3.4.16.4 (2,3)-alpha-methylene benzylpenicillin modeling of enzyme-inhibitor complex 95404 3.4.16.4 (2-phenylethyl)boronic acid 91% residual activity at 1 mM 158794 3.4.16.4 (2R)-2-amino-7-oxo-7-[(4,4,4-trifluoro-3-oxobutan-2-yl)amino]heptanoic acid i.e. D-alpha-aminopimelyl-(1,1,1-trifluoro-3-amino)butan-2-one 199477 3.4.16.4 (3-aminophenyl)boronic acid 20% residual activity at 1 mM 158888 3.4.16.4 (3-nitrophenyl)boronic acid 82% residual activity at 1 mM 158885 3.4.16.4 (3H)benzylpenicillin - 132386 3.4.16.4 (3R,5R)-3-(furyl-2')-4-dethia-4-oxa-penam - 67265 3.4.16.4 (3R,5R,6R)-6-methyl-3-(furyl-2')-4-dethia-4-oxa-penam - 67263 3.4.16.4 (3R,5R,6S)-6-methyl-3-(furyl-2')-4-dethia-4-oxa-penam - 67262 3.4.16.4 (3R,5S)-3-(furyl-2')-4-dethia-4-oxa-penam - 67264 3.4.16.4 (3R,5S,6R)-3-benzyloxycarbonyl-6-methyl-4-dethia-4-oxa-penam - 67269 3.4.16.4 (3R,5S,6R)-6-methyl-3-(furyl-2')-4-dethia-4-oxa-penam - 67261 3.4.16.4 (3S,5R)-3-(furyl-2')-4-dethia-4-oxa-penam - 67268 3.4.16.4 (3S,5R,6S)-3-benzyloxycarbonyl-6-methyl-4-dethia-4-oxa-penam - 67270 3.4.16.4 (3S,5R,6S)-6-methyl-3-(furyl-2')-4-dethia-4-oxa-penam - 67266 3.4.16.4 (3S,5S)-3-(furyl-2')-4-dethia-4-oxa-penam - 141818 3.4.16.4 (3S,5S,6R)-6-methyl-3-(furyl-2')-4-dethia-4-oxa-penam - 67267 3.4.16.4 (4-phenoxyphenyl)boronic acid 98% residual activity at 1 mM 158880 3.4.16.4 (5-acetylthiophen-2-yl)boronic acid 88% residual activity at 1 mM 158902 3.4.16.4 (5-chlorothiophen-2-yl)boronic acid 91% residual activity at 1 mM 158903 3.4.16.4 (5-cyanothiophen-2-yl)boronic acid 95% residual activity at 1 mM 158936 3.4.16.4 (5-formylthiophen-2-yl)boronic acid 99% residual activity at 1 mM 158796 3.4.16.4 (5R,6R)-6-[[(6S)-6-carboxy-6-(glycylamino)hexanoyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid - 138380 3.4.16.4 (6R,7R)-3-[(acetyloxy)methyl]-7-[(6S)-6-carboxy-6-(glycylamino)hexanoyl]amino-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid - 141817 3.4.16.4 1,2-Ethanedithiol - 15437 3.4.16.4 1,3-propanedithiol - 32001 3.4.16.4 1-benzothiophen-2-ylboronic acid 86% residual activity at 1 mM 158963 3.4.16.4 2,1-benzoxaborol-1(3H)-ol 45% residual activity at 1 mM 40217 3.4.16.4 2,3-dimercapto-1-propane-sulfonic acid - 99798 3.4.16.4 2,3-dimercapto-1-propanol - 5897 3.4.16.4 2-Methylpenem - 91115 3.4.16.4 2-Phenylpenem - 97581 3.4.16.4 3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoic acid 38% residual activity at 0.5 mM 158967 3.4.16.4 3-(acetylamino)-5-(dihydroxyboranyl)benzoic acid 50% residual activity at 1 mM 79229 3.4.16.4 3-(benzoylamino)-5-(dihydroxyboranyl)benzoic acid 9% residual activity at 1 mM 79230 3.4.16.4 3-(dihydroxyboranyl)-4-[(phenylacetyl)amino]benzoic acid 80% residual activity at 1 mM 158921 3.4.16.4 3-(dihydroxyboranyl)-5-[(2,6-dimethoxybenzoyl)amino]benzoic acid 84% residual activity at 1 mM 158974 3.4.16.4 3-(dihydroxyboranyl)-5-[(phenoxyacetyl)amino]benzoic acid 2% residual activity at 1 mM 79242 3.4.16.4 3-(dihydroxyboranyl)-5-[(thiophen-2-ylacetyl)amino]benzoic acid 5% residual activity at 1 mM 79243 3.4.16.4 3-(dihydroxyboranyl)-5-[(thiophen-2-ylcarbonyl)amino]benzoic acid 18% residual activity at 1 mM 79011 3.4.16.4 3-(dihydroxyboryl)-5-(2-methoxybenzamido)benzoic acid 10% residual acvtivity at 1 mM 80613 3.4.16.4 3-(dihydroxyboryl)-5-(2-phenylacetamido)benzoic acid 3% residual acvtivity at 1 mM 80612 3.4.16.4 3-(dihydroxyboryl)benzoic acid 20% residual acvtivity at 1 mM 80611 3.4.16.4 3-(N-glycyl-L-cysteinyl)-N-ethylpropionamide - 60683 3.4.16.4 3-(trifluoroacetyl)benzoic acid 60% residual activity at 1 mM 158968 3.4.16.4 3-formylbenzoic acid 77% residual activity at 1 mM 158785 3.4.16.4 4-(dihydroxyboranyl)benzoic acid 85% residual activity at 1 mM 158802 3.4.16.4 4-chloromercuribenzoate complete inhibition at 1 mM 388 3.4.16.4 4-[(phenylacetyl)amino]-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoic acid 81% residual activity at 1 mM 158897 3.4.16.4 5-(dihydroxyboranyl)thiophene-2-carboxylic acid 57% residual activity at 1 mM 158995 3.4.16.4 6-beta(alpha-N-acetyl-L-lysyl)-aminopenicillanic acid - 141815 3.4.16.4 6-beta(D-alpha-aminopimelyl)-aminopenicillanic acid - 37401 3.4.16.4 6-beta(D-alpha-aminosuberyl)-aminopenicillanic acid - 67259 3.4.16.4 6-beta(N-acetyl-L-alanyl-gamma-D-glutamyl-L-alanyl)-aminopenicillanic acid - 67260 3.4.16.4 7-(phenoxyacetamido)-3-desacetoxycephalosporamic acid - 97666 3.4.16.4 7-beta(alpha-N-acetyl-L-lysyl)-aminocephalosporanic acid - 141816 3.4.16.4 7-beta(D-alpha-aminopimelyl)-aminocephalosporanic acid - 37402 3.4.16.4 alpha-N-glycyl-epsilon-N-acetyl-L-lysine inhibits hydrolysis of 3-(N-glycyl-L-cysteinyl)-propanoyl-D-alanyl-D-thiolactate 132384 3.4.16.4 amoxicillin - 1774 3.4.16.4 ampicillin - 191 3.4.16.4 ampicillin complete inhibition at 0.57 mM, 95% inhibition at 0.285 mM 191 3.4.16.4 arylakylidene imino-thiazolidin-4-ones 10 86% inhibition 132399 3.4.16.4 arylakylidene imino-thiazolidin-4-ones 11 82% inhibition 132400 3.4.16.4 arylakylidene imino-thiazolidin-4-ones 12 64% inhibition 132401 3.4.16.4 arylakylidene imino-thiazolidin-4-ones 13 83% inhibition 132402 3.4.16.4 arylakylidene imino-thiazolidin-4-ones 16 100% inhibition 132403 3.4.16.4 arylakylidene imino-thiazolidin-4-ones 17 100% inhibition 132404 3.4.16.4 arylakylidene imino-thiazolidin-4-ones 18 96% inhibition 132405 3.4.16.4 arylakylidene imino-thiazolidin-4-ones 19 84% inhibition 132406 3.4.16.4 arylakylidene imino-thiazolidin-4-ones 5 89% inhibition 132395 3.4.16.4 arylakylidene imino-thiazolidin-4-ones 6 92% inhibition 132396 3.4.16.4 arylakylidene imino-thiazolidin-4-ones 8 99% inhibition 132397 3.4.16.4 arylakylidene imino-thiazolidin-4-ones 9 85% inhibition 132398 3.4.16.4 arylalkylidene rhodanine derivative 1 88% inhibition 132392 3.4.16.4 arylalkylidene rhodanine derivative 2 95% inhibition 35812 3.4.16.4 arylalkylidene rhodanine derivative 2 94% inhibition 35812 3.4.16.4 arylalkylidene rhodanine derivative 2 75% inhibition 35812 3.4.16.4 arylalkylidene rhodanine derivative 3 83% inhibition 132393 3.4.16.4 arylalkylidene rhodanine derivative 4 95% inhibition 132394 3.4.16.4 ayercillin dipeptide-releasing activity is penicillin sensitive 18062 3.4.16.4 benzylpenicillin - 348 3.4.16.4 benzylpenicillin ester-linked to serins 348 3.4.16.4 benzylpenicillin IC50: 0.00002 mg/ml, inhibition of the enzyme influences production of peptidoglycan precursors internally 348 3.4.16.4 benzylpenicillin classical non-specific beta-lactam 348 3.4.16.4 benzylpenicillin 80% inhibition at 0.1 mg/ml 348 3.4.16.4 beta-lactam R39 has a high beta-lactam binding activity 20161 3.4.16.4 beta-lactam - 20161 3.4.16.4 beta-lactams kinetic constants 12895 3.4.16.4 beta-lactams - 12895 3.4.16.4 biphenyl-4,4'-diyldiboronic acid 97% residual activity at 0.1 mM 158849 3.4.16.4 Boc-gamma-D-Glu-L-Lys-(Cbz)-D-boroAla-(-)-pinanediol effective inhibitor of the D-alanine CPase activity of PBP5 60684 3.4.16.4 Ca2+ - 15 3.4.16.4 Ca2+ 1 mM, no residual activity 15 3.4.16.4 carbenicillin - 1436 3.4.16.4 cefaclor - 2601 3.4.16.4 cefadroxil - 6128 3.4.16.4 cefalexin - 159775 3.4.16.4 cefalothin - 7661 3.4.16.4 cefmetazole - 13156 3.4.16.4 cephalexin - 1026 3.4.16.4 cephalosporidin - 92878 3.4.16.4 cephalosporin - 20181 3.4.16.4 cephalosporin with glycyl-L-alpha-amino-epsilon-pimelyl side-chain, this beta lactam might be a better antibiotic than a non-specific counterpart 20181 3.4.16.4 cephalosporin C classical non-specific beta-lactam 478 3.4.16.4 cephalothin - 354 3.4.16.4 cetyltrimethylammonium bromide - 2265 3.4.16.4 Cloxacillin - 1440 3.4.16.4 Co2+ - 23 3.4.16.4 Cu2+ - 19 3.4.16.4 D-Ala - 291 3.4.16.4 D-Ala(P,O)D-Ala acts as slow binding inhibitor 141814 3.4.16.4 D-Ala(P,O)D-Phe acts as slow binding inhibitor 141813 3.4.16.4 D-alpha-phenylpropionate - 25218 3.4.16.4 D-cysteine - 1350 3.4.16.4 D-hexahydromandelate - 25216 3.4.16.4 D-mandelate - 3457 3.4.16.4 D-phenyllactate - 5237 3.4.16.4 Delta2-(and Delta3)-Deacetoxy-7-phenylacetamidocephalosporanates - 97879 3.4.16.4 depsipeptides - 100455 3.4.16.4 diacetyl-L-Lys-D-Ala - 44029 3.4.16.4 Dicloxacillin - 93173 3.4.16.4 diisopropyl fluorophosphate 1 mM, 28% inhibition 244 3.4.16.4 dithiothreitol - 45 3.4.16.4 EDTA 4 mM, complete loss of activity. Ativity may be restored in presence of 8 mM Zn2+ 21 3.4.16.4 epsilon-N-glycyl-alpha-N-acetyl-L-alanyl-D-isoglutaminyl-L-lysine inhibits hydrolysis of 3-(N-glycyl-L-cysteinyl)-propanoyl-D-alanyl-D-thiolactate 132385 3.4.16.4 ethanol - 69 3.4.16.4 FeSO4 - 655 3.4.16.4 formaldehyde 1 mM, 53% inhibition 130 3.4.16.4 glycolyl-L-Phe - 25217 3.4.16.4 Hg2+ - 33 3.4.16.4 iodoacetamide 1 mM, 20% inhibition 67 3.4.16.4 L-cysteine - 74 3.4.16.4 Mercaptosuccinic acid - 30799 3.4.16.4 Methicillin - 2412 3.4.16.4 Mg2+ - 6 3.4.16.4 Mg2+ 1 mM, no residual activity 6 3.4.16.4 Moenomycin inhibits the glycosyl transferase activity 3650 3.4.16.4 Moenomycin - 3650 3.4.16.4 additional information serine enzyme not inhibited by PMSF 2 3.4.16.4 additional information no inhibition: EDTA 2 3.4.16.4 additional information no inhibition: penicillin G, ampicillin, cephalosporin C 2 3.4.16.4 additional information inhibition studies 2 3.4.16.4 additional information no significant inhibition by arylalkylidene rhodanine derivative 1 and 3 respectively and arylakylidene imino-thiazolidin-4-ones 6, 8, 13, 16, 17 and 19 respectively 2 3.4.16.4 additional information no significant inhibition by arylakylidene imino-thiazolidin-4-ones 7, 14 and 15 respectively 2 3.4.16.4 additional information no significant inhibition by arylalkylidene rhodanine derivative 1, 3 and 4 respectively and arylakylidene imino-thiazolidin-4-ones 5 to 19 2 3.4.16.4 additional information not inhibited by methyl 3-(dihydroxyboryl)-5-(2-phenylacetamido)benzoate 2 3.4.16.4 N,N-diacetyl-L-Lys-D-Ala-D-Ala inhibition of PBP3 by its own substrate above a ligand concentration of 15 mM 132387 3.4.16.4 N-(glycyl)-D,L-alpha-aminocaprylic acid inhibits hydrolysis of 3-(N-glycyl-L-cysteinyl)-propanoyl-D-alanyl-D-thiolactate 132383 3.4.16.4 N-benzoyl-beta-sultam time-dependent, irreversible active site directed inhibitor, the rate of inactivation is first order with respect to beta-sultam concentration and second order rate constants show dependence on pH 132390 3.4.16.4 N-Chlorosuccinimide 1 mM, 50% inhibition 6001 3.4.16.4 N-p-chloro-beta-sultam - 132389 3.4.16.4 N-p-methoxy-beta-sultam least effective inhibitor 132391 3.4.16.4 N-p-nitro-beta-sultam - 132388 3.4.16.4 Nalpha-tert-butoxycarbonyl-Nepsilon-benzyloxycarbonyl-L-Lys-D-Ala-D-Ala substrate inhibition above 30 mM 53983 3.4.16.4 NEM 1 mM, complete inhibition 89 3.4.16.4 nitrocefin - 326 3.4.16.4 nocardicin A - 6570 3.4.16.4 Oxacillin - 1030 3.4.16.4 Oxyimino-DELTA3-cephalosporins syn- and anti-isomers 46491 3.4.16.4 p-hydroxymercuribenzoate 1 mM, complete inhibition 98 3.4.16.4 Pb2+ - 139 3.4.16.4 Penicillanate - 94662 3.4.16.4 penicillin kinetic model of interaction 2664 3.4.16.4 penicillin - 2664 3.4.16.4 penicillin binds covalently to Ser36, Bacillus subtilis, Bacillus stearothermophilus 2664 3.4.16.4 penicillin having the glycyl-L-alpha-amino-epsilon-pimelyl side-chain of Streptomyces strain R61 peptidoglycan, this beta lactam might be the perfect antibiotic as compared to a non-specific counterpart 2664 3.4.16.4 penicillin the enzyme is sensitive to inhibition, penicillin-binding profile during development of spores, overview 2664 3.4.16.4 penicillin G - 181 3.4.16.4 penicillin G 100% inhibition 181 3.4.16.4 Penicillin V - 2755 3.4.16.4 phenoxymethylpenicillin - 15914 3.4.16.4 phenyl glycyl-L-alpha-aminopimelyl-epsilon-(D-2-aminoethyl)phosphonate - 117688 3.4.16.4 phenylboronic acid 1 mM, 26% inhibition 2577 3.4.16.4 phenylboronic acid 50% residual activity at 0.5 mM 2577 3.4.16.4 piperacillin - 766 3.4.16.4 sulfazecine - 47501 3.4.16.4 thiophen-2-ylboronic acid 88% residual activity at 1 mM 158831 3.4.16.4 thiosalicylic acid - 45938 3.4.16.4 Vancomycin vancomycin derivatives inhibit the glycosyl transferase activity 2101 3.4.16.4 Zn2+ - 14 3.4.16.4 Zn2+ 1 mM, no residual activity 14 3.4.16.4 [3-([[5-(dimethylamino)naphthalen-1-yl]sulfonyl]amino)phenyl]boronic acid 60% residual activity at 0.5 mM 158830 3.4.16.4 [3-[(2,6-dimethoxybenzoyl)amino]-5-(methoxycarbonyl)thiophen-2-yl]boronic acid 98% residual activity at 1 mM 158877