Literature summary for 3.4.24.13 extracted from

Shehaj, L.; Choudary, S.K.; Makwana, K.M.; Gallo, M.C.; Murphy, T.F.; Kritzer, J.A.
Small-molecule inhibitors of Haemophilus influenzae IgA1 protease (2019), ACS Infect. Dis., 5, 1129-1138 .

Search for more literature for 3.4.24.13

Inhibitors

Inhibitors	Comment	Organism
1-(tert-butylamino)-3-[[4-(morpholin-4-yl)-1,2,5-thiadiazol-3-yl]oxy]propan-2-ol	-	Haemophilus influenzae NTHI
2-(morpholin-4-yl)cyclohexyl cyclohexanecarboxylate	-	Haemophilus influenzae NTHI
2-(morpholin-4-yl)phenyl benzoate	-	Haemophilus influenzae NTHI
4-(morpholin-4-yl)-1,2,5-thiadiazol-3-ol	-	Haemophilus influenzae NTHI
4-(morpholin-4-yl)-1,2,5-thiadiazol-3-yl benzoate	-	Haemophilus influenzae NTHI
4-(morpholin-4-yl)-1,2,5-thiadiazol-3-yl diphenylcarbamate	-	Haemophilus influenzae NTHI
4-(morpholin-4-yl)-1,2,5-thiadiazol-3-yl morpholine-4-carboxylate	-	Haemophilus influenzae NTHI
4-(morpholin-4-yl)-1,2,5-thiadiazol-3-yl piperidine-1-carboxylate	-	Haemophilus influenzae NTHI
4-(morpholin-4-yl)-1,2,5-thiadiazol-3-yl pyrrolidine-1-carboxylate	-	Haemophilus influenzae NTHI
4-(piperidin-1-yl)-1,2,5-thiadiazol-3-yl diphenylcarbamate	-	Haemophilus influenzae NTHI
4-(piperidin-1-yl)-1,2,5-thiadiazol-3-yl morpholine-4-carboxylate	-	Haemophilus influenzae NTHI
4-methyl-N'-[(morpholin-4-ylcarbonyl)oxy]benzenecarboximidamide	-	Haemophilus influenzae NTHI
4-[4-(benzyloxy)-1,2,5-thiadiazol-3-yl]morpholine	-	Haemophilus influenzae NTHI
cyclopentane-1,2-diyl dibenzoate	-	Haemophilus influenzae NTHI
cyclopentyl 4-methylbenzoate	-	Haemophilus influenzae NTHI
methyl 3-[([[4-(morpholin-4-yl)-1,2,5-thiadiazol-3-yl]oxy]acetyl)amino]benzoate	-	Haemophilus influenzae NTHI
methyl 4-(morpholin-4-yl)-1,2,5-thiadiazol-3-yl carbonate	-	Haemophilus influenzae NTHI
additional information	detection of small molecule, nonpeptidic inhibitors of Haemophilus influenzae IgA1 proteases, inhibitor screening and structure-activity relationship analysis. Improved inhibition and selectivity for IgA protease over other serine proteases	Haemophilus influenzae NTHI
N-(1,3-benzodioxol-5-yl)-2-[[4-(morpholin-4-yl)-1,2,5-thiadiazol-3-yl]oxy]acetamide	-	Haemophilus influenzae NTHI
N-cyclopentyl-2-[[4-(morpholin-4-yl)-1,2,5-thiadiazol-3-yl]oxy]acetamide	-	Haemophilus influenzae NTHI
phenyl morpholine-4-carboxylate	-	Haemophilus influenzae NTHI

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
human immunoglobulin A1 + H2O	Haemophilus influenzae NTHI	cleavage of the hinge region	immunoglobulin Fc + immunoglobulin Fab	-	?

Organism

Organism	UniProt	Comment	Textmining
Haemophilus influenzae NTHI	-	Nontypeable Haemophilus influenzae, four IgA1 protease forms: A1, A2, B1, and B2	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
human immunoglobulin A1 + H2O	cleavage of the hinge region	Haemophilus influenzae NTHI	immunoglobulin Fc + immunoglobulin Fab	-	?
human immunoglobulin A1 + H2O	cleavage of the hinge region	Haemophilus influenzae NTHI	Fc fragment + Fab fragment	-	?

Synonyms

Synonyms	Comment	Organism
IgA1 protease	-	Haemophilus influenzae NTHI
IgA1P	-	Haemophilus influenzae NTHI
IgaA2	-	Haemophilus influenzae NTHI
igaB1	-	Haemophilus influenzae NTHI

General Information

General Information	Comment	Organism
physiological function	enzyme IgA1P cleaves human immunoglobulin A1 (IgA1), the predominant antibody on human mucosal surfaces. The actions of IgA1Ps impede IgA1 from neutralizing the bacteria. Specifically, IgA1P cleaves IgA1 at a unique hinge region, separating the Fc and Fab fragments of the immunoglobulin. This impairs its Fc-mediated effector response and can even allow bacteria to retain the Fab fragment on their surface in order to mask their polysaccharide capsule and other surface antigens	Haemophilus influenzae NTHI