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Chemical Compound Review

CHEMBL422849     5-[[4-[[(2S)-1-carboxy-3-oxo- propan-2...

Synonyms: AC1NS223
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Disease relevance of Inhibitor 3

  • The spinal cord ischemic tolerance induced by HBO preconditioning was attenuated when a CAT inhibitor, 3-amino-1,2,4-triazole,1 g/kg, was administered intraperitoneally 1 h before ischemia [1].
  • A protein-ligand X-ray crystal structure of inhibitor 3-bound HIV-1 protease (1.35 A resolution) revealed extensive interactions in the HIV protease active site including strong hydrogen bonding interactions with the backbone [2].
  • To investigate this, we have attempted to further characterise the suppression of bone formation by the potent bone resorption inhibitor 3-amino-1-hydroxypropylidine-1-bisphosphonate (AHPrBP) in ovariectomised adult female rats [3].
  • 6. Pretreatment with MK886 (5-lipoxygenase-activating protein inhibitor, 3 mg kg(-1)), CP 105696 (LTB(4) receptor antagonist; 3 mg kg(-1)) or dexamethasone (0.5 mg kg(-1)) inhibited the hypersensitivity from 1 to 5 h [4].
  • (Mono)ADP-ribosylation experiments with crude membranes in the presence of the (poly)ADP-ribosyltransferase inhibitor, 3-amino-benzamide, resulted in the detection of a cholera toxin substrate of 52 kDa and two pertussis toxin substrates, 33 and 39 kDa [5].

High impact information on Inhibitor 3

  • Tissue metalloproteinase inhibitor 3, clusterin, vitronectin, and serum albumin were the most common proteins observed in normal donor drusen whereas crystallin was detected more frequently in AMD donor drusen [6].
  • Structural basis for the inhibition of porcine pepsin by Ascaris pepsin inhibitor-3 [7].
  • Increasing the stationary concentration of UVB-induced DNA breaks by inhibition of repair in the presence of the adenosine diphosphoribose (ADPR)-transferase inhibitor 3-amino-benzamide suppressed the induction of c-fos [8].
  • However, the serpin PA inhibitory activity in extracts of both the normal brain and tumor is of the protease nexin I/PA inhibitor 3 type [9].
  • Herein, we show that inhibitor 3, in contrast to GM6001, had no effect on pro-MMP-2 activation by MT1-MMP [10].

Chemical compound and disease context of Inhibitor 3

  • This study examined the effectiveness of the cyclooxygenase/lipoxygenase inhibitor 3-amino-1-[m-(trifluoromethyl)phenyl]-2-pyrazoline (BW755C) in preventing the toxicity induced in male F-344 rats by methyl chloride (MeCl) [11].

Biological context of Inhibitor 3


Anatomical context of Inhibitor 3


Associations of Inhibitor 3 with other chemical compounds


Gene context of Inhibitor 3

  • However, when the small bowel juice had been pre-incubated with soybean trypsin inhibitor 3 g/l, casein 5 g/l or lactalbumin 30 g/l, the hydrolysis of PSTI diminished so that 95%, 32%, and 33% respectively, now eluted in the characteristic position of free (i.e. intact and not bound to an enzyme) PSTI [25].
  • We describe herein a set of mechanism-based inhibitors that show high selectivity to gelatinases and MMP-14 (inhibitor 3) and to only MMP-2 (inhibitors 5 and 7) [10].
  • The results show that (1) the dimericity of BS-RNase is essential for its full cytotoxic action; (2) the role of the dimeric structure in the antitumor activity is that of making the enzyme insensitive to the cytosolic RNase inhibitor; (3) a RNase may not be completely insensitive to cRI to exploit a full cytotoxic potential [26].
  • Activation of the rat serine proteinase inhibitor 3 gene by interferon gamma via the interleukin 6-responsive element [27].
  • The gene for cyclin-dependent protein kinase inhibitor 3 (CDKN3) was identified as a potential candidate gene in a differential display experiment [28].

Analytical, diagnostic and therapeutic context of Inhibitor 3


  1. Hyperbaric oxygen preconditioning induces tolerance against spinal cord ischemia by upregulation of antioxidant enzymes in rabbits. Nie, H., Xiong, L., Lao, N., Chen, S., Xu, N., Zhu, Z. J. Cereb. Blood Flow Metab. (2006) [Pubmed]
  2. Structure-based design of novel HIV-1 protease inhibitors to combat drug resistance. Ghosh, A.K., Sridhar, P.R., Leshchenko, S., Hussain, A.K., Li, J., Kovalevsky, A.Y., Walters, D.E., Wedekind, J.E., Grum-Tokars, V., Das, D., Koh, Y., Maeda, K., Gatanaga, H., Weber, I.T., Mitsuya, H. J. Med. Chem. (2006) [Pubmed]
  3. 3-Amino-1-hydroxypropylidine-1-bisphosphonate (AHPrBP) suppresses not only the induction of new, but also the persistence of existing bone-forming surfaces in rat cancellous bone. Tobias, J.H., Chow, J.W., Chambers, T.J. Bone (1993) [Pubmed]
  4. The critical role of leukotriene B4 in antigen-induced mechanical hyperalgesia in immunised rats. Cunha, J.M., Sachs, D., Canetti, C.A., Poole, S., Ferreira, S.H., Cunha, F.Q. Br. J. Pharmacol. (2003) [Pubmed]
  5. Signal transduction in Coprinus congregatus: evidence for the involvement of G proteins in blue light photomorphogenesis. Kozak, K.R., Ross, I.K. Biochem. Biophys. Res. Commun. (1991) [Pubmed]
  6. Drusen proteome analysis: an approach to the etiology of age-related macular degeneration. Crabb, J.W., Miyagi, M., Gu, X., Shadrach, K., West, K.A., Sakaguchi, H., Kamei, M., Hasan, A., Yan, L., Rayborn, M.E., Salomon, R.G., Hollyfield, J.G. Proc. Natl. Acad. Sci. U.S.A. (2002) [Pubmed]
  7. Structural basis for the inhibition of porcine pepsin by Ascaris pepsin inhibitor-3. Ng, K.K., Petersen, J.F., Cherney, M.M., Garen, C., Zalatoris, J.J., Rao-Naik, C., Dunn, B.M., Martzen, M.R., Peanasky, R.J., James, M.N. Nat. Struct. Biol. (2000) [Pubmed]
  8. UVB-induced DNA breaks interfere with transcriptional induction of c-fos. Ghosh, R., Amstad, P., Cerutti, P. Mol. Cell. Biol. (1993) [Pubmed]
  9. Serpin inhibitors of urokinase and thrombin in normal rat brain and the 9L brain tumor: evidence for elevated expression of protease nexin I-like inhibitor and a novel sodium dodecyl sulfate-activated tumor antithrombin. Rao, J.S., Baker, J.B., Morantz, R.A., Kimler, B., Evans, R., Festoff, B.W. Cancer Res. (1990) [Pubmed]
  10. Potent mechanism-based inhibitors for matrix metalloproteinases. Ikejiri, M., Bernardo, M.M., Bonfil, R.D., Toth, M., Chang, M., Fridman, R., Mobashery, S. J. Biol. Chem. (2005) [Pubmed]
  11. Inhibition of methyl chloride toxicity in male F-344 rats by the anti-inflammatory agent BW755C. Chellman, G.J., Morgan, K.T., Bus, J.S., Working, P.K. Toxicol. Appl. Pharmacol. (1986) [Pubmed]
  12. Anaplasma phagocytophilum delay of neutrophil apoptosis through the p38 mitogen-activated protein kinase signal pathway. Choi, K.S., Park, J.T., Dumler, J.S. Infect. Immun. (2005) [Pubmed]
  13. Ehrlichia chaffeensis and E. sennetsu, but not the human granulocytic ehrlichiosis agent, colocalize with transferrin receptor and up-regulate transferrin receptor mRNA by activating iron-responsive protein 1. Barnewall, R.E., Ohashi, N., Rikihisa, Y. Infect. Immun. (1999) [Pubmed]
  14. Renin inhibitors. Syntheses of subnanomolar, competitive, transition-state analogue inhibitors containing a novel analogue of statine. Boger, J., Payne, L.S., Perlow, D.S., Lohr, N.S., Poe, M., Blaine, E.H., Ulm, E.H., Schorn, T.W., LaMont, B.I., Lin, T.Y. J. Med. Chem. (1985) [Pubmed]
  15. Eicosanoid synthesis inhibition and renal allograft function during acute rejection. Mangino, M.J., Jendrisak, M.D., Brunt, E., Anderson, C.B. Transplantation (1988) [Pubmed]
  16. Two separate signal transducer and activator of transcription proteins regulate transcription of the serine proteinase inhibitor-3 gene in hepatic cells. Kordula, T., Ripperger, J., Morella, K.M., Travis, J., Baumann, H. J. Biol. Chem. (1996) [Pubmed]
  17. Pharmacological interruption of acute thrombus formation with minimal hemorrhagic complications by a small molecule tissue factor/factor VIIa inhibitor: comparison to factor Xa and thrombin inhibition in a nonhuman primate thrombosis model. Suleymanov, O.D., Szalony, J.A., Salyers, A.K., LaChance, R.M., Parlow, J.J., South, M.S., Wood, R.S., Nicholson, N.S. J. Pharmacol. Exp. Ther. (2003) [Pubmed]
  18. Isolation and characterization of coronary endothelial and smooth muscle cells from A1 adenosine receptor-knockout mice. Teng, B., Ansari, H.R., Oldenburg, P.J., Schnermann, J., Mustafa, S.J. Am. J. Physiol. Heart Circ. Physiol. (2006) [Pubmed]
  19. Protein phosphatase-1 inhibitor-3 is co-localized to the nucleoli and centrosomes with PP1gamma1 and PP1alpha, respectively. Huang, H.S., Pozarowski, P., Gao, Y., Darzynkiewicz, Z., Lee, E.Y. Arch. Biochem. Biophys. (2005) [Pubmed]
  20. Genome-wide expression profiling of fetal membranes reveals a deficient expression of proteinase inhibitor 3 in premature rupture of membranes. Tromp, G., Kuivaniemi, H., Romero, R., Chaiworapongsa, T., Kim, Y.M., Kim, M.R., Maymon, E., Edwin, S. Am. J. Obstet. Gynecol. (2004) [Pubmed]
  21. Clinical pharmacokinetic and pharmacodynamic studies with the nonclassical antifolate thymidylate synthase inhibitor 3, 4-dihydro-2-amino-6-methyl-4-oxo-5-(4-pyridylthio)-quinazolone dihydrochloride (AG337) given by 24-hour continuous intravenous infusion. Rafi, I., Taylor, G.A., Calvete, J.A., Boddy, A.V., Balmanno, K., Bailey, N., Lind, M., Calvert, A.H., Webber, S., Jackson, R.C. Clin. Cancer Res. (1995) [Pubmed]
  22. Design and synthesis of P2-P1'-linked macrocyclic human renin inhibitors. Weber, A.E., Halgren, T.A., Doyle, J.J., Lynch, R.J., Siegl, P.K., Parsons, W.H., Greenlee, W.J., Patchett, A.A. J. Med. Chem. (1991) [Pubmed]
  23. Synthesis and evaluation of tacrine-E2020 hybrids as acetylcholinesterase inhibitors for the treatment of Alzheimer's disease. Shao, D., Zou, C., Luo, C., Tang, X., Li, Y. Bioorg. Med. Chem. Lett. (2004) [Pubmed]
  24. Effect of WAY-100135 on the hippocampal acetylcholine release potentiated by 8-OH-DPAT, a serotonin1A receptor agonist, in normal and p-chlorophenylalanine-treated rats as measured by in vivo microdialysis. Nakai, K., Fujii, T., Fujimoto, K., Suzuki, T., Kawashima, K. Neurosci. Res. (1998) [Pubmed]
  25. Interactions of pancreatic secretory trypsin inhibitor in small intestinal juice: its hydrolysis and protection by intraluminal factors. Freeman, T.C., Davies, R., Calam, J. Clin. Chim. Acta (1990) [Pubmed]
  26. Antitumor action of seminal ribonuclease, its dimeric structure, and its resistance to the cytosolic ribonuclease inhibitor. Antignani, A., Naddeo, M., Cubellis, M.V., Russo, A., D'Alessio, G. Biochemistry (2001) [Pubmed]
  27. Activation of the rat serine proteinase inhibitor 3 gene by interferon gamma via the interleukin 6-responsive element. Kordula, T., Travis, J. Biochem. J. (1995) [Pubmed]
  28. Characterization of the porcine CDKN3 gene as a potential candidate for congenital splay leg in piglets. Maak, S., Jaesert, S., Neumann, K., von Lengerken, G. Genet. Sel. Evol. (2003) [Pubmed]
  29. Ikaros increases normal apoptosis in adult erythroid cells. Pulte, D., Lopez, R.A., Baker, S.T., Ward, M., Ritchie, E., Richardson, C.A., O'Neill, D.W., Bank, A. Am. J. Hematol. (2006) [Pubmed]
  30. Androgens contribute to the stimulation of cancellous bone formation by ovarian hormones in female rats. Gallagher, A.C., Chambers, T.J., Tobias, J.H. Am. J. Physiol. (1996) [Pubmed]
  31. Benefical effect of neutrophil elastase inhibitor on renal warm ischemia-reperfusion injury in the rat. Hayama, T., Matsuyama, M., Funao, K., Tanaka, T., Tsuchida, K., Takemoto, Y., Kawahito, Y., Sano, H., Nakatani, T., Yoshimura, R. Transplant. Proc. (2006) [Pubmed]
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