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Aurora inhibitor

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Harrington, Elizabeth A.; Bebbington, David; Moore, Jeff; Rasmussen, Richele K.; Ajose-Adeogun, Abi O.; Nakayama, Tomoko; Graham, Joanne A.; Demur, Cecile; Hercend, Thierry; Diu-Hercend, Anita; Su, Michael; Golec, Julian M C.; Miller, Karen M. (2004). "VX-680, a potent and selective small-molecule
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Ewart-Toland, Amanda; Briassouli, Paraskevi; De Koning, John P.; Mao, Jian-Hua; Yuan, Jinwei; Chan, Florence; Maccarthy-Morrogh, Lucy; Ponder, Bruce A J.; Nagase, Hiroki; Burn, John; Ball, Sarah; Almeida, Maria; Linardopoulos, Spiros; Balmain, Allan (2003). "Identification of Stk6/STK15 as a
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moiety and Aurora-2. Residues Lys-162 and Asp-274 are essential for Aurora-2 kinase activity but do not hydrogen bond to each other as seen in crystal structures of several other protein kinases.
237:. The protein backbone atoms of residues Glu-211, Ala-213 in the hinge region of Aurora-2, and the sidechain of residue Trp-277, located in the activation loop, bind adenosine through specific 3652: 765:"Aurora Kinase Inhibitor ZM447439 Blocks Chromosome-induced Spindle Assembly, the Completion of Chromosome Condensation, and the Establishment of the Spindle Integrity Checkpoint inXenopus 3647: 1009: 816:
Peters, Jan-Michael; Rieder, Conly L.; Van Meel, Jacques; Heckel, Armin; Walter, Rainer; Schnapp, Gisela; Zimmer, Christine; Laterra, Sabrina; Cole, Richard W.; Hauf, Silke (2003).
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Goto, Hidemasa; Yasui, Yoshihiro; Nigg, Erich A.; Inagaki, Masaki (2002). "Aurora-B phosphorylates Histone H3 at serine28 with regard to the mitotic chromosome condensation".
107:, have gained a great deal of attention as possible anticancer drug targets. The Aurora enzymes are particularly significant because they are involved in a direct path to the 3767: 3745: 1002: 1209: 3563: 818:"The small molecule Hesperadin reveals a role for Aurora B in correcting kinetochore–microtubule attachment and in maintaining the spindle assembly checkpoint" 1757: 2596: 1060: 3673: 2705: 1443: 1330: 1718: 3568: 3735: 2691: 2156: 1047: 1029: 2793: 2674: 2380: 1249: 3374: 2444: 1419: 2700: 1234: 165:, although the Phase II clinical trial was suspended in November, 2007 due to QT prolongation observed in one patient in Phase I trial. 4145: 3508: 2757: 2432: 72:
aurora kinase genes, encoding aurora A, B and C. Intense investigation has focused on aurora A and B as they appear to play a role in
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The structure and active site of Aurora-2-adenosine complex has been determined. The hinge (yellow), glycine-rich loop (blue), and
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Graham M. T. et al., Crystal Structure of Aurora-2, an Oncogenic Serine/Threonine Kinase J. Biol. Chem., (2002) 277: pp.42419-22
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Andrews, Paul D.; Knatko, Elena; Moore, William J.; Swedlow, Jason R. (2003). "Mitotic mechanics: The auroras come into view".
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Katayama, Hiroshi; Brinkley, W. R.; Sen, S. (2003). "The Aurora kinases: Role in cell transformation and tumorigenesis".
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A new approach to inhibiting cancer growth that shows great promise for structure-based drug development is targeting
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Yang, Hua; Ou, Chien Chen; Feldman, Richard I.; Nicosia, Santo V.; Kruk, Patricia A.; Cheng, Jin Q. (2004).
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Sakita-Suto, Shiho; Kanda, Akifumi; Suzuki, Fumio; Sato, Sunao; Takata, Takashi; Tatsuka, Masaaki (2007).
667:"Aurora-A Kinase Regulates Telomerase Activity through c-Myc in Human Ovarian and Breast Epithelial Cells" 158: 3908: 3827: 3409: 3364: 3066: 3051: 2987: 2967: 2865: 1479: 3980: 2850: 3323: 3318: 3198: 3061: 3041: 2950: 2046: 4135: 3944: 3586: 3578: 3359: 3026: 2962: 2926: 988: 264: 2554: 577:"DNA methylation promotes Aurora-B-driven phosphorylation of histone H3 in chromosomal subdomains" 3877: 3449: 3387: 3338: 3073: 2900: 2657: 2611: 940: 745: 696: 606: 522: 473: 430: 387: 343: 3464: 3454: 3444: 3369: 3353: 3312: 3298: 3293: 3031: 2994: 1917: 1626: 932: 896: 847: 798: 737: 688: 647: 598: 557: 514: 465: 422: 379: 335: 300: 405:
Nigg, Erich A. (2001). "Mitotic kinases as regulators of cell division and its checkpoints".
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Lee, Edmund Chun Yu; Frolov, Anna; Li, Rile; Ayala, Gustavo; Greenberg, Norman M. (2006).
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Keen, Nicholas; Taylor, Stephen (2004). "Aurora-kinase inhibitors as anticancer agents".
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Aurora-A (Serine/threonine-protein kinase 6, AIK, ARK1, AURA, BTAK, STK15, STK6)
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candidate low-penetrance tumor-susceptibility gene in mouse and human".
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Aurora-B (Serine/threonine-protein kinase 12, AIK2, AIM1, ARK2, STK12)
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inhibitor of the Aurora kinases, suppresses tumor growth in vivo".
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3-methyl-2-oxobutanoate dehydrogenase (acetyl-transferring) kinase
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and overexpressed in various forms of cancerous growth, including
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CDP-diacylglycerol—glycerol-3-phosphate 3-phosphatidyltransferase
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Aurora-C (Serine/threonine-protein kinase 13, AIE2, AIK3, STK13)
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enzymes could be potential targets for novel small-molecule
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So far three Aurora-kinase inhibitors have been described:
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Aurora case study – six inhibitors and their action during
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CDP-diacylglycerol—inositol 3-phosphatidyltransferase
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CDP-diacylglycerol—choline O-phosphatidyltransferase
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CDP-diacylglycerol—serine O-phosphatidyltransferase
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The last is in advanced stages (Phase II 3835: 3821: 3813: 3702: 3632: 3262: 3253: 2918: 2873: 2859: 2851: 2789: 2775: 2165: 2151: 1444:Goodpasture-antigen-binding protein kinase 1056: 1042: 1017: 1003: 995: 3768:serine/threonine-specific protein kinases 3746:serine/threonine-specific protein kinases 3569:Galactose-1-phosphate uridylyltransferase 2157:Serine/threonine-specific protein kinases 1331:(isocitrate dehydrogenase (NADP+)) kinase 1048:Serine/threonine-specific protein kinases 1030:Serine/threonine-specific protein kinases 890: 841: 792: 731: 682: 641: 592: 508: 2692:Receptor protein serine/threonine kinase 83:susceptibility gene in mice and humans. 4110: 2675:Low-density-lipoprotein receptor kinase 275: 167: 41:are a putative drug class for treating 1420:Fas-activated serine/threonine kinase 407:Nature Reviews Molecular Cell Biology 7: 2701:Bone morphogenetic protein receptors 1235:Dephospho-(reductase kinase) kinase 1690:G-protein coupled receptor kinases 76:with aurora A identified as a low 25: 3079:Glucose-1,6-bisphosphate synthase 1680:Beta adrenergic receptor kinase-2 1365:(tyrosine 3-monooxygenase) kinase 157:) of a joint drug development by 4113: 3220:Ribose-phosphate diphosphokinase 2372:Mitogen-activated protein kinase 554:10.1046/j.1356-9597.2001.00498.x 198: 184: 170: 2758:Anti-MĂĽllerian hormone receptor 2641:(acetyl-CoA carboxylase) kinase 2313:(RNA-polymerase)-subunit kinase 1675:Beta adrenergic receptor kinase 1666:Beta adrenergic receptor kinase 285:Current Opinion in Cell Biology 2381:Extracellular signal-regulated 229:(red) are key features of the 1: 3793:Protein-histidine tele-kinase 3788:Protein-histidine pros-kinase 3667:Glycosyl-1-phosphotransferase 2445:P38 mitogen-activated protein 1544:cGMP-dependent protein kinase 1505:cAMP-dependent protein kinase 1201:Pyruvate dehydrogenase kinase 1147:Ataxia telangiectasia mutated 871:Molecular Biology of the Cell 773:Molecular Biology of the Cell 733:10.1158/1541-7786.MCR-06-0208 684:10.1158/0008-5472.can-03-2907 643:10.1158/0008-5472.CAN-05-2796 510:10.1158/1078-0432.CCR-06-1405 320:Cancer and Metastasis Reviews 3499:RNA-dependent RNA polymerase 1244:AMP-activated protein kinase 985:Mitotic spindle & Aurora 3406:RNA-directed DNA polymerase 3274:DNA-directed DNA polymerase 2159:(EC 2.7.11.21-EC 2.7.11.30) 4162: 3759:: protein-dual-specificity 2086:Elongation factor 2 kinase 1050:(EC 2.7.11.1-EC 2.7.11.20) 64:, and thus are targets in 4146:Protein kinase inhibitors 3991:Michaelis–Menten kinetics 2788: 2774: 2481:MAP kinase kinase kinases 2164: 2150: 2013:Myosin light-chain kinase 1719:Ca2+/calmodulin-dependent 1384:Myosin-heavy-chain kinase 1055: 1041: 720:Molecular Cancer Research 297:10.1016/j.ceb.2003.10.013 233:fold involved in binding 68:therapy. There are three 3883:Diffusion-limited enzyme 3736:protein-serine/threonine 3636:Phosphatidyltransferases 3225:Thiamine diphosphokinase 2781:Dual-specificity kinases 497:Clinical Cancer Research 60:transit from G2 through 56:Aurora kinases regulate 39:Aurora kinase inhibitors 2204:Cyclin-dependent kinase 883:10.1091/mbc.e06-11-1021 822:Journal of Cell Biology 785:10.1091/mbc.e04-10-0891 581:Journal of Cell Science 332:10.1023/a:1023789416385 260:Cyclin-dependent kinase 18:Aurora kinase inhibitor 3556:Nucleotidyltransferase 3239:nucleotidyltransferase 3166:Nucleoside-diphosphate 222: 221:Aurora's active center 159:Vertex Pharmaceuticals 35: 3976:Eadie–Hofstee diagram 3909:Allosteric regulation 3410:Reverse transcriptase 834:10.1083/jcb.200208092 450:Nature Reviews Cancer 220: 30: 3986:Lineweaver–Burk plot 3199:diphosphotransferase 3181:Thiamine-diphosphate 2888:-containing groups ( 2047:Phosphorylase kinase 95:central to cellular 3781:: protein-histidine 3699:; protein acceptor) 3587:mRNA capping enzyme 3579:Guanylyltransferase 989:The Proteolysis Map 265:Signal transduction 3945:Enzyme superfamily 3878:Enzyme promiscuity 3057:Phosphoinositide 3 2901:phosphotransferase 2658:Tropomyosin kinase 2612:Tau-protein kinase 223: 36: 4101: 4100: 3810: 3809: 3806: 3805: 3682: 3681: 3621: 3620: 3522: 3521: 3435:Template-directed 3189: 3188: 3156:Phosphomevalonate 2848: 2847: 2844: 2843: 2840: 2839: 2770: 2769: 2766: 2765: 2146: 2145: 2142: 2141: 1627:Protein kinase N1 1582:Protein kinase Cζ 636:(10): 4996–5002. 594:10.1242/jcs.03326 587:(Pt 1): 101–114. 503:(23): 6869–6875. 51:enzyme inhibitors 16:(Redirected from 4153: 4118: 4117: 4109: 3981:Hanes–Woolf plot 3924:Enzyme activator 3919:Enzyme inhibitor 3893:Enzyme catalysis 3837: 3830: 3823: 3814: 3798:Histidine kinase 3721:tyrosine kinases 3711:protein-tyrosine 3703: 3633: 3440:RNA polymerase I 3263: 3254: 3107:Aspartate kinase 3102:Phosphoglycerate 2919: 2875: 2868: 2861: 2852: 2790: 2776: 2423:C-Jun N-terminal 2166: 2152: 1656:Rhodopsin kinase 1647:Rhodopsin kinase 1577:Protein kinase C 1568:Protein kinase C 1553:Protein kinase G 1514:Protein kinase A 1125:Protein kinase B 1057: 1043: 1019: 1012: 1005: 996: 958: 955: 949: 948: 911: 905: 904: 894: 877:(3): 1107–1117. 862: 856: 855: 845: 813: 807: 806: 796: 779:(3): 1305–1318. 760: 754: 753: 735: 711: 705: 704: 686: 662: 656: 655: 645: 621: 615: 614: 596: 572: 566: 565: 537: 531: 530: 512: 488: 482: 481: 445: 439: 438: 419:10.1038/35048096 402: 396: 395: 358: 352: 351: 315: 309: 308: 280: 213:Aurora structure 202: 188: 174: 87:Drug development 21: 4161: 4160: 4156: 4155: 4154: 4152: 4151: 4150: 4126: 4125: 4124: 4112: 4104: 4102: 4097: 4009:Oxidoreductases 3995: 3971:Enzyme kinetics 3959: 3955:List of enzymes 3928: 3897: 3868:Catalytic triad 3846: 3841: 3811: 3802: 3773: 3751: 3726: 3697: 3691: 3687:2.7.10-2.7.13: 3678: 3662: 3629:: miscellaneous 3617: 3591: 3573: 3550: 3533:exoribonuclease 3530: 3518: 3504:Polyadenylation 3421: 3247: 3241: 3229: 3211: 3207: 3201: 3185: 3147: 3134: 3111: 3083: 2913: 2907: 2899: 2893: 2879: 2849: 2836: 2784: 2762: 2686: 2669: 2652: 2635: 2606: 2466: 2366: 2337:P70-S6 Kinase 1 2307: 2198: 2160: 2138: 2104: 2080: 2041: 2007: 1713: 1684: 1660: 1641: 1562: 1538: 1499: 1455: 1438: 1414: 1408:Aurora C kinase 1403:Aurora B kinase 1398:Aurora A kinase 1378: 1359: 1325: 1296: 1229: 1195: 1051: 1037: 1023: 966: 961: 956: 952: 917:Nature Medicine 913: 912: 908: 864: 863: 859: 815: 814: 810: 762: 761: 757: 713: 712: 708: 671:Cancer Research 664: 663: 659: 630:Cancer Research 623: 622: 618: 574: 573: 569: 539: 538: 534: 490: 489: 485: 462:10.1038/nrc1502 456:(12): 927–936. 447: 446: 442: 404: 403: 399: 364:Nature Genetics 360: 359: 355: 317: 316: 312: 282: 281: 277: 273: 251: 227:activation loop 215: 208: 203: 194: 189: 180: 175: 163:Merck & Co. 132:prostate cancer 113:phosphorylating 105:Aurora Borealis 89: 23: 22: 15: 12: 11: 5: 4159: 4157: 4149: 4148: 4143: 4138: 4128: 4127: 4123: 4122: 4099: 4098: 4096: 4095: 4082: 4069: 4056: 4043: 4030: 4017: 4003: 4001: 3997: 3996: 3994: 3993: 3988: 3983: 3978: 3973: 3967: 3965: 3961: 3960: 3958: 3957: 3952: 3947: 3942: 3936: 3934: 3933:Classification 3930: 3929: 3927: 3926: 3921: 3916: 3911: 3905: 3903: 3899: 3898: 3896: 3895: 3890: 3885: 3880: 3875: 3870: 3865: 3860: 3854: 3852: 3848: 3847: 3842: 3840: 3839: 3832: 3825: 3817: 3808: 3807: 3804: 3803: 3801: 3800: 3795: 3790: 3784: 3782: 3775: 3774: 3772: 3771: 3762: 3760: 3753: 3752: 3750: 3749: 3740: 3738: 3728: 3727: 3725: 3724: 3715: 3713: 3700: 3695: 3689:protein kinase 3684: 3683: 3680: 3679: 3677: 3676: 3670: 3668: 3664: 3663: 3661: 3660: 3655: 3650: 3645: 3639: 3637: 3630: 3623: 3622: 3619: 3618: 3616: 3615: 3610: 3599: 3597: 3593: 3592: 3590: 3589: 3583: 3581: 3575: 3574: 3572: 3571: 3566: 3560: 3558: 3552: 3551: 3549: 3548: 3543: 3537: 3535: 3528:Phosphorolytic 3524: 3523: 3520: 3519: 3517: 3516: 3511: 3506: 3501: 3496: 3495: 3494: 3489: 3484: 3474: 3473: 3472: 3462: 3457: 3452: 3447: 3442: 3437: 3431: 3429: 3427:RNA polymerase 3423: 3422: 3420: 3419: 3418: 3417: 3407: 3403: 3402: 3401: 3400: 3395: 3390: 3379: 3378: 3377: 3372: 3367: 3362: 3351: 3345: 3344: 3343: 3336: 3331: 3326: 3321: 3310: 3309: 3308: 3301: 3296: 3291: 3286: 3275: 3271: 3269: 3267:DNA polymerase 3260: 3251: 3245: 3231: 3230: 3228: 3227: 3222: 3216: 3214: 3209: 3205: 3191: 3190: 3187: 3186: 3184: 3183: 3178: 3173: 3168: 3163: 3158: 3152: 3150: 3145: 3136: 3135: 3133: 3132: 3126: 3124: 3113: 3112: 3110: 3109: 3104: 3098: 3096: 3085: 3084: 3082: 3081: 3076: 3071: 3070: 3069: 3064: 3054: 3052:Diacylglycerol 3049: 3044: 3039: 3034: 3029: 3024: 3019: 3014: 3013: 3012: 3002: 2997: 2992: 2991: 2990: 2985: 2980: 2975: 2970: 2963:Phosphofructo- 2960: 2955: 2954: 2953: 2943: 2938: 2932: 2930: 2916: 2911: 2895: 2894: 2880: 2878: 2877: 2870: 2863: 2855: 2846: 2845: 2842: 2841: 2838: 2837: 2835: 2834: 2829: 2824: 2819: 2814: 2809: 2804: 2798: 2796: 2786: 2785: 2779: 2772: 2771: 2768: 2767: 2764: 2763: 2761: 2760: 2755: 2750: 2745: 2740: 2735: 2730: 2725: 2724: 2723: 2718: 2713: 2708: 2697: 2695: 2694:(EC 2.7.11.30) 2688: 2687: 2685: 2684: 2680: 2678: 2677:(EC 2.7.11.29) 2671: 2670: 2668: 2667: 2663: 2661: 2660:(EC 2.7.11.28) 2654: 2653: 2651: 2650: 2646: 2644: 2643:(EC 2.7.11.27) 2637: 2636: 2634: 2633: 2628: 2623: 2617: 2615: 2614:(EC 2.7.11.26) 2608: 2607: 2605: 2604: 2599: 2594: 2593: 2592: 2587: 2582: 2577: 2572: 2567: 2562: 2552: 2551: 2550: 2545: 2540: 2535: 2525: 2524: 2523: 2518: 2513: 2508: 2503: 2498: 2493: 2488: 2477: 2475: 2474:(EC 2.7.11.25) 2468: 2467: 2465: 2464: 2463: 2462: 2457: 2452: 2442: 2441: 2440: 2435: 2430: 2420: 2419: 2418: 2413: 2408: 2403: 2398: 2393: 2388: 2377: 2375: 2374:(EC 2.7.11.24) 2368: 2367: 2365: 2364: 2359: 2354: 2349: 2344: 2339: 2334: 2329: 2324: 2318: 2316: 2315:(EC 2.7.11.23) 2309: 2308: 2306: 2305: 2300: 2295: 2290: 2285: 2280: 2275: 2270: 2265: 2260: 2255: 2250: 2245: 2240: 2235: 2230: 2225: 2220: 2215: 2209: 2207: 2206:(EC 2.7.11.22) 2200: 2199: 2197: 2196: 2191: 2186: 2181: 2175: 2173: 2172:(EC 2.7.11.21) 2162: 2161: 2155: 2148: 2147: 2144: 2143: 2140: 2139: 2137: 2136: 2131: 2126: 2121: 2115: 2113: 2112:(EC 2.7.11.21) 2106: 2105: 2103: 2102: 2097: 2091: 2089: 2088:(EC 2.7.11.20) 2082: 2081: 2079: 2078: 2073: 2068: 2063: 2058: 2052: 2050: 2049:(EC 2.7.11.19) 2043: 2042: 2040: 2039: 2034: 2029: 2024: 2018: 2016: 2015:(EC 2.7.11.18) 2009: 2008: 2006: 2005: 2000: 1995: 1990: 1985: 1980: 1975: 1970: 1965: 1960: 1955: 1950: 1945: 1940: 1935: 1930: 1925: 1920: 1915: 1910: 1905: 1900: 1895: 1890: 1885: 1880: 1875: 1870: 1865: 1860: 1855: 1850: 1845: 1840: 1835: 1830: 1825: 1820: 1815: 1810: 1805: 1800: 1795: 1790: 1785: 1780: 1775: 1770: 1765: 1760: 1755: 1750: 1745: 1740: 1735: 1730: 1724: 1722: 1721:(EC 2.7.11.17) 1715: 1714: 1712: 1711: 1706: 1701: 1695: 1693: 1692:(EC 2.7.11.16) 1686: 1685: 1683: 1682: 1677: 1671: 1669: 1668:(EC 2.7.11.15) 1662: 1661: 1659: 1658: 1652: 1650: 1649:(EC 2.7.11.14) 1643: 1642: 1640: 1639: 1634: 1629: 1624: 1619: 1614: 1609: 1604: 1599: 1594: 1589: 1584: 1579: 1573: 1571: 1570:(EC 2.7.11.13) 1564: 1563: 1561: 1560: 1555: 1549: 1547: 1546:(EC 2.7.11.12) 1540: 1539: 1537: 1536: 1531: 1526: 1521: 1516: 1510: 1508: 1507:(EC 2.7.11.11) 1501: 1500: 1498: 1497: 1492: 1487: 1482: 1477: 1472: 1466: 1464: 1463:(EC 2.7.11.10) 1457: 1456: 1454: 1453: 1449: 1447: 1440: 1439: 1437: 1436: 1431: 1425: 1423: 1416: 1415: 1413: 1412: 1411: 1410: 1405: 1400: 1389: 1387: 1380: 1379: 1377: 1376: 1370: 1368: 1361: 1360: 1358: 1357: 1352: 1347: 1342: 1336: 1334: 1327: 1326: 1324: 1323: 1318: 1313: 1307: 1305: 1298: 1297: 1295: 1294: 1293: 1292: 1287: 1282: 1274: 1273: 1272: 1267: 1259: 1258: 1257: 1252: 1240: 1238: 1231: 1230: 1228: 1227: 1222: 1217: 1212: 1206: 1204: 1197: 1196: 1194: 1193: 1192: 1191: 1181: 1180: 1179: 1174: 1169: 1164: 1154: 1149: 1144: 1143: 1142: 1137: 1132: 1122: 1117: 1112: 1107: 1102: 1097: 1092: 1087: 1082: 1077: 1072: 1066: 1064: 1053: 1052: 1046: 1039: 1038: 1024: 1022: 1021: 1014: 1007: 999: 993: 992: 982: 977: 972: 965: 964:External links 962: 960: 959: 950: 929:10.1038/nm1003 923:(3): 262–267. 906: 857: 828:(2): 281–294. 808: 755: 706: 677:(2): 463–467. 657: 616: 567: 542:Genes to Cells 532: 483: 440: 397: 376:10.1038/ng1220 370:(4): 403–412. 353: 326:(4): 451–464. 310: 291:(6): 672–683. 274: 272: 269: 268: 267: 262: 257: 250: 247: 239:hydrogen bonds 231:protein kinase 214: 211: 210: 209: 204: 197: 195: 190: 183: 181: 176: 169: 155:clinical trial 88: 85: 24: 14: 13: 10: 9: 6: 4: 3: 2: 4158: 4147: 4144: 4142: 4139: 4137: 4134: 4133: 4131: 4121: 4116: 4111: 4107: 4093: 4089: 4088: 4083: 4080: 4076: 4075: 4070: 4067: 4063: 4062: 4057: 4054: 4050: 4049: 4044: 4041: 4037: 4036: 4031: 4028: 4024: 4023: 4018: 4015: 4011: 4010: 4005: 4004: 4002: 3998: 3992: 3989: 3987: 3984: 3982: 3979: 3977: 3974: 3972: 3969: 3968: 3966: 3962: 3956: 3953: 3951: 3950:Enzyme family 3948: 3946: 3943: 3941: 3938: 3937: 3935: 3931: 3925: 3922: 3920: 3917: 3915: 3914:Cooperativity 3912: 3910: 3907: 3906: 3904: 3900: 3894: 3891: 3889: 3886: 3884: 3881: 3879: 3876: 3874: 3873:Oxyanion hole 3871: 3869: 3866: 3864: 3861: 3859: 3856: 3855: 3853: 3849: 3845: 3838: 3833: 3831: 3826: 3824: 3819: 3818: 3815: 3799: 3796: 3794: 3791: 3789: 3786: 3785: 3783: 3780: 3776: 3770: 3769: 3764: 3763: 3761: 3758: 3754: 3748: 3747: 3742: 3741: 3739: 3737: 3733: 3729: 3723: 3722: 3717: 3716: 3714: 3712: 3708: 3704: 3701: 3698: 3690: 3685: 3675: 3672: 3671: 3669: 3665: 3659: 3656: 3654: 3651: 3649: 3646: 3644: 3641: 3640: 3638: 3634: 3631: 3628: 3624: 3614: 3611: 3608: 3604: 3601: 3600: 3598: 3594: 3588: 3585: 3584: 3582: 3580: 3576: 3570: 3567: 3565: 3562: 3561: 3559: 3557: 3553: 3547: 3544: 3542: 3539: 3538: 3536: 3534: 3529: 3525: 3515: 3512: 3510: 3507: 3505: 3502: 3500: 3497: 3493: 3490: 3488: 3485: 3483: 3480: 3479: 3478: 3475: 3471: 3468: 3467: 3466: 3463: 3461: 3458: 3456: 3453: 3451: 3448: 3446: 3443: 3441: 3438: 3436: 3433: 3432: 3430: 3428: 3424: 3416: 3413: 3412: 3411: 3408: 3405: 3404: 3399: 3396: 3394: 3391: 3389: 3386: 3385: 3383: 3380: 3376: 3373: 3371: 3368: 3366: 3363: 3361: 3358: 3357: 3355: 3352: 3349: 3346: 3342: 3341: 3337: 3335: 3332: 3330: 3327: 3325: 3322: 3320: 3317: 3316: 3314: 3311: 3307: 3306: 3302: 3300: 3297: 3295: 3292: 3290: 3287: 3285: 3282: 3281: 3279: 3276: 3273: 3272: 3270: 3268: 3264: 3261: 3259: 3255: 3252: 3249: 3240: 3236: 3232: 3226: 3223: 3221: 3218: 3217: 3215: 3212: 3200: 3196: 3192: 3182: 3179: 3177: 3174: 3172: 3169: 3167: 3164: 3162: 3159: 3157: 3154: 3153: 3151: 3148: 3141: 3137: 3131: 3128: 3127: 3125: 3122: 3118: 3114: 3108: 3105: 3103: 3100: 3099: 3097: 3094: 3090: 3086: 3080: 3077: 3075: 3072: 3068: 3067:Class II PI 3 3065: 3063: 3060: 3059: 3058: 3055: 3053: 3050: 3048: 3045: 3043: 3042:Deoxycytidine 3040: 3038: 3035: 3033: 3030: 3028: 3025: 3023: 3020: 3018: 3015: 3011: 3010:ADP-thymidine 3008: 3007: 3006: 3003: 3001: 2998: 2996: 2993: 2989: 2986: 2984: 2981: 2979: 2976: 2974: 2971: 2969: 2966: 2965: 2964: 2961: 2959: 2956: 2952: 2949: 2948: 2947: 2944: 2942: 2939: 2937: 2934: 2933: 2931: 2928: 2924: 2920: 2917: 2914: 2906: 2902: 2896: 2891: 2887: 2883: 2876: 2871: 2869: 2864: 2862: 2857: 2856: 2853: 2833: 2830: 2828: 2825: 2823: 2820: 2818: 2815: 2813: 2810: 2808: 2805: 2803: 2800: 2799: 2797: 2795: 2791: 2787: 2782: 2777: 2773: 2759: 2756: 2754: 2751: 2749: 2746: 2744: 2741: 2739: 2736: 2734: 2731: 2729: 2726: 2722: 2719: 2717: 2714: 2712: 2709: 2707: 2704: 2703: 2702: 2699: 2698: 2696: 2693: 2689: 2682: 2681: 2679: 2676: 2672: 2665: 2664: 2662: 2659: 2655: 2648: 2647: 2645: 2642: 2638: 2632: 2629: 2627: 2624: 2622: 2619: 2618: 2616: 2613: 2609: 2603: 2600: 2598: 2595: 2591: 2588: 2586: 2583: 2581: 2578: 2576: 2573: 2571: 2568: 2566: 2563: 2561: 2558: 2557: 2556: 2553: 2549: 2546: 2544: 2541: 2539: 2536: 2534: 2531: 2530: 2529: 2526: 2522: 2519: 2517: 2514: 2512: 2509: 2507: 2504: 2502: 2499: 2497: 2494: 2492: 2489: 2487: 2484: 2483: 2482: 2479: 2478: 2476: 2473: 2469: 2461: 2458: 2456: 2453: 2451: 2448: 2447: 2446: 2443: 2439: 2436: 2434: 2431: 2429: 2426: 2425: 2424: 2421: 2417: 2414: 2412: 2409: 2407: 2404: 2402: 2399: 2397: 2394: 2392: 2389: 2387: 2384: 2383: 2382: 2379: 2378: 2376: 2373: 2369: 2363: 2360: 2358: 2355: 2353: 2350: 2348: 2345: 2343: 2340: 2338: 2335: 2333: 2330: 2328: 2325: 2323: 2320: 2319: 2317: 2314: 2310: 2304: 2301: 2299: 2296: 2294: 2291: 2289: 2286: 2284: 2281: 2279: 2276: 2274: 2271: 2269: 2266: 2264: 2261: 2259: 2256: 2254: 2251: 2249: 2246: 2244: 2241: 2239: 2236: 2234: 2231: 2229: 2226: 2224: 2221: 2219: 2216: 2214: 2211: 2210: 2208: 2205: 2201: 2195: 2192: 2190: 2187: 2185: 2182: 2180: 2177: 2176: 2174: 2171: 2167: 2163: 2158: 2153: 2149: 2135: 2132: 2130: 2127: 2125: 2122: 2120: 2117: 2116: 2114: 2111: 2107: 2101: 2098: 2096: 2093: 2092: 2090: 2087: 2083: 2077: 2074: 2072: 2069: 2067: 2064: 2062: 2059: 2057: 2054: 2053: 2051: 2048: 2044: 2038: 2035: 2033: 2030: 2028: 2025: 2023: 2020: 2019: 2017: 2014: 2010: 2004: 2001: 1999: 1996: 1994: 1991: 1989: 1986: 1984: 1981: 1979: 1976: 1974: 1971: 1969: 1966: 1964: 1961: 1959: 1956: 1954: 1951: 1949: 1946: 1944: 1941: 1939: 1936: 1934: 1931: 1929: 1926: 1924: 1921: 1919: 1916: 1914: 1911: 1909: 1906: 1904: 1901: 1899: 1896: 1894: 1891: 1889: 1886: 1884: 1881: 1879: 1876: 1874: 1871: 1869: 1866: 1864: 1861: 1859: 1856: 1854: 1851: 1849: 1846: 1844: 1841: 1839: 1836: 1834: 1831: 1829: 1826: 1824: 1821: 1819: 1816: 1814: 1811: 1809: 1806: 1804: 1801: 1799: 1796: 1794: 1791: 1789: 1786: 1784: 1781: 1779: 1776: 1774: 1771: 1769: 1766: 1764: 1761: 1759: 1756: 1754: 1751: 1749: 1746: 1744: 1741: 1739: 1736: 1734: 1731: 1729: 1726: 1725: 1723: 1720: 1716: 1710: 1707: 1705: 1702: 1700: 1697: 1696: 1694: 1691: 1687: 1681: 1678: 1676: 1673: 1672: 1670: 1667: 1663: 1657: 1654: 1653: 1651: 1648: 1644: 1638: 1635: 1633: 1630: 1628: 1625: 1623: 1620: 1618: 1615: 1613: 1610: 1608: 1605: 1603: 1600: 1598: 1595: 1593: 1590: 1588: 1585: 1583: 1580: 1578: 1575: 1574: 1572: 1569: 1565: 1559: 1556: 1554: 1551: 1550: 1548: 1545: 1541: 1535: 1532: 1530: 1527: 1525: 1522: 1520: 1517: 1515: 1512: 1511: 1509: 1506: 1502: 1496: 1493: 1491: 1488: 1486: 1483: 1481: 1478: 1476: 1473: 1471: 1468: 1467: 1465: 1462: 1458: 1451: 1450: 1448: 1446:(EC 2.7.11.9) 1445: 1441: 1435: 1432: 1430: 1427: 1426: 1424: 1422:(EC 2.7.11.8) 1421: 1417: 1409: 1406: 1404: 1401: 1399: 1396: 1395: 1394: 1393:Aurora kinase 1391: 1390: 1388: 1386:(EC 2.7.11.7) 1385: 1381: 1375: 1372: 1371: 1369: 1367:(EC 2.7.11.6) 1366: 1362: 1356: 1353: 1351: 1348: 1346: 1343: 1341: 1338: 1337: 1335: 1333:(EC 2.7.11.5) 1332: 1328: 1322: 1319: 1317: 1314: 1312: 1309: 1308: 1306: 1304:(EC 2.7.11.4) 1303: 1299: 1291: 1288: 1286: 1283: 1281: 1278: 1277: 1275: 1271: 1268: 1266: 1263: 1262: 1260: 1256: 1253: 1251: 1248: 1247: 1245: 1242: 1241: 1239: 1237:(EC 2.7.11.3) 1236: 1232: 1226: 1223: 1221: 1218: 1216: 1213: 1211: 1208: 1207: 1205: 1203:(EC 2.7.11.2) 1202: 1198: 1190: 1187: 1186: 1185: 1182: 1178: 1175: 1173: 1170: 1168: 1165: 1163: 1160: 1159: 1158: 1157:EIF-2 kinases 1155: 1153: 1150: 1148: 1145: 1141: 1138: 1136: 1133: 1131: 1128: 1127: 1126: 1123: 1121: 1118: 1116: 1113: 1111: 1108: 1106: 1103: 1101: 1098: 1096: 1093: 1091: 1088: 1086: 1083: 1081: 1078: 1076: 1073: 1071: 1068: 1067: 1065: 1063:(EC 2.7.11.1) 1062: 1058: 1054: 1049: 1044: 1040: 1035: 1031: 1027: 1020: 1015: 1013: 1008: 1006: 1001: 1000: 997: 990: 986: 983: 981: 978: 976: 973: 971: 968: 967: 963: 954: 951: 946: 942: 938: 934: 930: 926: 922: 918: 910: 907: 902: 898: 893: 888: 884: 880: 876: 872: 868: 861: 858: 853: 849: 844: 839: 835: 831: 827: 823: 819: 812: 809: 804: 800: 795: 790: 786: 782: 778: 774: 770: 768: 759: 756: 751: 747: 743: 739: 734: 729: 725: 721: 717: 710: 707: 702: 698: 694: 690: 685: 680: 676: 672: 668: 661: 658: 653: 649: 644: 639: 635: 631: 627: 620: 617: 612: 608: 604: 600: 595: 590: 586: 582: 578: 571: 568: 563: 559: 555: 551: 547: 543: 536: 533: 528: 524: 520: 516: 511: 506: 502: 498: 494: 487: 484: 479: 475: 471: 467: 463: 459: 455: 451: 444: 441: 436: 432: 428: 424: 420: 416: 412: 408: 401: 398: 393: 389: 385: 381: 377: 373: 369: 365: 357: 354: 349: 345: 341: 337: 333: 329: 325: 321: 314: 311: 306: 302: 298: 294: 290: 286: 279: 276: 270: 266: 263: 261: 258: 256: 253: 252: 248: 246: 244: 240: 236: 232: 228: 219: 212: 207: 201: 196: 193: 187: 182: 179: 173: 168: 166: 164: 160: 156: 152: 148: 144: 139: 137: 136:breast cancer 133: 129: 125: 121: 117: 114: 110: 106: 102: 98: 94: 86: 84: 82: 79: 75: 71: 67: 63: 59: 54: 52: 48: 47:Aurora kinase 44: 40: 34: 29: 19: 4087:Translocases 4084: 4071: 4058: 4045: 4032: 4022:Transferases 4019: 4006: 3863:Binding site 3765: 3743: 3718: 3339: 3304: 3062:Class I PI 3 3027:Pantothenate 2898:2.7.1-2.7.4: 2882:Transferases 2332:P70S6 kinase 953: 920: 916: 909: 874: 870: 860: 825: 821: 811: 776: 772: 766: 758: 723: 719: 709: 674: 670: 660: 633: 629: 619: 584: 580: 570: 548:(1): 11–17. 545: 541: 535: 500: 496: 486: 453: 449: 443: 413:(1): 21–32. 410: 406: 400: 367: 363: 356: 323: 319: 313: 288: 284: 278: 224: 140: 128:colon cancer 90: 55: 38: 37: 3858:Active site 3613:Transposase 3603:Recombinase 3248:-nucleoside 3074:Sphingosine 2783:(EC 2.7.12) 2170:Polo kinase 2110:Polo kinase 726:(1): 1–10. 74:oncogenesis 62:cytokinesis 33:cytokinesis 4136:Cell cycle 4130:Categories 4061:Isomerases 4035:Hydrolases 3902:Regulation 3415:Telomerase 3258:Polymerase 3032:Mevalonate 2995:Riboflavin 2886:phosphorus 1461:IÎşB kinase 1036:2.7.11-12) 991:-animation 271:References 192:Hesperadin 147:hesperadin 109:nucleosome 78:penetrance 58:cell cycle 3940:EC number 3607:Integrase 3531:3' to 5' 3176:Guanylate 3171:Uridylate 3161:Adenylate 3005:Thymidine 3000:Shikimate 1587:PKC alpha 769:Extracts" 435:205011994 235:adenosine 120:oncogenic 70:mammalian 3964:Kinetics 3888:Cofactor 3851:Activity 3541:RNase PH 3149:acceptor 3130:Creatine 3123:acceptor 3095:acceptor 3037:Pyruvate 3022:Glycerol 2983:Platelet 2958:Galacto- 2929:acceptor 1943:KIAA0999 1838:MAPKAPK5 1833:MAPKAPK3 1828:MAPKAPK2 945:12918452 937:14981513 901:17215513 852:12707311 803:15616188 750:22233833 742:17259342 701:11727346 693:14744757 652:16707419 611:30767479 603:17164288 562:11856369 527:34256297 519:17145803 478:28256419 470:15573114 427:11413462 392:29442841 384:12881723 348:25350728 340:12884918 305:14644191 249:See also 178:ZM447439 143:ZM447439 138:tumors. 124:leukemia 4141:Mitosis 4120:Biology 4074:Ligases 3844:Enzymes 3492:PrimPol 3477:Primase 2951:Hepatic 2946:Fructo- 2602:MAP3K14 2580:MAP3K11 2575:MAP3K10 2565:MAP3K13 2560:MAP3K12 2362:RPS6KC1 2357:RPS6KA1 2352:RPS6KA3 2347:RPS6KA2 2342:RPS6KB2 2327:RPS6KA4 2322:RPS6KA5 1973:Kalirin 1938:SNF1LK2 1177:EIF2AK4 1172:EIF2AK3 1026:Kinases 987:- PMAP 892:1805108 843:2172906 116:histone 101:mitotic 97:mitosis 93:enzymes 45:. The 4106:Portal 4048:Lyases 3779:2.7.13 3757:2.7.12 3732:2.7.11 3707:2.7.10 3546:PNPase 3514:PNPase 3470:POLRMT 3465:ssRNAP 2978:Muscle 2941:Gluco- 2905:kinase 2832:MAP2K7 2827:MAP2K6 2822:MAP2K5 2817:MAP2K4 2812:MAP2K3 2807:MAP2K2 2802:MAP2K1 2753:ACVRL1 2748:ACVR2B 2743:ACVR2A 2738:ACVR1C 2733:ACVR1B 2716:BMPR1B 2711:BMPR1A 2585:MAP3K7 2570:MAP3K9 2521:MAP3K8 2516:MAP3K7 2511:MAP3K6 2506:MAP3K5 2501:MAP3K4 2496:MAP3K3 2491:MAP3K2 2486:MAP3K1 2460:MAPK14 2455:MAPK13 2450:MAPK11 2438:MAPK10 2416:MAPK15 2411:MAPK12 2303:CDC2L1 2278:CDC2L5 1953:SNF1LK 1778:CAMK2G 1773:CAMK2D 1768:CAMK2B 1763:CAMK2A 1753:CAMK1G 1748:CAMK1D 1743:CAMK1B 1738:CAMK1A 1592:PRKCB1 1529:PRKACA 1524:PRKACB 1519:PRKACG 1495:IKBKAP 1321:BCKDHB 1316:BCKDHA 1290:PRKAG3 1285:PRKAG2 1280:PRKAG1 1270:PRKAB2 1265:PRKAB1 1255:PRKAA2 1250:PRKAA1 1095:STK38L 943:  935:  899:  889:  850:  840:  801:  794:551494 791:  748:  740:  699:  691:  650:  609:  601:  560:  525:  517:  476:  468:  433:  425:  390:  382:  346:  338:  303:  255:Kinome 243:ribose 206:VX-680 151:VX-680 66:cancer 43:cancer 4000:Types 3627:2.7.8 3596:Other 3235:2.7.7 3195:2.7.6 3140:2.7.4 3117:2.7.3 3089:2.7.2 2973:Liver 2936:Hexo- 2923:2.7.1 2794:MAP2K 2728:ACVR1 2721:BMPR2 2706:BMPR1 2631:GSK-3 2472:MAP3K 2433:MAPK9 2428:MAPK8 2406:MAPK7 2401:MAPK6 2396:MAPK4 2391:MAPK3 2386:MAPK1 2298:PFTK1 2293:PCTK3 2288:PCTK2 2283:PCTK1 2273:CDK12 2268:CDK10 2243:CDKL5 2223:CDKL2 2100:STK19 2095:EEF2K 2076:PHKG2 2071:PHKG1 2061:PHKA2 2056:PHKA1 2037:MYLK4 2032:MYLK3 2027:MYLK2 2003:DCLK1 1998:Titin 1988:TRIB3 1983:TRIB2 1978:TRIB1 1968:TSSK2 1948:STK40 1933:PSKH1 1928:PRKD3 1923:PRKD2 1903:PHKG2 1898:PHKG1 1888:OBSCN 1883:NUAK2 1878:NUAK1 1873:MKNK2 1868:MKNK1 1858:MARK4 1853:MARK3 1848:MARK2 1843:MARK1 1823:STK11 1818:DAPK3 1813:DAPK2 1808:DAPK1 1803:CHEK2 1798:CHEK1 1783:CAMK4 1758:CAMK2 1733:CAMK1 1728:BRSK2 1622:PRKCQ 1617:PRKCI 1612:PRKCG 1607:PRKCH 1602:PRKCE 1597:PRKCD 1558:PRKG1 1490:IKBKG 1485:IKBKE 1434:STK10 1429:FASTK 1355:IDH3G 1350:IDH3B 1345:IDH3A 1311:BCKDK 1105:ROCK1 1090:STK38 1085:MAST2 1080:MAST1 1075:LATS2 1070:LATS1 941:S2CID 746:S2CID 697:S2CID 607:S2CID 523:S2CID 474:S2CID 431:S2CID 388:S2CID 344:S2CID 81:tumor 4092:list 4085:EC7 4079:list 4072:EC6 4066:list 4059:EC5 4053:list 4046:EC4 4040:list 4033:EC3 4027:list 4020:EC2 4014:list 4007:EC1 3766:see 3744:see 3719:see 3093:COOH 2892:2.7) 2621:TPK1 2597:CDC7 2555:MLKs 2548:KSR2 2543:KSR1 2538:BRAF 2533:ARAF 2528:RAFs 2263:CDK9 2258:CDK8 2253:CDK7 2248:CDK6 2238:CDK5 2233:CDK4 2228:CDK3 2218:CDK2 2213:CDK1 2194:PLK4 2189:PLK3 2184:PLK2 2179:PLK1 2134:PLK4 2129:PLK3 2124:PLK2 2119:PLK1 2066:PHKB 2022:MYLK 1993:TRIO 1963:SPEG 1958:SNRK 1918:PKD1 1913:PIM2 1908:PIM1 1893:PASK 1863:MELK 1793:CASK 1788:MLCK 1709:GRK6 1704:GRK5 1699:GRK4 1637:PKN3 1632:PKN2 1534:PRKY 1480:TBK1 1475:IKK2 1470:CHUK 1374:STK4 1340:IDH2 1225:PDK4 1220:PDK3 1215:PDK2 1210:PDK1 1189:WEE1 1184:Wee1 1152:mTOR 1140:AKT3 1135:AKT2 1130:AKT1 1120:SGK3 1115:SGK2 933:PMID 897:PMID 848:PMID 799:PMID 738:PMID 689:PMID 648:PMID 599:PMID 558:PMID 515:PMID 466:PMID 423:PMID 380:PMID 336:PMID 301:PMID 149:and 134:and 3509:PAP 3450:III 3384:/Y 3375:TDT 3356:/X 3348:III 3340:Pfu 3315:/B 3305:Taq 3280:/A 3047:PFP 3017:NAD 2626:TTK 2590:ZAK 1167:HRI 1162:PKR 1110:SGK 1100:CIT 925:doi 887:PMC 879:doi 838:PMC 830:doi 826:161 789:PMC 781:doi 767:Egg 728:doi 679:doi 638:doi 589:doi 585:120 550:doi 505:doi 458:doi 415:doi 372:doi 328:doi 293:doi 111:by 4132:: 3734:: 3709:: 3694:PO 3455:IV 3445:II 3354:IV 3350:/C 3313:II 3299:T7 3244:PO 3237:: 3197:: 3144:PO 3142:: 3119:: 3091:: 2927:OH 2925:: 2910:PO 2890:EC 2884:: 1276:Îł 1261:β 1246:α 1034:EC 1028:: 939:. 931:. 921:10 919:. 895:. 885:. 875:18 873:. 869:. 846:. 836:. 824:. 820:. 797:. 787:. 777:16 775:. 771:. 744:. 736:. 722:. 718:. 695:. 687:. 675:64 673:. 669:. 646:. 634:66 632:. 628:. 605:. 597:. 583:. 579:. 556:. 544:. 521:. 513:. 501:12 499:. 495:. 472:. 464:. 452:. 429:. 421:. 409:. 386:. 378:. 368:34 366:. 342:. 334:. 324:22 322:. 299:. 289:15 287:. 145:, 130:, 126:, 53:. 4108:: 4094:) 4090:( 4081:) 4077:( 4068:) 4064:( 4055:) 4051:( 4042:) 4038:( 4029:) 4025:( 4016:) 4012:( 3836:e 3829:t 3822:v 3696:4 3692:( 3609:) 3605:( 3487:2 3482:1 3460:V 3398:Îş 3393:Îą 3388:η 3382:V 3370:ÎĽ 3365:λ 3360:β 3334:ζ 3329:ε 3324:δ 3319:α 3294:ν 3289:θ 3284:Îł 3278:I 3250:) 3246:4 3242:( 3213:) 3210:7 3208:O 3206:2 3204:P 3202:( 3146:4 3121:N 2988:2 2968:1 2915:) 2912:4 2908:( 2903:/ 2874:e 2867:t 2860:v 2683:- 2666:- 2649:- 1452:- 1032:( 1018:e 1011:t 1004:v 947:. 927:: 903:. 881:: 854:. 832:: 805:. 783:: 752:. 730:: 724:5 703:. 681:: 654:. 640:: 613:. 591:: 564:. 552:: 546:7 529:. 507:: 480:. 460:: 454:4 437:. 417:: 411:2 394:. 374:: 350:. 330:: 307:. 295:: 20:)

Index

Aurora kinase inhibitor

cytokinesis
cancer
Aurora kinase
enzyme inhibitors
cell cycle
cytokinesis
cancer
mammalian
oncogenesis
penetrance
tumor
enzymes
mitosis
mitotic
Aurora Borealis
nucleosome
phosphorylating
histone
oncogenic
leukemia
colon cancer
prostate cancer
breast cancer
ZM447439
hesperadin
VX-680
clinical trial
Vertex Pharmaceuticals

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