Literature for peptidase S01.140: chymase (Homo sapiens-type)

Summary Gene structure Alignment Tree Sequences Sequence features Distribution Structure Literature Substrates Pharma

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    2024
  1. Furstner,C., Ackerstaff,J., Meier,H., Straub,A., Mittendorf,J., Schamberger,J., Schafer,M., Borngen,K., Jorissen,H., Zubov,D., Zimmermann,K., Tersteegen,A., Geiss,V., Hartmann,E., Albrecht-Kupper,B., D'Orleans-Juste,P., Lapointe,C., Vincent,L., Heitmeier,S. and Tinel,H.
    Discovery and Preclinical Characterization of Fulacimstat (BAY 1142524), a Potent and Selective Chymase Inhibitor As a New Profibrinolytic Approach for Safe Thrombus Resolution
    J Med Chem PubMed  Europe PubMed DOI  I
  2. 2020
  3. Dungen,H.D., Kim,R.J., Zahger,D., Orvin,K., Kornowski,R., Admon,D., Kettner,J., Shimony,A., Otto,C., Becka,M., Kanefendt,F., Romo,A.I., Hasin,T., Ostadal,P., Rojas,G.C. and Senni,M.
    Effects of the chymase inhibitor fulacimstat on adverse cardiac remodeling after acute myocardial infarction: results of the chymase inhibitor in adverse remodeling after myocardial infarction (CHIARA MIA) 2 trial
    Am Heart J224, 129-137. PubMed  Europe PubMed DOI  I
  4. 2019
  5. Bivona,B.J., Takai,S., Seth,D.M., Satou,R. and Harrison-Bernard,L.M.
    Chymase inhibition retards albuminuria in type 2 diabetes
    Physiol Rep7, e14302-e14302. PubMed  Europe PubMed DOI  I
  6. Jin,D., Takai,S., Nonaka,Y., Yamazaki,S., Fujiwara,M. and Nakamura,Y.
    A chymase inhibitory RNA aptamer improves cardiac function and survival after myocardial infarction
    Mol Ther Nucleic Acids14, 41-51. PubMed  Europe PubMed DOI  I
  7. Kanefendt,F., Thuss,U., Becka,M., Boxnick,S., Berse,M., Schultz,A. and Otto,C.
    Pharmacokinetics, safety, and tolerability of the novel chymase inhibitor BAY 1142524 in healthy male volunteers
    Clin Pharmacol Drug Dev8, 467-479. PubMed  Europe PubMed DOI  I
  8. Ozawa,S.I., Takahashi,M., Yamaotsu,N. and Hirono,S.
    Structure-based virtual screening for novel chymase inhibitors by in silico fragment mapping
    J Mol Graph Model89, 102-108. PubMed  Europe PubMed DOI  I
  9. Tomimori,Y., Manno,A., Tanaka,T., Futamura-Takahashi,J., Muto,T. and Nagahira,K.
    ASB17061, a novel chymase inhibitor, prevented the development of angiotensin II-induced abdominal aortic aneurysm in apolipoprotein E-deficient mice
    Eur J Pharmacol856, 172403-172403. PubMed  Europe PubMed DOI  I
  10. 2018
  11. Ahmad,S. and Ferrario,C.M.
    Chymase inhibitors for the treatment of cardiac diseases: a patent review (2010-2018)
    Expert Opin Ther Pat28, 755-764. PubMed  Europe PubMed DOI  I
  12. Ansary,T.M., Urushihara,M., Fujisawa,Y., Nagata,S., Urata,H., Nakano,D., Hirofumi,H., Kitamura,K., Kagami,S. and Nishiyama,A.
    Effects of the selective chymase inhibitor TEI-F00806 on the intrarenal renin-angiotensin system in salt-treated angiotensin I-infused hypertensive mice
    Exp Physiol103, 1524-1531. PubMed  Europe PubMed DOI  I
  13. Dubey,A., Dotolo,S., Ramteke,P.W., Facchiano,A. and Marabotti,A.
    Searching for chymase inhibitors among chamomile compounds using a computational-based approach
    Biomolecules9, PubMed  Europe PubMed DOI  I
  14. Futamura-Takahashi,J., Tanaka,T., Sugawara,H., Iwashita,S., Imajo,S., Oyama,Y. and Muto,T.
    Structure-based design, synthesis, and binding mode analysis of novel and potent chymase inhibitors
    Bioorg Med Chem Lett28, 188-192. PubMed  Europe PubMed DOI  I
  15. 2016
  16. Dubey,A., Marabotti,A., Ramteke,P.W. and Facchiano,A.
    Interaction of human chymase with ginkgolides, terpene trilactones of Ginkgo biloba investigated by molecular docking simulations
    Biochem Biophys Res Commun473, 449-454. PubMed  Europe PubMed DOI  I
  17. Dubey,A., Facchiano,A., Ramteke,P.W. and Marabotti,A.
    In silico approach to find chymase inhibitors among biogenic compounds
    Future Med Chem8, 841-851. PubMed  Europe PubMed DOI  I
  18. Sansoe,G., Aragno,M., Mastrocola,R., Mengozzi,G., Novo,E. and Parola,M.
    Role of chymase in the development of liver cirrhosis and its complications: experimental and human data
    PLoS ONE11, e0162644-e0162644. PubMed  Europe PubMed DOI  I
  19. Takai,S. and Jin,D.
    Improvement of cardiovascular remodelling by chymase inhibitor
    Clin Exp Pharmacol Physiol43, 387-393. PubMed  Europe PubMed DOI  I
  20. Zhang,M., Huang,W., Bai,J., Nie,X. and Wang,W.
    Chymase inhibition protects diabetic rats from renal lesions
    Mol Med Rep14, 121-128. PubMed  Europe PubMed DOI  I
  21. 2015
  22. Arooj,M., Sakkiah,S., Cao,G.P., Kim,S., Arulalapperumal,V. and Lee,K.W.
    Finding off-targets, biological pathways, and target diseases for chymase inhibitors via structure-based systems biology approach
    Proteins83, 1209-1224. PubMed  Europe PubMed DOI  I
  23. Devarajan,S., Yahiro,E., Uehara,Y., Habe,S., Nishiyama,A., Miura,S., Saku,K. and Urata,H.
    Depressor effect of chymase inhibitor in mice with high salt-induced moderate hypertension
    Am J Physiol Heart Circ Physiol309, H1987-H1996. PubMed  Europe PubMed DOI  I
  24. Semaan,W., Desbiens,L., Houde,M., Labonte,J., Gagnon,H., Yamamoto,D., Takai,S., Laidlaw,T., Bkaily,G., Schwertani,A., Pejler,G., Levesque,C., Desjardins,R., Day,R. and D'Orleans-Juste,P.
    Chymase inhibitor-sensitive synthesis of endothelin-1 (1-31) by recombinant mouse mast cell protease 4 and human chymase
    Biochem Pharmacol94, 91-100. PubMed  Europe PubMed DOI  I
  25. 2014
  26. Fei,X., Yuan,Y., Lee,Y.-M., Jeong,K.W. and Seo,S.-Y.
    Synthesis, biological evaluation of SPF-32629A-based 2- and 4-pyridone analogs as chymase inhibitors
    Bull Korean Chem Soc35, 2547-2550. DOI  I
  27. 2013
  28. Ahooghalandari,P., Hanke,N., Thorpe,M., Witte,A., Messinger,J. and Hellman,L.
    Mutations in Arg143 and Lys192 of the human mast cell chymase markedly affect the activity of five potent human chymase inhibitors
    PLoS ONE8, e65988-e65988. PubMed  Europe PubMed DOI  I
  29. Arooj,M., Kim,S., Sakkiah,S., Cao,G.P., Lee,Y. and Lee,K.W.
    Molecular modeling study for inhibition mechanism of human chymase and its application in inhibitor design
    PLoS ONE8, e62740-e62740. PubMed  Europe PubMed DOI  I
  30. Matsumoto,Y., Kakuda,S., Koizumi,M., Mizuno,T., Muroga,Y., Kawamura,T. and Takimoto-Kamimura,M.
    Crystal structure of a complex of human chymase with its benzimidazole derived inhibitor
    J Synchrotron Radiat20, 914-918. PubMed  Europe PubMed DOI  S  I
  31. Tanaka,T., Sugawara,H., Maruoka,H., Imajo,S. and Muto,T.
    Discovery of novel series of 6-benzyl substituted 4-aminocarbonyl-1,4-diazepane-2,5-diones as human chymase inhibitors using structure-based drug design
    Bioorg Med Chem21, 4233-4249. PubMed  Europe PubMed DOI  I
  32. Taylor,S.J., Padyana,A.K., Abeywardane,A., Liang,S., Hao,M.H., De Lombaert,S., Proudfoot,J., Farmer,B.S., III, Li,X., Collins,B., Martin,L., Albaugh,D.R., Hill-Drzewi,M., Pullen,S.S. and Takahashi,H.
    Discovery of potent, selective chymase inhibitors via fragment linking strategies
    J Med Chem56, 4465-4481. PubMed  Europe PubMed DOI  I
  33. Yahiro,E., Miura,S., Imaizumi,S., Uehara,Y. and Saku,K.
    Chymase inhibitors
    Curr Pharm Des19, 3065-3071. PubMed  Europe PubMed DOI  I
  34. 2012
  35. Maeda,Y., Inoguchi,T., Takei,R., Hendarto,H., Ide,M., Inoue,T., Kobayashi,K., Urata,H., Nishiyama,A. and Takayanagi,R.
    Chymase inhibition prevents myocardial fibrosis through the attenuation of NOX4-associated oxidative stress in diabetic hamsters
    J Diabetes Investig3, 354-361. PubMed  Europe PubMed DOI  I
  36. Takai,S., Jin,D. and Miyazaki,M.
    Multiple mechanisms for the action of chymase inhibitors
    J Pharmacol Sci118, 311-316. PubMed  Europe PubMed DOI  I
  37. 2011
  38. Ahmad,S., Simmons,T., Varagic,J., Moniwa,N., Chappell,M.C. and Ferrario,C.M.
    Chymase-dependent generation of angiotensin II from angiotensin-(1-12) in human atrial tissue
    PLoS ONE6, e28501-e28501. PubMed  Europe PubMed DOI  I
  39. Arooj,M., Thangapandian,S., John,S., Hwang,S., Park,J.K. and Lee,K.W.
    3D QSAR pharmacophore modeling, in silico screening, and density functional theory (DFT) approaches for identification of human chymase inhibitors
    Int J Mol Sci12, 9236-9264. PubMed  Europe PubMed DOI  I
  40. Lo,H.Y., Nemoto,P.A., Kim,J.M., Hao,M.H., Qian,K.C., Farrow,N.A., Albaugh,D.R., Fowler,D.M., Schneiderman,R.D., Michael August,E., Martin,L., Hill-Drzewi,M., Pullen,S.S., Takahashi,H. and De Lombaert,S.
    Benzimidazolone as potent chymase inhibitor: modulation of reactive metabolite formation in the hydrophobic (P1) region
    Bioorg Med Chem Lett21, 4533-4539. PubMed  Europe PubMed DOI  I
  41. Oyamada,S., Bianchi,C., Takai,S., Chu,L.M. and Sellke,F.W.
    Chymase inhibition reduces infarction and matrix metalloproteinase-9 activation and attenuates inflammation and fibrosis after acute myocardial ischemia/reperfusion
    J Pharmacol Exp Ther339, 143-151. PubMed  Europe PubMed DOI  I
  42. Takai,S., Jin,D. and Miyazaki,M.
    Targets of chymase inhibitors
    Expert Opin Ther Targets15, 519-527. PubMed  Europe PubMed DOI  I
  43. 2010
  44. Kervinen,J., Crysler,C., Bayoumy,S., Abad,M.C., Spurlino,J., Deckman,I., Greco,M.N., Maryanoff,B.E. and de Garavilla,L.
    Potency variation of small-molecule chymase inhibitors across species
    Biochem Pharmacol80, 1033-1041. PubMed  Europe PubMed DOI  I
  45. Maeda,Y., Inoguchi,T., Takei,R., Sawada,F., Sasaki,S., Fujii,M., Kobayashi,K., Urata,H., Nishiyama,A. and Takayanagi,R.
    Inhibition of chymase protects against diabetes-induced oxidative stress and renal dysfunction in hamsters
    Am J Physiol Renal Physiol299, F1328-F1338. PubMed  Europe PubMed DOI  I
  46. Pat,B., Chen,Y., Killingsworth,C., Gladden,J.D., Shi,K., Zheng,J., Powell,P.C., Walcott,G., Ahmed,M.I., Gupta,H., Desai,R., Wei,C.C., Hase,N., Kobayashi,T., Sabri,A., Granzier,H., Denney,T., Tillson,M., Dillon,A.R., Husain,A. and Dell'Italia,L.J.
    Chymase inhibition prevents fibronectin and myofibrillar loss and improves cardiomyocyte function and LV torsion angle in dogs with isolated mitral regurgitation
    Circulation122, 1488-1495. PubMed  Europe PubMed DOI  I
  47. 2009
  48. Matsumoto,C., Hayashi,T., Kitada,K., Yamashita,C., Miyamura,M., Mori,T., Ukimura,A., Ohkita,M., Jin,D., Takai,S., Miyazaki,M., Okada,Y., Kitaura,Y. and Matsumura,Y.
    Chymase plays an important role in left ventricular remodeling induced by intermittent hypoxia in mice
    Hypertension54, 164-171. PubMed  Europe PubMed DOI  I
  49. 2008
  50. D'Orleans-Juste,P., Houde,M., Rae,G.A., Bkaily,G., Carrier,E. and Simard,E.
    Endothelin-1 (1-31): from chymase-dependent synthesis to cardiovascular pathologies
    Vascul Pharmacol49, 51-62. PubMed  Europe PubMed DOI  I
  51. Doggrell,S.A.
    Therapeutic potential of non-peptide chymase inhibitors
    Expert Opin Ther Pat18, 485-499. DOI  T  I
  52. 2007
  53. Greco,M.N., Hawkins,M.J., Powell,E.T., Almond,H.R., Jr., de Garavilla,L., Hall,J., Minor,L.K., Wang,Y., Corcoran,T.W., Di Cera,E., Cantwell,A.M., Savvides,S.N., Damiano,B.P. and Maryanoff,B.E.
    Discovery of potent, selective, orally active, nonpeptide inhibitors of human mast cell chymase
    J Med Chem50, 1727-1730. PubMed  Europe PubMed DOI  I
  54. Jin,D., Ueda,H., Takai,S., Muramatsu,M., Furubayashi,K., Ibaraki,T., Kishi,K., Katsuoka,Y. and Miyazaki,M.
    Roles of chymase in stenosis occurring after polytetrafluoroethylene graft implantations
    Life Sci81, 1291-1300. PubMed  Europe PubMed DOI  I
  55. Maruoka,H., Muto,T., Tanaka,T., Imajo,S., Tomimori,Y., Fukuda,Y. and Nakatsuka,T.
    Development of 6-benzyl substituted 4-aminocarbonyl-1,4-diazepane-2,5-diones as orally active human chymase inhibitors
    Bioorg Med Chem Lett17, 3435-3439. PubMed  Europe PubMed DOI  I
  56. Tanaka,T., Muto,T., Maruoka,H., Imajo,S., Fukami,H., Tomimori,Y., Fukuda,Y. and Nakatsuka,T.
    Identification of 6-substituted 4-arylsulfonyl-1,4-diazepane-2,5-diones as a novel scaffold for human chymase inhibitors
    Bioorg Med Chem Lett17, 3431-3434. PubMed  Europe PubMed DOI  I
  57. 2006
  58. Kanemitsu,H., Takai,S., Tsuneyoshi,H., Nishina,T., Yoshikawa,K., Miyazaki,M., Ikeda,T. and Komeda,M.
    Chymase inhibition prevents cardiac fibrosis and dysfunction after myocardial infarction in rats
    Hypertens Res29, 57-64. PubMed  Europe PubMed DOI  I
  59. Shimatani,T., Hosotani,N., Ohnishi,M., Kumagai,K. and Saji,I.
    SPF-32629 A and B, novel human chymase inhibitors produced by Penicillium sp
    J Antibiot (Tokyo)59, 29-34. PubMed  Europe PubMed DOI  I
  60. 2005
  61. [YEAR:28-2-2005]de Garavilla,L., Greco,M.N., Sukumar,N., Chen,Z.W., Pineda,A.O., Mathews,F.S., Di Cera,E., Giardino,E.C., Wells,G.I., Haertlein,B.J., Kauffman,J.A., Corcoran,T.W., Derian,C.K., Eckardt,A.J., Damiano,B.P., Andrade-Gordon,P. and Maryanoff,B.E.
    A novel, potent dual inhibitor of the leukocyte proteases cathepsin G and chymase: molecular mechanisms and anti-inflammatory activity in vivo
    J Biol Chem280, 18001-18007. PubMed  Europe PubMed DOI  I
  62. 2004
  63. Alagille,D., Pfeiffer,B., Scalbert,E., Ferry,G., Boutin,J.A., Renard,P. and Viaud-Massuard,M.C.
    Design and synthesis of indole and tetrahydroisoquinoline hydantoin derivatives as human chymase inhibitors
    J Enzyme Inhib Med Chem19, 137-143. PubMed  Europe PubMed DOI  I
  64. [YEAR:1-3-2004]Doggrell,S.A. and Wanstall,J.C.
    Vascular chymase: pathophysiological role and therapeutic potential of inhibition
    Cardiovasc Res61, 653-662. PubMed  Europe PubMed DOI  I
  65. [YEAR:12-2-2004]Maryanoff,B.E.
    Inhibitors of serine proteases as potential therapeutic agents: the road from thrombin to tryptase to cathepsin G
    J Med Chem47, 769-787. PubMed  Europe PubMed DOI  I
  66. Takai,S., Jin,D., Sakaguchi,M. and Miyazaki,M.
    A single treatment with a specific chymase inhibitor, TY-51184, prevents vascular proliferation in canine grafted veins
    J Pharmacol Sci94, 443-448. PubMed  Europe PubMed DOI  I
  67. [YEAR:6-10-2004]Takai,S., Jin,D., Muramatsu,M., Okamoto,Y. and Miyazaki,M.
    Therapeutic applications of chymase inhibitors in cardiovascular diseases and fibrosis
    Eur J Pharmacol501, 1-8. PubMed  Europe PubMed DOI  I
  68. 2003
  69. Hoshino,F., Urata,H., Inoue,Y., Saito,Y., Yahiro,E., Ideishi,M., Arakawa,K. and Saku,K.
    Chymase inhibitor improves survival in hamsters with myocardial infarction
    J Cardiovasc Pharmacol41 Suppl 1, S11-S18. PubMed  Europe PubMed  I
  70. [YEAR:6-1-2003]Koide,Y., Tatsui,A., Hasegawa,T., Murakami,A., Satoh,S., Yamada,H., Kazayama,S. and Takahashi,A.
    Identification of a stable chymase inhibitor using a pharmacophore-based database search
    Bioorg Med Chem Lett13, 25-29. PubMed  Europe PubMed DOI  I
  71. [YEAR:17-11-2003]Masaki,H., Mizuno,Y., Tatui,A., Murakami,A., Koide,Y., Satoh,S. and Takahashi,A.
    Structure-activity relationship of benzo[b]thiophene-2-sulfonamide derivatives as novel human chymase inhibitors
    Bioorg Med Chem Lett13, 4085-4088. PubMed  Europe PubMed DOI  I
  72. Takai,S., Sakonjo,H., Fukuda,K., Jin,D., Sakaguchi,M., Kamoshita,K., Ishida,K., Sukenaga,Y. and Miyazaki,M.
    A novel chymase inhibitor, 2-(5-formylamino-6-oxo-2-phenyl-1,6-dihydropyrimidine-1-yl)-N-[[,4-dioxo-1-phenyl-7-(2-pyridyloxy)]2-heptyl]acetamide (NK3201), suppressed intimal hyperplasia after balloon injury
    J Pharmacol Exp Ther304, 841-844. PubMed  Europe PubMed DOI  I
  73. 2002
  74. Murakami,Y., Takei,M., Shindo,K., Kitazume,C., Tanaka,J., Higa,T. and Fukamachi,H.
    Cyclotheonamide E4 and E5, new potent tryptase inhibitors from an Ircinia species of sponge
    J Nat Prod65, 259-261. PubMed  Europe PubMed DOI  I
  75. [YEAR:4-10-2002]Muramatsu,M., Yamada,M., Takai,S. and Miyazaki,M.
    Suppression of basic fibroblast growth factor-induced angiogenesis by a specific chymase inhibitor, BCEAB, through the chymase-angiotensin-dependent pathway in hamster sponge granulomas
    Br J Pharmacol137, 554-560. PubMed  Europe PubMed DOI  I
  76. Okamoto,Y., Takai,S., Yamada,M. and Miyazaki,M.
    Chymase inhibitors may prevent postoperative adhesion formation
    Fertil Steril77, 1044-1048. PubMed  Europe PubMed DOI  I
  77. 2001
  78. [YEAR:9-7-2001]Aoyama,Y., Konoike,T., Kanda,A., Naya,N. and Nakajima,M.
    Total synthesis of human chymase inhibitor methyllinderone and structure-activity relationships of its derivatives
    Bioorg Med Chem Lett11, 1695-1697. PubMed  Europe PubMed DOI  I
  79. Aoyama,Y., Uenaka,M., Kii,M., Tanaka,M., Konoike,T., Hayasaki-Kajiwara,Y., Naya,N. and Nakajima,M.
    Design, synthesis and pharmacological evaluation of 3-benzylazetidine-2-one-based human chymase inhibitors
    Bioorg Med Chem9, 3065-3075. PubMed  Europe PubMed DOI  I
  80. Neumann,U., Schechter,N.M. and Gutschow,M.
    Inhibition of human chymase by 2-amino-3,1-benzoxazin-4-ones
    Bioorg Med Chem9, 947-954. PubMed  Europe PubMed DOI  I
  81. 2000
  82. [YEAR:6-11-2000]Aoyama,Y., Uenaka,M., Konoike,T., Iso,Y., Nishitani,Y., Kanda,A., Naya,N. and Nakajima,M.
    1-Oxacephem-based human chymase inhibitors: discovery of stable inhibitors in human plasma
    Bioorg Med Chem Lett10, 2403-2406. PubMed  Europe PubMed  I
  83. [YEAR:7-2-2000]Hayashi,Y., Iijima,K., Katada,J. and Kiso,Y.
    Structure-activity relationship studies of chloromethyl ketone derivatives for selective human chymase inhibitors
    Bioorg Med Chem Lett10, 199-201. PubMed  Europe PubMed DOI  I
  84. 1999
  85. [YEAR:2-8-1999]Groutas,W.C., Schechter,N.M., He,S., Yu,H., Huang,P. and Tu,J.
    Human chymase inhibitors based on the 1,2,5-thiadiazolidin-3-one 1,1 dioxide scaffold
    Bioorg Med Chem Lett9, 2199-2204. PubMed  Europe PubMed DOI  I
  86. [YEAR:12-2-1999]Pereira,P.J., Wang,Z.M., Rubin,H., Huber,R., Bode,W., Schechter,N.M. and Strobl,S.
    The 2.2 A crystal structure of human chymase in complex with succinyl-Ala-Ala-Pro-Phe-chloromethylketone: structural explanation for its dipeptidyl carboxypeptidase specificity
    J Mol Biol286, 163-173. PubMed  Europe PubMed DOI  S  I
  87. 1998
  88. Eda,M., Ashimori,A., Akahoshi,F., Yoshimura,T., Inoue,Y., Fukaya,C., Nakajima,M., Fukuyama,H., Imada,T., Takai,S., Shiota,N., Miyazaki,M. and Nakamura,N.
    Peptidyl human heart chymase inhibitors. 2. Discovery of highly selective difluoromethylene ketone derivatives with Glu at P3 site
    Bioorg Med Chem Lett8, 919-924. PubMed  Europe PubMed DOI  I
  89. 1995
  90. Bastos,M., Maeji,N.J. and Abeles,R.H.
    Inhibitors of human heart chymase based on a peptide library
    Proc Natl Acad Sci U S A92, 6738-6742. PubMed  Europe PubMed DOI  I
  91. 1985
  92. [YEAR:9-4-1985]Powers,J.C., Tanaka,T., Harper,J.W., Minematsu,Y., Barker,L., Lincoln,D., Crumley,K.V., Fraki,J.E., Schechter,N.M., Lazarus,G.G., Nakajima,K., Nakashino,K., Neurath,H. and Woodbury,R.G.
    Mammalian chymotrypsin-like enzymes. Comparative reactivities of rat mast cell proteases, human and dog skin chymases, and human cathepsin G with peptide 4-nitroanilide substrates and with peptide chloromethyl ketone and sulfonyl fluoride inhibitors
    Biochemistry24, 2048-2058. PubMed  Europe PubMed  I