Literature summary for 3.4.21.76 extracted from

Guarino, C.; Gruba, N.; Grzywa, R.; Dyguda-Kazimierowicz, E.; Hamon, Y.; Legowska, M.; Skorenski, M.; Dallet-Choisy, S.; Marchand-Adam, S.; Kellenberger, C.; Jenne, D.E.; Sienczyk, M.; Lesner, A.; Gauthier, F.; Korkmaz, B.
Exploiting the S4-S5 specificity of human neutrophil proteinase 3 to improve the potency of peptidyl di(chlorophenyl)-phosphonate ester inhibitors a kinetic and molecular modeling analysis (2018), J. Med. Chem., 61, 1858-1870 .

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Inhibitors

Inhibitors	Comment	Organism
1-acetyl-L-prolyl-L-tyrosyl-N-[1-[bis(4-chlorophenoxy)phosphoryl]ethyl]-L-alpha-asparagine	-	Homo sapiens
1-[11,21-dioxo-25-[(3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl]-4,7,14,17-tetraoxa-10,20-diazapentacosanan-1-oyl]-L-prolyl-L-tyrosyl-N-[1-[bis(4-chlorophenoxy)phosphoryl]ethyl]-L-alpha-asparagine	-	Homo sapiens
1-[5-[(3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl]pentanoyl]-L-prolyl-L-tyrosyl-N-[1-[bis(4-chlorophenoxy)phosphoryl]butyl]-L-alpha-asparagine	-	Homo sapiens
1-[5-[(3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl]pentanoyl]-L-prolyl-L-tyrosyl-N-[1-[bis(4-chlorophenoxy)phosphoryl]ethyl]-L-alpha-asparagine	-	Homo sapiens
4-methyl-N-[5-[(3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl]pentanoyl]-L-norleucyl-L-tyrosyl-N-[1-[bis(4-chlorophenoxy)phosphoryl]ethyl]-L-alpha-asparagine	-	Homo sapiens
biotin-Val-Tyr-Asp-NvaP(O-C6H4-4-Cl)2	occupancy of the S1 subsite of PR3 by a NVA residue and of the S4-S5 subsites by a biotinylated Val residue enhances the second-order inhibition constant toward PR3 by more than 10 times as compared to the best phosphonate PR3 inhibitor reported. The inhibitor shows no significant inhibitory activity toward human neutrophil elastase and resists proteolytic degradation in sputa from cystic fibrosis patients. It also inhibits macaque PR3 but not the PR3 from rodents	Homo sapiens
additional information	potencies of peptidyl di(chlorophenyl)-phosphonate ester inhibitors, kinetics and molecular docking and modeling, overview	Homo sapiens
N-[5-[(3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl]pentanoyl]-L-leucyl-L-tyrosyl-N-[1-[bis(4-chlorophenoxy)phosphoryl]ethyl]-L-alpha-asparagine	-	Homo sapiens
N-[5-[(3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl]pentanoyl]-L-norleucyl-L-tyrosyl-N-[1-[bis(4-chlorophenoxy)phosphoryl]ethyl]-L-alpha-asparagine	-	Homo sapiens
N-[5-[(3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl]pentanoyl]-L-valyl-L-tyrosyl-N-[1-[bis(4-chlorophenoxy)phosphoryl]butyl]-L-alpha-asparagine	-	Homo sapiens
N-[5-[(3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl]pentanoyl]-L-valyl-L-tyrosyl-N-[1-[bis(4-chlorophenoxy)phosphoryl]ethyl]-L-alpha-asparagine	-	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	P24158	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
neutrophil	-	Homo sapiens	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
additional information	analysis of S4-S5 specificity of human neutrophil proteinase 3	Homo sapiens	?	-	?

Synonyms

Synonyms	Comment	Organism
neutrophil proteinase 3	-	Homo sapiens
neutrophilic serine protease proteinase 3	-	Homo sapiens
PR3	-	Homo sapiens
proteinase 3	-	Homo sapiens

General Information

General Information	Comment	Organism
physiological function	the neutrophilic serine protease proteinase 3 (PR3) is involved in inflammation and immune response and is a therapeutic target for a variety of infectious and inflammatory diseases	Homo sapiens