2.4.2.17 (4E)-4-[(4-chlorophenyl)(hydroxy)methylidene]-1-(pyridin-3-ylmethyl)-5-(3,4,5-trimethoxyphenyl)pyrrolidine-2,3-dione binds to the cavity between the domains I and II. The terminal chlorobenzoyl group of 1 makes hydrophobic interactions with the amphiphilic pocket near the phosphoribosyl pyrophosphate binding site 76506 2.4.2.17 1,2,4-Triazole-3-alanine - 29236 2.4.2.17 1-(5-phospho-alpha-D-ribosyl)-ATP product inhibition, competitive to both substrates 51101 2.4.2.17 1-(5-phospho-beta-D-ribosyl)-ATP product inhibition 44706 2.4.2.17 1-[(5,6-diphenyl-1,2,4-triazin-3-yl)sulfanyl]-3-(1,3-thiazol-2-yl)propan-2-one most potent inhibitor, spans the PR-ATP binding site, exhibits greater than 50% inhibition at 0.01 mM, 40% inhibition at 0.001 mM 39577 2.4.2.17 2-([7-[(3-hydroxyphenyl)amino]-4-nitro-2,1,3-benzoxadiazol-5-yl]amino)-5-nitrophenol exhibits 46% inhibition 76537 2.4.2.17 2-([7-[(3-hydroxyphenyl)amino]-4-nitro-2,1,3-benzoxadiazol-5-yl]amino)-5-nitrophenol has whole-cell activity at 0.012 mM 76537 2.4.2.17 2-methyl-L-histidine - 112427 2.4.2.17 2-thiazol-DL-alanine - 112455 2.4.2.17 2-[(2-bromo-3,5-dinitrophenyl)carbonyl]-N-phenylhydrazinecarboxamide exhibits 71% inhibition 39582 2.4.2.17 2-[(2-bromo-3,5-dinitrophenyl)carbonyl]-N-phenylhydrazinecarboxamide has whole-cell activity at 0.025 mM 39582 2.4.2.17 4-methoxybenzyl 2-methyl-5-oxo-4,7-dithiophen-2-yl-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate interacts with the phosphoribosyl diphosphate binding site but less strongly compared to compound 6 , exhibits greater than 50% inhibition at 0.01 mM 76644 2.4.2.17 5-phospho-alpha-D-ribose 1-diphosphate noncompetitive inhibitor with respect to both substrates in the reaction producing ATP and 5-phospho-alpha-D-ribose 1-diphosphate 158 2.4.2.17 adenine competitive to ATP and 5-phospho-alpha-D-ribose 1-diphosphate 144 2.4.2.17 ADP competitive to ATP, in the presence of histidine inhibition by AMP and ADP becomes positively cooperative and much more potent 13 2.4.2.17 ADP - 13 2.4.2.17 ADP competitive to ATP 13 2.4.2.17 ADP orthosteric inhibition 13 2.4.2.17 Ag+ - 75 2.4.2.17 AMP competitive inhibitor to 5-phospho-alpha-D-ribose 1-diphosphate, in the presence of histidine inhibition by AMP and ADP becomes positively cooperative and much more potent 30 2.4.2.17 AMP linear competitive inhibitor with respect to ATP, stabilizes the enzyme to thermal inactivation, protect the ordered enzymatic structure against thermodenaturation 30 2.4.2.17 AMP inhibits the enzyme complex together with histidine to the T-state 30 2.4.2.17 AMP binding structure and inhibition mode 30 2.4.2.17 AMP competitive 30 2.4.2.17 AMP competitive to ATP 30 2.4.2.17 AMP competitive inhibition 30 2.4.2.17 AMP - 30 2.4.2.17 AMP AMP is an inhibitor of subunit HisGS 30 2.4.2.17 AMP about 10% inhibition at 0.25 mM 30 2.4.2.17 ATP inhibits the reaction at high concentrations 4 2.4.2.17 beta,gamma-methylene-ATP competitive with respect to N-1-(5-phosphoribosyl)-ATP, noncompetitive with respect to diphosphate; inhibitor of the reaction producing ATP and 5-phospho-alpha-D-ribose 1-diphosphate 3802 2.4.2.17 beta-(2-thiazolyl)-DL-alanine - 209516 2.4.2.17 Ca2+ moderate inhibitory effect 15 2.4.2.17 Cd2+ - 52 2.4.2.17 Co2+ - 23 2.4.2.17 Cu2+ - 19 2.4.2.17 dicoumarol competitive with respect to ATP, inhibitor in both directions, diminishes yield of phosphoribosyladenosine triphosphate by acting as parasite substrate 754 2.4.2.17 dinitrophenol diminishes yield of phosphoribosyladenosine triphosphate by acting as parasite substrate 4519 2.4.2.17 diphosphate non competitive to both substrates 17 2.4.2.17 EDTA - 21 2.4.2.17 EDTA moderate inhibitory effect 21 2.4.2.17 ethyl [(6-nitro-1,3-benzothiazol-2-yl)amino](oxo)acetate exhibits 39% inhibition 154924 2.4.2.17 Fe2+ - 25 2.4.2.17 Fe3+ - 70 2.4.2.17 Guanosine 5'-diphosphate-3'-diphosphate in presence of partially inhibiting concentrations of histidine guanosine 5'-diphosphate-3'-diphosphate becomes a potent inhibitor of the residual activity of ATP phosphoribosyltransferase, no inhibition in absence of histidine, inhibition is slowly reversible 44202 2.4.2.17 Hg2+ - 33 2.4.2.17 Hg2+ moderate inhibitory effect 33 2.4.2.17 histidine feedback inhibition, inhibits the enzyme complex together with ATP to the T-state, no inhibition of mutants E130A and Y268F/Y269F 1063 2.4.2.17 histidine noncompetitive feedback inhibition 1063 2.4.2.17 histidine noncompetitive 1063 2.4.2.17 L-histidine feed-back inhibition; reversed by Hg2+, p-hydroxymercuribenzoate, methylmercuric bromide, Ni2+; the L-configuration is essential, substitution of alpha-amino group appreciably reduces inhibition, non competitive inhibitor with respect to both substrates 349 2.4.2.17 L-histidine feed-back inhibition; stabilizes the enzyme to thermal inactivation, protects the ordered enzymatic structure against thermodenaturation, no interaction with binding sites 349 2.4.2.17 L-histidine feed-back inhibition 349 2.4.2.17 L-histidine feed-back inhibition; inhibits reverse reaction cooperatively and completely 349 2.4.2.17 L-histidine feed-back inhibition; feed-back inhibition 349 2.4.2.17 L-histidine allosteric inhibition, synergistically favored by AMP; feed-back inhibition 349 2.4.2.17 L-histidine allosteric inhibitor, inhibition dependent on pH, uncompetitive versus ATP, noncompetitive versus 5-phospho-alpha-D-ribosyl diphosphate 349 2.4.2.17 L-histidine noncompetitive, alkaline pH decreases the inhibitory effect 349 2.4.2.17 L-histidine - 349 2.4.2.17 L-histidine allosterical inhibition 349 2.4.2.17 L-histidine complete inhibition at 0.1 mM 349 2.4.2.17 L-histidine in the presence of histidine, subunit HisZ mediates allosteric inhibition of the enzyme 349 2.4.2.17 L-histidine complete inhibition at 1 mM, about 10% inhibition at 0.25 mM 349 2.4.2.17 L-histidine noncompetitive inhibition, subunit HisZ activates subunit HisGS and mediates allosteric inhibition by histidine 349 2.4.2.17 L-histidine histidine allosterically inhibits the enzyme in a negative feedback control mechanism 349 2.4.2.17 Methylmercuric bromide - 30185 2.4.2.17 Mg2+ at high concentrations, Ki = 23 mM 6 2.4.2.17 Mn2+ moderate inhibitory effect 11 2.4.2.17 additional information carbonylcyanide m-chlorophenylhydrazone, which is a potent inhibitor of several enzymes with adenine-containing substrates or coenzymes has no effect 2 2.4.2.17 N-ethylmaleimide - 49 2.4.2.17 N-[3-[(6-nitro-1,3-benzothiazol-2-yl)amino]-3-oxo-1-phenylpropyl]benzamide occupies only the phosphoribosyl diphosphate binding site, exhibits greater than 50% inhibition at 0.01 mM, 35% inhibition at 0.001 mM 39628 2.4.2.17 Ni2+ - 38 2.4.2.17 p-hydroxymercuribenzoate - 98 2.4.2.17 Pentachlorophenol competitive to ATP, inhibitor in both directions, diminishes yield of phosphoribosyladenosine triphosphate by acting as parasite substrate 1077 2.4.2.17 Zn2+ - 14 2.4.2.17 Zn2+ moderate inhibitory effect 14