Literature summary for 3.4.24.34 extracted from

Pochetti, G.; Gavuzzo, E.; Campestre, C.; Agamennone, M.; Tortorella, P.; Consalvi, V.; Gallina, C.; Hiller, O.; Tschesche, H.; Tucker, P.A.; Mazza, F.
Structural insight into the stereoselective inhibition of MMP-8 by enantiomeric sulfonamide phosphonates (2006), J. Med. Chem., 49, 923-931.

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Crystallization (Commentary)

Crystallization (Comment)	Organism
MMP-8 in complex with inhibitors (S)- and (R)-alpha-arylsulfonylamino phosphonate, hanging drop vapor diffusion method at 18°C, mixing of 0.0015 ml of protein solution containing 6 mg/mL protein in 5 mM CaCl2, 100 mM NaCl, 0.5 mM ZnCl2, 3 mM MES-NaOH, 0.02% NaN3, pH 6.0, with 0.001 ml of inhibitor solution containing 1 mM inhibitor in 0.2 M MES-NaOH, 20% MeOH, pH 6.0, and 0.005 ml of PEG solution containing 10% m/v PEG 6000, 0.2 M MES-NaOH, 0.02% NaN3, pH 6.0, droplets are concentrated against a reservoir buffer containing 1.6 M sodium phosphate buffer, 0.02% NaN3, pH 6.0, X-ray diffraction structure determination and anaylsis at 1.56-1.94 A resolution	Homo sapiens

Crystallization (Comment)

Organism

MMP-8 in complex with inhibitors (S)- and (R)-alpha-arylsulfonylamino phosphonate, hanging drop vapor diffusion method at 18°C, mixing of 0.0015 ml of protein solution containing 6 mg/mL protein in 5 mM CaCl2, 100 mM NaCl, 0.5 mM ZnCl2, 3 mM MES-NaOH, 0.02% NaN3, pH 6.0, with 0.001 ml of inhibitor solution containing 1 mM inhibitor in 0.2 M MES-NaOH, 20% MeOH, pH 6.0, and 0.005 ml of PEG solution containing 10% m/v PEG 6000, 0.2 M MES-NaOH, 0.02% NaN3, pH 6.0, droplets are concentrated against a reservoir buffer containing 1.6 M sodium phosphate buffer, 0.02% NaN3, pH 6.0, X-ray diffraction structure determination and anaylsis at 1.56-1.94 A resolution

Homo sapiens

Inhibitors

Inhibitors	Comment	Organism
(1R)-[1-(4'-methoxybiphenyl-4-sulfonylamino)-2-methylpropyl]carboxylate	-	Homo sapiens
(1R)-[1-(4'-methoxybiphenyl-4-sulfonylamino)-2-methylpropyl]hydroxamate	-	Homo sapiens
(1R)-[1-(4'-methoxybiphenyl-4-sulfonylamino)-2-methylpropyl]phosphonate	binding structure at the S1' pocket, detailed mode of binding, overview	Homo sapiens
(1S)-[1-(4'-methoxybiphenyl-4-sulfonylamino)-2-methylpropyl]carboxylate	-	Homo sapiens
(1S)-[1-(4'-methoxybiphenyl-4-sulfonylamino)-2-methylpropyl]hydroxamate	-	Homo sapiens
(1S)-[1-(4'-methoxybiphenyl-4-sulfonylamino)-2-methylpropyl]phosphonate	binding structure at the S1' pocket, detailed mode of binding, overview	Homo sapiens
additional information	inhibitor-induced conformational changes at the active site, structure-activity relationships, overview	Homo sapiens
N-hydroxy-N2-[(4-phenoxyphenyl)sulfonyl]valinamide	-	Homo sapiens

Metals/Ions

Metals/Ions	Comment	Organism	Structure
Ca2+	-	Homo sapiens
Zn2+	a zinc metalloendoprotease	Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
additional information	Homo sapiens	MMP-8 can degrade all the components of the extracellular matrix	?	-	?

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
additional information	MMP-8 can degrade all the components of the extracellular matrix	Homo sapiens	?	-	?

Synonyms

Synonyms	Comment	Organism
MMP-8	-	Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C]	Temperature Optimum Maximum [°C]	Comment	Organism
25	-	assay at	Homo sapiens

pH Optimum

pH Optimum Minimum	pH Optimum Maximum	Comment	Organism
7.5	-	assay at	Homo sapiens

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.0000006	-	pH 7.5, 25°C	Homo sapiens	(1R)-[1-(4'-methoxybiphenyl-4-sulfonylamino)-2-methylpropyl]phosphonate
0.0007	-	pH 7.5, 25°C	Homo sapiens	(1S)-[1-(4'-methoxybiphenyl-4-sulfonylamino)-2-methylpropyl]phosphonate