the K142A/S217A double mutant, compared to the K142A and S217A single mutants, suggests that Lys142 and Ser217 cooperate to deprotonate Ser241 Rattus norvegicus
S217A the greater reduction of Ser241 labelling rate in the K142A/S217A double mutant, compared to the K142A and S217A single mutants, suggests that Lys142 and Ser217 cooperate to deprotonate Ser241 Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
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Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information hybrid quantum mechanics/molecular mechanics (QM/MM) calculations reveal a new mechanism of nucleophile activation involving a Lys–Ser–Ser catalytic triad. The proposed mechanism, shows that Lys142 and cis-Ser217 have a direct role in the activation of Ser241, in agreement with kinetic labelling experiments employing the highly reactive fluorophosphonatetetramethyl rhodamine. The greater reduction of Ser241 labelling rate in the K142A/S217A double mutant, compared to the K142A and S217A single mutants, suggests that Lys142 and Ser217 cooperate to deprotonate Ser241 Rattus norvegicus ?
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Synonyms

Synonyms Comment Organism
FAAH
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Rattus norvegicus