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Literature summary for 3.4.24.86 extracted from

  • Rabinowitz, M.H.; Andrews, R.C.; Becherer, J.D.; Bickett, D.M.; Bubacz, D.G.; Conway, J.G.; Cowan, D.J.; Gaul, M.; Glennon, K.; Lambert, M.H.; Leesnitzer, M.A.; McDougald, D.L.; Moss, M.L.; Musso, D.L.; Rizzolio, M.C.
    Design of selective and soluble inhibitors of tumor necrosis factor-alpha converting enzyme (TACE) (2001), J. Med. Chem., 44, 4252-4267.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(2R)-5-nitroguanyl-2-([(2R,3S)-2-(cyclohexylmethyl)-3-cyclopropyl-3-[formyl(hydroxy)amino]propanoyl]-amino)-N-(1,3-thiazol-2-yl)pentanamide
-
Homo sapiens
(2R)-5-nitroguanyl-2-([(2R,3S)-2-(cyclohexylmethyl)-3-cyclopropyl-3-[formyl(hydroxy)amino]propanoyl]-amino)-N-(1,3-thiazol-2-yl)pentanamide
-
Mus musculus
(2R,3S)-N-[(1S)-4-(2-pyridylsulfonyl)guanyl-1-[(1,3-thiazol-2-ylamino)-carbonyl]butyl]-3-[formyl(hydroxy)amino]-2-isobutylhexanamide
-
Homo sapiens
(2R,3S)-N-[(1S)-4-(2-pyridylsulfonyl)guanyl-1-[(1,3-thiazol-2-ylamino)-carbonyl]butyl]-3-[formyl(hydroxy)amino]-2-isobutylhexanamide
-
Mus musculus
(2R,3S)-N-[(1S)-4-(2-pyridylsulfonyl)guanyl-1-[(1,3-thiazol-2-ylamino)-carbonyl]butyl]-3-[formyl(hydroxy)amino]-2-[(4-methylcyclohexyl)-methyl]hexanamide
-
Homo sapiens
(2R,3S)-N-[(1S)-4-(2-pyridylsulfonyl)guanyl-1-[(1,3-thiazol-2-ylamino)-carbonyl]butyl]-3-[formyl(hydroxy)amino]-2-[(4-methylcyclohexyl)-methyl]hexanamide
-
Mus musculus
(2R,3S)-N-[(1S)-4-(2-pyridylsulfonyl)guanyl-1-[(1,3-thiazol-2-ylamino)-carbonyl]butyl]-3-[formyl(hydroxy)amino]-2-[(5-methyl-2-thienyl)methyl]hexanamide
-
Homo sapiens
(2R,3S)-N-[(1S)-4-(2-pyridylsulfonyl)guanyl-1-[(1,3-thiazol-2-ylamino)-carbonyl]butyl]-3-[formyl(hydroxy)amino]-2-[(5-methyl-2-thienyl)methyl]hexanamide
-
Mus musculus
(2R,3S)-N-[(1S)-4-(2-pyridylsulfonyl)guanyl-1-[(1,3-thiazol-2-ylamino)-carbonyl]butyl]-3-[formyl(hydroxy)amino]-4-methyl-2-[(4-methylcyclohexyl)methyl]pentanamide
-
Homo sapiens
(2R,3S)-N-[(1S)-4-(2-pyridylsulfonyl)guanyl-1-[(1,3-thiazol-2-ylamino)-carbonyl]butyl]-3-[formyl(hydroxy)amino]-4-methyl-2-[(4-methylcyclohexyl)methyl]pentanamide
-
Mus musculus
(2R,3S)-N-[(1S)-4-methanesulfonylguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl(hydroxy)amino]-2-isobutyl-4-methylpentanamide
-
Homo sapiens
(2R,3S)-N-[(1S)-4-methanesulfonylguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl(hydroxy)amino]-2-isobutyl-4-methylpentanamide
-
Mus musculus
(2R,3S)-N-[(1S)-4-methanesulfonylguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl(hydroxy)amino]-2-isobutylhexanamide
-
Homo sapiens
(2R,3S)-N-[(1S)-4-methanesulfonylguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl(hydroxy)amino]-2-isobutylhexanamide
-
Mus musculus
(2R,3S)-N-[(1S)-4-methanesulfonylguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl(hydroxy)amino]-4-methyl-2-[(4-methylcyclohexyl)methyl]pentanamide
-
Homo sapiens
(2R,3S)-N-[(1S)-4-methanesulfonylguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl(hydroxy)amino]-4-methyl-2-[(4-methylcyclohexyl)methyl]pentanamide
-
Mus musculus
(2R,3S)-N-[(1S)-4-methanesulfonylguanyl-2-methyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl-(hydroxy)amino]-2-isobutyl-4-methylpentanamide
-
Homo sapiens
(2R,3S)-N-[(1S)-4-methanesulfonylguanyl-2-methyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl-(hydroxy)amino]-2-isobutyl-4-methylpentanamide
-
Mus musculus
(2R,3S)-N-[(1S)-4-methanesulfonylguanyl-2-methyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl-(hydroxy)amino]-2-isobutylhexanamide
-
Homo sapiens
(2R,3S)-N-[(1S)-4-methanesulfonylguanyl-2-methyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl-(hydroxy)amino]-2-isobutylhexanamide
-
Mus musculus
(2R,3S)-N-[(1S)-4-methanesulfonylguanyl-2-methyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-6,6,6-trifluoro-3-[formyl(hydroxy)amino]-2-isobutylhexanamide
-
Homo sapiens
(2R,3S)-N-[(1S)-4-methanesulfonylguanyl-2-methyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-6,6,6-trifluoro-3-[formyl(hydroxy)amino]-2-isobutylhexanamide
-
Mus musculus
(2R,3S)-N-[(1S)-4-nitroguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-2-(cyclohexylmethyl)-3-[formyl(hydroxy)amino]hexanamide
-
Homo sapiens
(2R,3S)-N-[(1S)-4-nitroguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-2-(cyclohexylmethyl)-3-[formyl(hydroxy)amino]hexanamide
-
Mus musculus
(2R,3S)-N-[(1S)-4-nitroguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-2-(cyclohexylmethyl)-6,6,6-trifluoro-3-[formyl(hydroxy)amino]hexanamide
-
Homo sapiens
(2R,3S)-N-[(1S)-4-nitroguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-2-(cyclohexylmethyl)-6,6,6-trifluoro-3-[formyl(hydroxy)amino]hexanamide
-
Mus musculus
(2R,3S)-N-[(1S)-4-nitroguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-2-[(1S)-1-[formyl(hydroxy)amino]-2-phenylethyl]-4-methylpentanamide
-
Homo sapiens
(2R,3S)-N-[(1S)-4-nitroguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-2-[(1S)-1-[formyl(hydroxy)amino]-2-phenylethyl]-4-methylpentanamide
-
Mus musculus
(2R,3S)-N-[(1S)-4-nitroguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl(hydroxy)amino]-2-[5-methyl-2-thienylmethyl]hexanamide
-
Homo sapiens
(2R,3S)-N-[(1S)-4-nitroguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl(hydroxy)amino]-2-[5-methyl-2-thienylmethyl]hexanamide
-
Mus musculus
(2R,3S)-N-[(1S)-4-nitroguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl(hydroxy)amino]-4-methyl-2-[(4-methylcyclohexyl)methyl]hexanamide
-
Homo sapiens
(2R,3S)-N-[(1S)-4-nitroguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl(hydroxy)amino]-4-methyl-2-[(4-methylcyclohexyl)methyl]hexanamide
-
Mus musculus
(2R,3S)-N-[(1S)-4-nitroguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl(hydroxy)amino]-4-methyl-2-[(4-methylcyclohexyl)methyl]pentanamide
-
Homo sapiens
(2R,3S)-N-[(1S)-4-nitroguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl(hydroxy)amino]-4-methyl-2-[(4-methylcyclohexyl)methyl]pentanamide
-
Mus musculus
(2R,3S)-N-[(1S,2R)-4-nitroguanyl-2-methyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl(hydroxy)amino]-2-isobutylhexanamide
-
Homo sapiens
(2R,3S)-N-[(1S,2R)-4-nitroguanyl-2-methyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl]-3-[formyl(hydroxy)amino]-2-isobutylhexanamide
-
Mus musculus
(2R,3S)-N-{(1R)-4-nitroguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl}-3-[formyl(hydroxy)amino]-2-isobutylhexanamide
-
Homo sapiens
(2R,3S)-N-{(1R)-4-nitroguanyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butyl}-3-[formyl(hydroxy)amino]-2-isobutylhexanamide
-
Mus musculus
(2S)-2-amino-5-({(E)-amino[(methylsulfonyl)imino]-methyl}amino)-N-(1,3-thiazol-2-yl)pentanamide hydrochloride
-
Homo sapiens
(2S)-2-amino-5-({(E)-amino[(methylsulfonyl)imino]-methyl}amino)-N-(1,3-thiazol-2-yl)pentanamide hydrochloride
-
Mus musculus
(2S)-2-[(tert-butoxycarbonyl)amino]-5-({(Z)-(methyl-sulfanyl)[(methylsulfonyl)imino]methyl}amino)pentanoic acid
-
Homo sapiens
(2S)-2-[(tert-butoxycarbonyl)amino]-5-({(Z)-(methyl-sulfanyl)[(methylsulfonyl)imino]methyl}amino)pentanoic acid
-
Mus musculus
(2S,3R)-2-[(tert-butoxycarbonyl)amino]-5-{[imino(2-oxido-2-oxohydrazino)methyl]amino}-3-methylpentanoic acid (3R) Nalpha-boc-Ngamma-nitro-3-methyl L-arginine
-
Homo sapiens
(2S,3R)-2-[(tert-butoxycarbonyl)amino]-5-{[imino(2-oxido-2-oxohydrazino)methyl]amino}-3-methylpentanoic acid (3R) Nalpha-boc-Ngamma-nitro-3-methyl L-arginine
-
Mus musculus
(2S,3R)-2-{[(benzyloxy)carbonyl]amino}-3-methyl-5-({(Z)-(methylsulfanyl)[(methylsulfonyl)imino]methyl}-amino)pentanoic acid
-
Homo sapiens
(2S,3R)-2-{[(benzyloxy)carbonyl]amino}-3-methyl-5-({(Z)-(methylsulfanyl)[(methylsulfonyl)imino]methyl}-amino)pentanoic acid
-
Mus musculus
(2S,3R)-5-methanesulfonylguanyl-2-[((2R)-2-[(1S)-1-[formyl(hydroxy)amino]ethyl]-4-methylpentanoyl)amino]-3-methyl-N-(1,3-thiazol-2-yl)pentanamide
-
Homo sapiens
(2S,3R)-5-methanesulfonylguanyl-2-[((2R)-2-[(1S)-1-[formyl(hydroxy)amino]ethyl]-4-methylpentanoyl)amino]-3-methyl-N-(1,3-thiazol-2-yl)pentanamide
-
Mus musculus
(2S,3R)-5-nitroguanyl-2-[((2R)-2-[(1S)-1-[formyl(hydroxy)amino]ethyl]-4-methylpentanoyl)amino]-3-methyl-N-(1,3-thiazol-2-yl)pentanamide
-
Homo sapiens
(2S,3R)-5-nitroguanyl-2-[((2R)-2-[(1S)-1-[formyl(hydroxy)amino]ethyl]-4-methylpentanoyl)amino]-3-methyl-N-(1,3-thiazol-2-yl)pentanamide
-
Mus musculus
benzyl (1S,2R)-4-({(E)-amino[(methylsulfonyl)imino]-methyl}amino)-2-methyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butylcarbamate
-
Homo sapiens
benzyl (1S,2R)-4-({(E)-amino[(methylsulfonyl)imino]-methyl}amino)-2-methyl-1-[(1,3-thiazol-2-ylamino)carbonyl]butylcarbamate
-
Mus musculus
GW 3333 N-hydroxyformamide TACE inhibitor Homo sapiens
L-NG-(2-pyridylsulfonyl)arginine2-aminothiazole amide hydochloride
-
Homo sapiens
L-NG-(2-pyridylsulfonyl)arginine2-aminothiazole amide hydochloride
-
Mus musculus
L-NG-nitroarginine 2-aminothiazole amide dihydrochloride
-
Homo sapiens
L-NG-nitroarginine 2-aminothiazole amide dihydrochloride
-
Mus musculus
tert-butyl (1S,2R)-4-{[imino(2-oxido-2-oxohydrazino)-methyl]amino}-2-methyl-1-[1,3-thiazol-2-ylaminocarbonyl]butylcarbamate
-
Homo sapiens
tert-butyl (1S,2R)-4-{[imino(2-oxido-2-oxohydrazino)-methyl]amino}-2-methyl-1-[1,3-thiazol-2-ylaminocarbonyl]butylcarbamate
-
Mus musculus
tert-butyl (2S,3R)-2-{[(benzyloxy)carbonyl]amino}-3-methyl-4-pentenoate
-
Homo sapiens
tert-butyl (2S,3R)-2-{[(benzyloxy)carbonyl]amino}-3-methyl-4-pentenoate
-
Mus musculus
tert-butyl (2S,3R)-2-{[(benzyloxy)carbonyl]amino}-5-amino-3-methylpentanoate
-
Homo sapiens
tert-butyl (2S,3R)-2-{[(benzyloxy)carbonyl]amino}-5-amino-3-methylpentanoate
-
Mus musculus
tert-butyl (2S,3R)-2-{[(benzyloxy)carbonyl]amino}-5-azido-3-methylpentanoate
-
Homo sapiens
tert-butyl (2S,3R)-2-{[(benzyloxy)carbonyl]amino}-5-azido-3-methylpentanoate
-
Mus musculus
tert-butyl (2S,3R)-2-{[(benzyloxy)carbonyl]amino}-5-hydroxy-3-methylpentanoate
-
Homo sapiens
tert-butyl (2S,3R)-2-{[(benzyloxy)carbonyl]amino}-5-hydroxy-3-methylpentanoate
-
Mus musculus
tert-butyl(1S)-4-({(Z)-(methylsulfanyl)[(methylsulfonyl)-imino]methyl}amino)-1-[(1,3-thiazol-2-ylamino)carbonyl]butylcarbamate
-
Homo sapiens
tert-butyl(1S)-4-({(Z)-(methylsulfanyl)[(methylsulfonyl)-imino]methyl}amino)-1-[(1,3-thiazol-2-ylamino)carbonyl]butylcarbamate
-
Mus musculus
[((3R,4S)-4-{[(benzyloxy)carbonyl]}-4-carboxy-3-methylbutyl)amino](imino)methanaminium nitrate (3R) 3-methyl L-arginine nitric acid salt
-
Homo sapiens
[((3R,4S)-4-{[(benzyloxy)carbonyl]}-4-carboxy-3-methylbutyl)amino](imino)methanaminium nitrate (3R) 3-methyl L-arginine nitric acid salt
-
Mus musculus

Localization

Localization Comment Organism GeneOntology No. Textmining
membrane membrane-bound Mus musculus 16020
-
membrane membrane-bound Homo sapiens 16020
-

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Mus musculus
-
-
-
Rattus norvegicus
-
-
-
Rattus norvegicus
-
rat
-
Rattus norvegicus Lewis
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
blood
-
Mus musculus
-
blood
-
Homo sapiens
-
endothelium
-
Mus musculus
-
endothelium
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
75kDaTNFR2 + H2O
-
Homo sapiens ?
-
?
p55 TNFR1 + H2O
-
Mus musculus ?
-
?
p55 TNFR1 + H2O
-
Homo sapiens ?
-
?
proTNF-alpha + H2O
-
Mus musculus soluble TNF-alpha
-
?
proTNF-alpha + H2O
-
Homo sapiens soluble TNF-alpha
-
?
transforming growth factor alpha + H2O
-
Mus musculus ?
-
?
transforming growth factor alpha + H2O
-
Homo sapiens ?
-
?
transforming growth factor alpha + H2O
-
Rattus norvegicus ?
-
?
transforming growth factor alpha + H2O
-
Rattus norvegicus Lewis ?
-
?