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3.4.21.105: rhomboid protease

This is an abbreviated version!
For detailed information about rhomboid protease, go to the full flat file.

Word Map on EC 3.4.21.105

Reaction

cleaves type-1 transmembrane domains using a catalytic dyad composed of serine and histidine that are contributed by different transmembrane domains =

Synonyms

AAR, AarA, AqRho, Derlin-1, EhROM1, GlpG, GlpP, intramembrane protease, microneme rhomboid protease, More, paGlpG, PARL, PBANKA_110650, PbROM1, Pcp1, Pcp1/Rbd1, pfROM4, presenilin associated rhomboid like protein, presenilin-associated rhomboid-like, presenilin-associated rhomboid-like protein, presenilins-associated rhomboid-like protein, PSARL, Rbd1, Rbd1p, RBL1, RBL10, RBL11, RBL12, RBL2, RBL3, RBL4, RBL5, RBL6, RBL7, RBL8, RBL9, Rhbdd1, RHBDL, RHBDL2, RHBDL4, RHDBL-2, Rho, RHO-1, rho-4, Rho-7, RhoII, Rhomboid, Rhomboid 4, rhomboid intramembrane protease, rhomboid Pcp1/Rbd1, rhomboid peptidase Pcp1, rhomboid protease, Rhomboid protease AarA, Rhomboid protease glpG, Rhomboid protease gluP, rhomboid protease Pcp1, rhomboid protease PSARL, Rhomboid protein, rhomboid protein 1, rhomboid protein 4, rhomboid pseudoprotease, rhomboid serine protease, rhomboid-1, rhomboid-1 protease, rhomboid-2, rhomboid-3, rhomboid-4, rhomboid-like protein, rhomboid-like protein 10, rhomboid-related protein 4, rhomboid-type protease Pcp1, ROM1, ROM4, ROM5, Spitz protease, TgROM1, TgROM2, TgROM3, TgROM4, TgROM5, Ygr101w, Yqgp

ECTree

     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.21 Serine endopeptidases
                3.4.21.105 rhomboid protease

Inhibitors

Inhibitors on EC 3.4.21.105 - rhomboid protease

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(3S,4S)-1-[(4-chlorophenyl)sulfonyl]-3-methyl-4-phenylazetidin-2-one
(3S,4S)-3-butyl-4-(pent-4-yn-1-yl)oxetan-2-one
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(3S,4S)-3-methyl-1-[(4-methylphenyl)sulfonyl]-4-phenylazetidin-2-one
-
-
1,2-dihexanoyl-sn-glycero-3-phosphocholine
-
1,2-dimyristoyl-sn-glycero-3-phosphocholine additionally added, paGlpG purified in detergent causes 37% reduction in activity
1,2-dimyristoyl-sn-glycero-3-phosphocholine
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paGlpG purified in detergent causes 5% reduction in activity
1-(2,3-dihydro-4H-1,4-benzoxazin-4-yl)-3,3,3-trifluoro-2-(trifluoromethyl)propan-1-one
1-(biphenyl-3-ylsulfonyl)-4-phenylazetidin-2-one
1-(biphenyl-4-ylsulfonyl)-4-phenylazetidin-2-one
1-myristoyl-sn-glycero-3-phosphocholine
-
paGlpG purified in detergent causes 10% reduction in activity
1-palmitoyl-sn-glycero-3-phospho-rac-(1-glycerol)
-
paGlpG purified in detergent causes 20% reduction in activity
1-[(3'-methylbiphenyl-4-yl)sulfonyl]-4-phenylazetidin-2-one
1-[(3-bromophenyl)sulfonyl]-4-phenylazetidin-2-one
1-[(3-chlorophenyl)sulfonyl]-4-(2-phenylethyl)azetidin-2-one
1-[(3-chlorophenyl)sulfonyl]-4-(propan-2-yl)azetidin-2-one
1-[(4'-chlorobiphenyl-4-yl)sulfonyl]-4-phenylazetidin-2-one
1-[(4-bromophenyl)sulfonyl]-4-phenylazetidin-2-one
1-[(4-chlorophenyl)sulfonyl]-3-methylazetidin-2-one
1-[(4-methylphenyl)sulfonyl]-4-phenylazetidin-2-one
2-(benzyloxy)-5-chloro-4H-3,1-benzoxazin-4-one
2-(benzyloxy)-5-methyl-4H-3,1-benzoxazin-4-one
2-methylpropyl 2-oxo-4-phenylazetidine-1-carboxylate
beta-lactam inhibitor, forms a single bond to the catalytic serine and the carbonyl oxygen of the inhibitor faces away from the oxyanion hole. The hydrophobic N-substituent of the inhibitor points into a cavity within the enzyme, providing a structural explanation for the specificity of beta-lactams on rhomboid proteases. This same cavity probably represents the S2' substrate binding site
3,3,3-trifluoro-N-[(5-methyl-2-phenyl-2H-1,2,3-triazol-4-yl)methyl]-2-(trifluoromethyl)propanamide
3,3,3-trifluoro-N-[2-(propan-2-yloxy)phenyl]-2-(trifluoromethyl)propanamide
3,4-dichloro-1H-2-benzopyran-1-one
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-
3,4-dichloroisocoumarin
3-butyl-4-(pent-4-yn-1-yl)oxetan-2-one
-
3-methyl-1-[(4-methylphenyl)sulfonyl]-4-phenylazetidin-2-one
-
-
3-[(3-cholamidopropyl)-dimethylammonio]-1-propansulfonate
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1,2-dimyristoyl-sn-glycero-3-phosphocholine additionally added, paGlpG purified in detergent causes 37% reduction in activity
4-(2-chlorophenyl)-1-[(3-chlorophenyl)sulfonyl]azetidin-2-one
4-(3-bromophenyl)-1-[(3-chlorophenyl)sulfonyl]azetidin-2-one
4-chloro-7-nitro-3-[(5-phenylpentyl)oxy]-1H-2-benzopyran-1-one
inhibitor reacts with virtually all tested rhomboids
4-[(3-methyl-2-oxoazetidin-1-yl)sulfonyl]benzonitrile
7-amino-3-butoxy-4-chloro-1H-isochromen-1-one
-
7-amino-4-chloro-3-(2-phenylethoxy)-1H-isochromen-1-one
-
7-amino-4-chloro-3-methoxyisocoumarin
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7-amino-4-chloro-3-[(5-phenylpentyl)oxy]-1H-isochromen-1-one
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acetyl-L-Ile-L-Ala-L-Thr-L-Ala-chloromethylketone
-
inhibitor derived from the natural rhomboid substrate TatA from bacterium Providencia stuartii, binds in a substrate-like manner
acetyl-L-Phe-L-Ala-L-Thr-L-Ala-chloromethylketone
-
inhibitor derived from the natural rhomboid substrate TatA from bacterium Providencia stuartii, binds in a substrate-like manner
benzyl (2S)-1-[(4-methylphenyl)sulfonyl]-4-oxoazetidine-2-carboxylate
cyclopentyl 2-oxo-4-phenylazetidine-1-carboxylate
beta-lactam inhibitor, forms a single bond to the catalytic serine and the carbonyl oxygen of the inhibitor faces away from the oxyanion hole. The hydrophobic N-substituent of the inhibitor points into a cavity within the enzyme, providing a structural explanation for the specificity of beta-lactams on rhomboid proteases. This same cavity probably represents the S2' substrate binding site
dichloroisocoumarin
diisopropyl fluorophosphonate
irreversible inhibition; mechansim-based inhibitor
dodecyl maltoside
-
paGlpG purified in detergent causes 77% reduction in activity
N-(2,6-dimethylphenyl)-3,3,3-trifluoro-2-(trifluoromethyl)propanamide
n-nonyl-beta-D-glucoside
-
paGlpG purified in detergent causes 45% reduction in activity
N-[2-(cyclopentyloxy)phenyl]-3,3,3-trifluoro-2-(trifluoromethyl)propanamide
N-[2-(cyclopropylmethoxy)phenyl]-3,3,3-trifluoro-2-(trifluoromethyl)propanamide
phenyl 2-oxo-4-phenylazetidine-1-carboxylate
tert-butyl 2-[[3,3,3-trifluoro-2-(trifluoromethyl)propanoyl]amino]benzoate
additional information
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