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Chemical Compound Review

Agenerase     [(3S)-oxolan-3-yl] N-[(2S,3R)-4-[(4...

Synonyms: Prozei, Vertex, amprenavir, CHEMBL116, Agenerase (TM), ...
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Disease relevance of AMP

  • These analyses support the virological observation that the addition of M46I and I47V mutations on the I50V mutant background enables increased survival of the HIV-1 virus as it replicates in the presence of VX-478 [1].
  • Passage of human immunodeficiency virus type-1 (HIV-1) in T-lymphocyte cell lines in the presence of increasing concentrations of the hydroxylethylamino sulfonamide inhibitor VX-478 or VB-11328 results in sequential accumulation of mutations in HIV-1 protease [1].
  • Within 10 to 15 weeks of serial passage, three major mutations-I54M, I82F, and L90M-arose in HIV-2 viral cultures exposed to APV, NFV, and IDV, whereas I82L was selected with TPV [2].
  • Twenty-seven patients (1 female, 26 males, age 62+/-9 years) with lung cancer or indeterminate pulmonary nodules were studied on the same day with a full-ring PET scanner (Siemens ECAT EXACT) and a coincidence gamma camera system (ADAC Vertex MCD) [3].

Psychiatry related information on AMP

  • At GlaxoSmithKline (GSK) and Vertex Pharmaceuticals, this effort focused on two key issues, patient compliance and viral resistance [4].
  • Individual differences in auditory electric responses: comparisons of between-subject and within-subject variability. II. Amplitude of brainstem Vertex-positive peaks [5].

High impact information on AMP


Chemical compound and disease context of AMP


Biological context of AMP

  • Single-dose safety and pharmacokinetics of amprenavir (141W94), a human immunodeficiency virus type 1 (HIV-1) protease inhibitor, in HIV-infected children [11].
  • He has founded several successful biotechnology firms, including Vertex Pharmaceuticals in 1989, ARIAD Pharmaceuticals in 1991, and Infinity Pharmaceuticals in 2001 [12].
  • The effects of protein binding on the antiviral activity of VX-478 are minor, as expected for a weak drug-protein interaction [13].
  • The structure of the two inhibitors 6-Cl-IMP and SAD binding in the IMP and NAD pockets of IMPDH, respectively, gives information for the binding mode of the di-nucleotide cofactor to the enzyme.At Vertex Pharmaceuticals a structure-based drug design program for the design of IMPDH inhibitors was initiated [14].
  • The average concentration of 141W94 at 8 and 12 h after single doses of 900 and 1200 mg, respectively, was in excess of 10 times the IC50 [15].

Anatomical context of AMP


Associations of AMP with other chemical compounds

  • Pharmacokinetic sampling was performed on day 8 of each treatment, and samples were analyzed for FPV, amprenavir (APV), LPV, and RTV concentrations by high-performance liquid chromatography-tandem mass spectrometry [20].
  • Compound 141W94 (Vertex VX478) (3S)-tetrahydro-3-furyl N-[((S,2R)-3-(4-amino-N-isobutylbenzenesulfonamido)-1-benzyl- 2-hydroxypropyl] carbamate, is a potent HIV-protease inhibitor and is currently undergoing clinical trials [21].
  • Urinary symptom scores were significantly lower for the Inlay stent on day 3 than for the Vertex (P = 0.01), Contour (P = 0.05), Endo-Sof (P = 0.03), and Classic (P = 0.02) stents [22].
  • The binding of 141W94 to human alpha 1-acid glycoprotein was relatively weak (Kd = 4 microM) and the off-rate for the drug is very fast (> or = 100 s-1) [15].
  • Resistant viruses were raised in vitro by passage of HIV-1IIIB in the presence of increasing concentrations of VX-478 and the related hydroxyethylamino sulfonamide inhibitor VB-11,328 [23].

Gene context of AMP

  • Amprenavir (141W94) is extensively metabolized by P450 cytochromes, specifically, CYP3A4 [24].
  • Role of P-glycoprotein on the CNS disposition of amprenavir (141W94), an HIV protease inhibitor [25].
  • We show that solving the footprint sorting problem requires the solution of the "Minimum Weight Vertex Feedback Set Problem", which is known to be NP-complete and APX-hard [26].
  • Quasistatic loading was done at a rate of 2.5 mm/s. Impact loading tests were conducted at a rate of 7.1 to 8.0 m/s. Vertex, parietal, temporal, frontal, and occipital regions were selected as the loading sites [27].
  • For the second problem of computing a PPH solution that minimizes the number of distinct haplotypes, we show that the problem is NP-hard using a reduction from Vertex Cover (Garey and Johnson, 1979) [28].

Analytical, diagnostic and therapeutic context of AMP


  1. Kinetic characterization of human immunodeficiency virus type-1 protease-resistant variants. Pazhanisamy, S., Stuver, C.M., Cullinan, A.B., Margolin, N., Rao, B.G., Livingston, D.J. J. Biol. Chem. (1996) [Pubmed]
  2. Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors. Ntemgwa, M., Brenner, B.G., Oliveira, M., Moisi, D., Wainberg, M.A. Antimicrob. Agents Chemother. (2007) [Pubmed]
  3. Imaging of lung cancer with fluorine-18 fluorodeoxyglucose: comparison of a dual-head gamma camera in coincidence mode with a full-ring positron emission tomography system. Weber, W.A., Neverve, J., Sklarek, J., Ziegler, S.I., Bartenstein, P., King, B., Treumann, T., Enterrottacher, A., Krapf, M., Häussinger, K.E., Lichte, H., Präuer, H.W., Thetter, O., Schwaiger, M. European journal of nuclear medicine. (1999) [Pubmed]
  4. Discovery of Next Generation Inhibitors of HIV Protease. Spaltenstein, A., Kazmierski, W.M., Miller, J.F., Samano, V. Current topics in medicinal chemistry. (2005) [Pubmed]
  5. Individual differences in auditory electric responses: comparisons of between-subject and within-subject variability. II. Amplitude of brainstem Vertex-positive peaks. Lauter, J.L., Loomis, R.L. Scandinavian audiology. (1988) [Pubmed]
  6. Novel inosine monophosphate dehydrogenase inhibitor VX-944 induces apoptosis in multiple myeloma cells primarily via caspase-independent AIF/Endo G pathway. Ishitsuka, K., Hideshima, T., Hamasaki, M., Raje, N., Kumar, S., Podar, K., Le Gouill, S., Shiraishi, N., Yasui, H., Roccaro, A.M., Tai, Y.Z., Chauhan, D., Fram, R., Tamura, K., Jain, J., Anderson, K.C. Oncogene (2005) [Pubmed]
  7. A mutation in human immunodeficiency virus type 1 protease, N88S, that causes in vitro hypersensitivity to amprenavir. Ziermann, R., Limoli, K., Das, K., Arnold, E., Petropoulos, C.J., Parkin, N.T. J. Virol. (2000) [Pubmed]
  8. In vitro selection and characterization of human immunodeficiency virus type 1 (HIV-1) isolates with reduced sensitivity to hydroxyethylamino sulfonamide inhibitors of HIV-1 aspartyl protease. Partaledis, J.A., Yamaguchi, K., Tisdale, M., Blair, E.E., Falcione, C., Maschera, B., Myers, R.E., Pazhanisamy, S., Futer, O., Cullinan, A.B. J. Virol. (1995) [Pubmed]
  9. 1592U89, a novel carbocyclic nucleoside analog with potent, selective anti-human immunodeficiency virus activity. Daluge, S.M., Good, S.S., Faletto, M.B., Miller, W.H., St Clair, M.H., Boone, L.R., Tisdale, M., Parry, N.R., Reardon, J.E., Dornsife, R.E., Averett, D.R., Krenitsky, T.A. Antimicrob. Agents Chemother. (1997) [Pubmed]
  10. A computational study of the resistance of HIV-1 aspartic protease to the inhibitors ABT-538 and VX-478 and design of new analogues. Nair, A.C., Miertus, S., Tossi, A., Romeo, D. Biochem. Biophys. Res. Commun. (1998) [Pubmed]
  11. Single-dose safety and pharmacokinetics of amprenavir (141W94), a human immunodeficiency virus type 1 (HIV-1) protease inhibitor, in HIV-infected children. Yogev, R., Kovacs, A., Chadwick, E.G., Homans, J.D., Lou, Y., Symonds, W.T. Antimicrob. Agents Chemother. (2005) [Pubmed]
  12. Stuart Schreiber: biology from a chemist's perspective. Interview by Joanna Owens. Schreiber, S.L. Drug Discov. Today (2004) [Pubmed]
  13. Weak binding of VX-478 to human plasma proteins and implications for anti-human immunodeficiency virus therapy. Livington, D.J., Pazhanisamy, S., Porter, D.J., Partaledis, J.A., Tung, R.D., Painter, G.R. J. Infect. Dis. (1995) [Pubmed]
  14. The structure of inosine 5'-monophosphate dehydrogenase and the design of novel inhibitors. Sintchak, M.D., Nimmesgern, E. Immunopharmacology (2000) [Pubmed]
  15. In vitro antiviral activity of 141W94 (VX-478) in combination with other antiretroviral agents. St Clair, M.H., Millard, J., Rooney, J., Tisdale, M., Parry, N., Sadler, B.M., Blum, M.R., Painter, G. Antiviral Res. (1996) [Pubmed]
  16. Metabolism of amprenavir in liver microsomes: role of CYP3A4 inhibition for drug interactions. Decker, C.J., Laitinen, L.M., Bridson, G.W., Raybuck, S.A., Tung, R.D., Chaturvedi, P.R. Journal of pharmaceutical sciences. (1998) [Pubmed]
  17. Frequency following auditory brain stem responses in man. Huis in't Veld, F., Osterhammel, P., Terkildsen, K. Scandinavian audiology. (1977) [Pubmed]
  18. The frequency selectivity of the 500 HZ frequency following response. Huis in't Veld, F., Osterhammel, P., Terkildsen, K. Scandinavian audiology. (1977) [Pubmed]
  19. Cranio-cervical stabilization of traumatic atlanto-occipital dislocation with minimal resultant neurological deficit. Seibert, P.S., Stridh-Igo, P., Whitmore, T.A., Dufty, B.M., Zimmerman, C.G. Acta neurochirurgica. (2005) [Pubmed]
  20. Dose separation does not overcome the pharmacokinetic interaction between fosamprenavir and lopinavir/ritonavir. Corbett, A.H., Patterson, K.B., Tien, H.C., Kalvass, L.A., Eron, J.J., Ngo, L.T., Lim, M.L., Kashuba, A.D. Antimicrob. Agents Chemother. (2006) [Pubmed]
  21. In vitro metabolism of a potent HIV-protease inhibitor (141W94) using rat, monkey and human liver S9. Singh, R., Chang, S.Y., Taylor, L.C. Rapid Commun. Mass Spectrom. (1996) [Pubmed]
  22. Randomized evaluation of Ureteral Stents using validated Symptom Questionnaire. Lee, C., Kuskowski, M., Premoli, J., Skemp, N., Monga, M. J. Endourol. (2005) [Pubmed]
  23. In vitro selection and characterization of VX-478 resistant HIV-1 variants. Pazhanisamy, S., Partaledis, J.A., Rao, B.G., Livingston, D.J. Adv. Exp. Med. Biol. (1998) [Pubmed]
  24. Single-dose pharmacokinetics of amprenavir, a human immunodeficiency virus type 1 protease inhibitor, in subjects with normal or impaired hepatic function. Veronese, L., Rautaureau, J., Sadler, B.M., Gillotin, C., Petite, J.P., Pillegand, B., Delvaux, M., Masliah, C., Fosse, S., Lou, Y., Stein, D.S. Antimicrob. Agents Chemother. (2000) [Pubmed]
  25. Role of P-glycoprotein on the CNS disposition of amprenavir (141W94), an HIV protease inhibitor. Polli, J.W., Jarrett, J.L., Studenberg, S.D., Humphreys, J.E., Dennis, S.W., Brouwer, K.R., Woolley, J.L. Pharm. Res. (1999) [Pubmed]
  26. The footprint sorting problem. Fried, C., Hordijk, W., Prohaska, S.J., Stadler, C.R., Stadler, P.F. Journal of chemical information and computer sciences. (2004) [Pubmed]
  27. Biomechanics of skull fracture. Yoganandan, N., Pintar, F.A., Sances, A., Walsh, P.R., Ewing, C.L., Thomas, D.J., Snyder, R.G. J. Neurotrauma (1995) [Pubmed]
  28. A note on efficient computation of haplotypes via perfect phylogeny. Bafna, V., Gusfield, D., Hannenhalli, S., Yooseph, S. J. Comput. Biol. (2004) [Pubmed]
  29. Safety and pharmacokinetics of amprenavir (141W94), a human immunodeficiency virus (HIV) type 1 protease inhibitor, following oral administration of single doses to HIV-infected adults. Sadler, B.M., Hanson, C.D., Chittick, G.E., Symonds, W.T., Roskell, N.S. Antimicrob. Agents Chemother. (1999) [Pubmed]
  30. Performance of simultaneous emission-transmission systems for attenuation-corrected SPEct: a method for validation applied to two camera systems. Almquist, H., Norrgren, K., Palmer, J., Jonson, B., Wollmer, P. Nuclear medicine communications. (2001) [Pubmed]
  31. Effect of storage duration on tensile bond strength of acrylic or silicone-based soft denture liners to a processed denture base polymer. Meşe, A., Güzel, K.G., Uysal, E. Acta Odontol. Scand. (2005) [Pubmed]
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