Selective Aurora A-TPX2 Interaction Inhibitors Have In Vivo Efficacy as Targeted Antimitotic Agents
Aurora A kinase, a cell division regulator, is frequently overexpressed in various cancers, provoking genome instability and resistance to antimitotic chemotherapy. Localization and enzymatic activity of Aurora A are regulated by its interaction with the spindle assembly factor TPX2. We have used fr...
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| Published in | Journal of medicinal chemistry Vol. 67; no. 17; pp. 15521 - 15536 |
|---|---|
| Main Authors | , , , , , , , , , , , , , , , , , , , , , , , , |
| Format | Journal Article |
| Language | English |
| Published |
WASHINGTON
Amer Chemical Soc
12.09.2024
American Chemical Society |
| Subjects | |
| Online Access | Get full text |
| ISSN | 0022-2623 1520-4804 1520-4804 |
| DOI | 10.1021/acs.jmedchem.4c01165 |
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| Abstract | Aurora A kinase, a cell division regulator, is frequently overexpressed in various cancers, provoking genome instability and resistance to antimitotic chemotherapy. Localization and enzymatic activity of Aurora A are regulated by its interaction with the spindle assembly factor TPX2. We have used fragment-based, structure-guided lead discovery to develop small molecule inhibitors of the Aurora A-TPX2 protein-protein interaction (PPI). Our lead compound, CAM2602, inhibits Aurora A:TPX2 interaction, binding Aurora A with 19 nM affinity. CAM2602 exhibits oral bioavailability, causes pharmacodynamic biomarker modulation, and arrests the growth of tumor xenografts. CAM2602 acts by a novel mechanism compared to ATP-competitive inhibitors and is highly specific to Aurora A over Aurora B. Consistent with our finding that Aurora A overexpression drives taxane resistance, these inhibitors synergize with paclitaxel to suppress the outgrowth of pancreatic cancer cells. Our results provide a blueprint for targeting the Aurora A-TPX2 PPI for cancer therapy and suggest a promising clinical utility for this mode of action. |
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| AbstractList | Aurora A kinase, a cell division regulator, is frequently
overexpressed
in various cancers, provoking genome instability and resistance to
antimitotic chemotherapy. Localization and enzymatic activity of Aurora
A are regulated by its interaction with the spindle assembly factor
TPX2. We have used fragment-based, structure-guided lead discovery
to develop small molecule inhibitors of the Aurora A-TPX2 protein–protein
interaction (PPI). Our lead compound,
CAM2602
, inhibits
Aurora A:TPX2 interaction, binding Aurora A with 19 nM affinity.
CAM2602
exhibits oral bioavailability, causes pharmacodynamic
biomarker modulation, and arrests the growth of tumor xenografts.
CAM2602
acts by a novel mechanism compared to ATP-competitive
inhibitors and is highly specific to Aurora A over Aurora B. Consistent
with our finding that Aurora A overexpression drives taxane resistance,
these inhibitors synergize with paclitaxel to suppress the outgrowth
of pancreatic cancer cells. Our results provide a blueprint for targeting
the Aurora A-TPX2 PPI for cancer therapy and suggest a promising clinical
utility for this mode of action. Aurora A kinase, a cell division regulator, is frequently overexpressed in various cancers, provoking genome instability and resistance to antimitotic chemotherapy. Localization and enzymatic activity of Aurora A are regulated by its interaction with the spindle assembly factor TPX2. We have used fragment-based, structure-guided lead discovery to develop small molecule inhibitors of the Aurora A-TPX2 protein-protein interaction (PPI). Our lead compound, CAM2602, inhibits Aurora A:TPX2 interaction, binding Aurora A with 19 nM affinity. CAM2602 exhibits oral bioavailability, causes pharmacodynamic biomarker modulation, and arrests the growth of tumor xenografts. CAM2602 acts by a novel mechanism compared to ATP-competitive inhibitors and is highly specific to Aurora A over Aurora B. Consistent with our finding that Aurora A overexpression drives taxane resistance, these inhibitors synergize with paclitaxel to suppress the outgrowth of pancreatic cancer cells. Our results provide a blueprint for targeting the Aurora A-TPX2 PPI for cancer therapy and suggest a promising clinical utility for this mode of action.Aurora A kinase, a cell division regulator, is frequently overexpressed in various cancers, provoking genome instability and resistance to antimitotic chemotherapy. Localization and enzymatic activity of Aurora A are regulated by its interaction with the spindle assembly factor TPX2. We have used fragment-based, structure-guided lead discovery to develop small molecule inhibitors of the Aurora A-TPX2 protein-protein interaction (PPI). Our lead compound, CAM2602, inhibits Aurora A:TPX2 interaction, binding Aurora A with 19 nM affinity. CAM2602 exhibits oral bioavailability, causes pharmacodynamic biomarker modulation, and arrests the growth of tumor xenografts. CAM2602 acts by a novel mechanism compared to ATP-competitive inhibitors and is highly specific to Aurora A over Aurora B. Consistent with our finding that Aurora A overexpression drives taxane resistance, these inhibitors synergize with paclitaxel to suppress the outgrowth of pancreatic cancer cells. Our results provide a blueprint for targeting the Aurora A-TPX2 PPI for cancer therapy and suggest a promising clinical utility for this mode of action. Aurora A kinase, a cell division regulator, is frequently overexpressed in various cancers, provoking genome instability and resistance to antimitotic chemotherapy. Localization and enzymatic activity of Aurora A are regulated by its interaction with the spindle assembly factor TPX2. We have used fragment-based, structure-guided lead discovery to develop small molecule inhibitors of the Aurora A-TPX2 protein-protein interaction (PPI). Our lead compound, , inhibits Aurora A:TPX2 interaction, binding Aurora A with 19 nM affinity. exhibits oral bioavailability, causes pharmacodynamic biomarker modulation, and arrests the growth of tumor xenografts. acts by a novel mechanism compared to ATP-competitive inhibitors and is highly specific to Aurora A over Aurora B. Consistent with our finding that Aurora A overexpression drives taxane resistance, these inhibitors synergize with paclitaxel to suppress the outgrowth of pancreatic cancer cells. Our results provide a blueprint for targeting the Aurora A-TPX2 PPI for cancer therapy and suggest a promising clinical utility for this mode of action. Aurora A kinase, a cell division regulator, is frequently overexpressed in various cancers, provoking genome instability and resistance to antimitotic chemotherapy. Localization and enzymatic activity of Aurora A are regulated by its interaction with the spindle assembly factor TPX2. We have used fragment-based, structure-guided lead discovery to develop small molecule inhibitors of the Aurora A-TPX2 protein-protein interaction (PPI). Our lead compound, CAM2602, inhibits Aurora A:TPX2 interaction, binding Aurora A with 19 nM affinity. CAM2602 exhibits oral bioavailability, causes pharmacodynamic biomarker modulation, and arrests the growth of tumor xenografts. CAM2602 acts by a novel mechanism compared to ATP-competitive inhibitors and is highly specific to Aurora A over Aurora B. Consistent with our finding that Aurora A overexpression drives taxane resistance, these inhibitors synergize with paclitaxel to suppress the outgrowth of pancreatic cancer cells. Our results provide a blueprint for targeting the Aurora A-TPX2 PPI for cancer therapy and suggest a promising clinical utility for this mode of action. |
| Author | Scott, Duncan E. Rocaboy, Mathieu Srinivasan, Rajavel Rossmann, Maxim Alcaide, Anna Alza, Esther Dagostin, Claudio Stockwell, Simon R. Higueruelo, Alicia Skidmore, John McKenzie, Grahame Spring, David R. Rooney, Timothy P. C. Moschetti, Tommaso Blaszczyk, Beata Asteian, Alice Abell, Chris Wang, Xuelu Hyvönen, Marko Fischer, Gerhard Blundell, Tom L. Guarino, Estrella Venkitaraman, Ashok R. Perrior, Trevor R. Feng, Tzu-Shean |
| Author_xml | – sequence: 1 givenname: Simon R. surname: Stockwell fullname: Stockwell, Simon R. organization: Medical Research Council Cancer Unit, University of Cambridge, Cambridge CB2 0XZ, U.K – sequence: 2 givenname: Duncan E. surname: Scott fullname: Scott, Duncan E. organization: Yusuf Hamied Department of Chemistry, University of Cambridge, Cambridge CB2 1EW, U.K – sequence: 3 givenname: Gerhard surname: Fischer fullname: Fischer, Gerhard organization: Department of Biochemistry, University of Cambridge, Cambridge CB2 1GA, U.K – sequence: 4 givenname: Estrella surname: Guarino fullname: Guarino, Estrella organization: Medical Research Council Cancer Unit, University of Cambridge, Cambridge CB2 0XZ, U.K – sequence: 5 givenname: Timothy P. C. orcidid: 0000-0001-6788-5526 surname: Rooney fullname: Rooney, Timothy P. C. organization: Yusuf Hamied Department of Chemistry, University of Cambridge, Cambridge CB2 1EW, U.K – sequence: 6 givenname: Tzu-Shean surname: Feng fullname: Feng, Tzu-Shean organization: Yusuf Hamied Department of Chemistry, University of Cambridge, Cambridge CB2 1EW, U.K – sequence: 7 givenname: Tommaso surname: Moschetti fullname: Moschetti, Tommaso organization: Department of Biochemistry, University of Cambridge, Cambridge CB2 1GA, U.K – sequence: 8 givenname: Rajavel surname: Srinivasan fullname: Srinivasan, Rajavel organization: Yusuf Hamied Department of Chemistry, University of Cambridge, Cambridge CB2 1EW, U.K – sequence: 9 givenname: Esther surname: Alza fullname: Alza, Esther organization: Yusuf Hamied Department of Chemistry, University of Cambridge, Cambridge CB2 1EW, U.K – sequence: 10 givenname: Alice surname: Asteian fullname: Asteian, Alice organization: Yusuf Hamied Department of Chemistry, University of Cambridge, Cambridge CB2 1EW, U.K – sequence: 11 givenname: Claudio surname: Dagostin fullname: Dagostin, Claudio organization: Yusuf Hamied Department of Chemistry, University of Cambridge, Cambridge CB2 1EW, U.K – sequence: 12 givenname: Anna surname: Alcaide fullname: Alcaide, Anna organization: Yusuf Hamied Department of Chemistry, University of Cambridge, Cambridge CB2 1EW, U.K – sequence: 13 givenname: Mathieu surname: Rocaboy fullname: Rocaboy, Mathieu organization: Department of Biochemistry, University of Cambridge, Cambridge CB2 1GA, U.K – sequence: 14 givenname: Beata surname: Blaszczyk fullname: Blaszczyk, Beata organization: Department of Biochemistry, University of Cambridge, Cambridge CB2 1GA, U.K – sequence: 15 givenname: Alicia surname: Higueruelo fullname: Higueruelo, Alicia organization: Department of Biochemistry, University of Cambridge, Cambridge CB2 1GA, U.K – sequence: 16 givenname: Xuelu surname: Wang fullname: Wang, Xuelu organization: Department of Biochemistry, University of Cambridge, Cambridge CB2 1GA, U.K – sequence: 17 givenname: Maxim surname: Rossmann fullname: Rossmann, Maxim organization: Department of Biochemistry, University of Cambridge, Cambridge CB2 1GA, U.K – sequence: 18 givenname: Trevor R. surname: Perrior fullname: Perrior, Trevor R. – sequence: 19 givenname: Tom L. surname: Blundell fullname: Blundell, Tom L. organization: Department of Biochemistry, University of Cambridge, Cambridge CB2 1GA, U.K – sequence: 20 givenname: David R. surname: Spring fullname: Spring, David R. organization: Yusuf Hamied Department of Chemistry, University of Cambridge, Cambridge CB2 1EW, U.K – sequence: 21 givenname: Grahame surname: McKenzie fullname: McKenzie, Grahame organization: Medical Research Council Cancer Unit, University of Cambridge, Cambridge CB2 0XZ, U.K – sequence: 22 givenname: Chris orcidid: 0000-0001-9174-1987 surname: Abell fullname: Abell, Chris organization: Yusuf Hamied Department of Chemistry, University of Cambridge, Cambridge CB2 1EW, U.K – sequence: 23 givenname: John orcidid: 0000-0001-9108-7858 surname: Skidmore fullname: Skidmore, John organization: Yusuf Hamied Department of Chemistry, University of Cambridge, Cambridge CB2 1EW, U.K – sequence: 24 givenname: Ashok R. surname: Venkitaraman fullname: Venkitaraman, Ashok R. organization: Medical Research Council Cancer Unit, University of Cambridge, Cambridge CB2 0XZ, U.K – sequence: 25 givenname: Marko orcidid: 0000-0001-8683-4070 surname: Hyvönen fullname: Hyvönen, Marko organization: Department of Biochemistry, University of Cambridge, Cambridge CB2 1GA, U.K |
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| Cites_doi | 10.1016/j.ygyno.2010.09.003 10.1074/jbc.M306275200 10.3389/fonc.2015.00295 10.1242/jcs.075457 10.1093/protein/gzx017 10.3389/fonc.2015.00285 10.1158/2159-8290.CD-18-0469 10.1007/s00280-011-1618-8 10.1083/jcb.200204155 10.1038/nature08675 10.1038/cdd.2012.169 10.1016/S1535-6108(02)00235-0 10.1038/nrc1502 10.3390/cells12131798 10.1158/1535-7163.MCT-12-1232 10.1016/j.ygeno.2013.03.005 10.1016/j.ccr.2014.07.015 10.1016/j.biotechadv.2014.10.011 10.1016/j.lrr.2014.06.003 10.1038/srep28528 10.1517/14728220903307483 10.1107/S2052520616003954 10.18632/oncotarget.16738 10.3389/fonc.2015.00278 10.1158/1541-7786.MCR-06-0208 10.1002/med.21317 10.1038/s41591-018-0264-7 10.1016/j.ccell.2016.03.001 10.1016/j.chembiol.2017.07.009 10.1021/cb300663j 10.4161/cc.3.4.777 10.1038/s41388-018-0470-2 10.3389/fonc.2016.00088 10.1177/1947601912473306 10.1083/jcb.200802005 10.1002/chem.201900815 10.4161/cc.29267 10.18632/oncotarget.7335 10.1038/nrc.2016.138 10.1158/1078-0432.CCR-12-0571 10.1016/j.tips.2017.05.003 10.1111/j.1399-3038.2008.00843.x 10.1530/ERC-17-0120 10.2174/1568009615666150421110401 10.1158/1535-7163.MCT-09-0323 10.1038/nrm1245 10.1016/j.ctrv.2012.02.011 10.1038/ncb936 10.1158/1078-0432.CCR-11-1536 10.4049/jimmunol.177.2.885 10.1158/1078-0432.CCR-12-0589 10.1038/s41598-017-18210-3 10.1073/pnas.1610626113 10.1158/0008-5472.CAN-05-2796 10.18632/oncotarget.18970 10.1038/onc.2014.14 10.1158/0008-5472.CAN-10-1030 10.1016/j.critrevonc.2017.09.006 10.1016/j.blre.2016.02.001 10.1242/jcs.03145 10.1021/acschembio.7b00537 10.1083/jcb.152.4.669 10.1016/j.bbcan.2010.08.001 10.1016/j.pharmthera.2015.10.002 10.1016/S1097-2765(03)00392-7 10.1158/1535-7163.MCT-10-0299 10.1038/2496 10.1007/s00280-013-2305-8 10.1038/bjc.2012.450 10.1021/acschembio.6b00709 10.1038/s41580-021-00404-3 |
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| Keywords | A ACTIVATION TAXANE RESISTANCE ALISERTIB MLN8237 STRUCTURAL BASIS PANCREATIC-CANCER SOLID TUMORS SAFETY CELL-CYCLE KINASE INHIBITOR PHASE-I SMALL-MOLECULE INHIBITOR |
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| References | ref9/cit9 ref45/cit45 ref3/cit3 ref27/cit27 Cirak Y. (ref12/cit12) 2015; 20 ref63/cit63 ref56/cit56 ref16/cit16 ref52/cit52 ref23/cit23 ref8/cit8 ref31/cit31 ref59/cit59 ref2/cit2 ref34/cit34 ref71/cit71 ref37/cit37 ref20/cit20 ref48/cit48 ref60/cit60 Li D. (ref5/cit5) 2003; 9 ref17/cit17 ref10/cit10 ref35/cit35 ref53/cit53 ref19/cit19 ref21/cit21 ref42/cit42 ref49/cit49 ref13/cit13 ref61/cit61 ref67/cit67 ref24/cit24 ref38/cit38 Bayliss R. (ref46/cit46) 2004; 3 ref50/cit50 ref64/cit64 ref54/cit54 ref6/cit6 ref36/cit36 ref18/cit18 ref65/cit65 ref11/cit11 ref25/cit25 ref29/cit29 ref72/cit72 ref32/cit32 ref39/cit39 ref14/cit14 ref57/cit57 ref51/cit51 ref43/cit43 ref28/cit28 ref40/cit40 ref68/cit68 ref26/cit26 ref55/cit55 ref69/cit69 ref15/cit15 ref62/cit62 ref66/cit66 ref41/cit41 ref58/cit58 ref22/cit22 ref33/cit33 ref4/cit4 ref30/cit30 ref47/cit47 ref1/cit1 ref44/cit44 ref70/cit70 ref7/cit7 Heinzlmeir, S (WOS:000390179700024) 2016; 11 Macarulla, T (WOS:000282724600019) 2010; 9 Palani, S (WOS:000327387000010) 2013; 72 Kaestner, P (WOS:000268005700033) 2009; 8 Neel, NF (WOS:000329815200013) 2014; 13 Wang, SP (WOS:000351321400017) 2015; 33 Visconti, R (WOS:000408115800013) 2017; 24 Carol, H (WOS:000297124400022) 2011; 68 Cervantes, A (WOS:000309964500031) 2012; 18 Manfredi, MG (WOS:000298410300013) 2011; 17 Tsai, MY (WOS:000181322500018) 2003; 5 Gong, XQ (WOS:000458154500013) 2019; 9 Asteriti, IA (WOS:000401003200118) 2017; 8 Anand, S (WOS:000180630600008) 2003; 3 Giet, R (WOS:000167114800004) 2001; 152 Garrido, G (WOS:000374216300001) 2016; 6 Rossmann, M (WOS:000404476100002) 2017; 30 Dees, EC (WOS:000309964500032) 2012; 18 Shafer, D (WOS:000381172200004) 2016; 30 Lee, CC (WOS:000270662700003) 2009; 20 Bayliss, R (WOS:000222361700006) 2004; 3 Giovinazzi, S (WOS:000317264800006) 2013; 20 Wu, P (WOS:000366952600006) 2015; 156 Lee, ECY (WOS:000237679900004) 2006; 66 Keen, N (WOS:000225454300011) 2004; 4 Pérez de Castro, Ignacio (MEDLINE:23634259) 2012; 3 Tayyar, Y (WOS:000415392100008) 2017; 119 Richards, MW (WOS:000388835700063) 2016; 113 Goldenson, B (WOS:000348853500001) 2015; 34 Chakravarty, A (WOS:000286830300008) 2011; 71 de Groot, CO (WOS:000366811700001) 2015; 5 Cirak, Y (WOS:000369355100004) 2015; 20 Giubettini, M (WOS:000285242200013) 2011; 124 Narvaez, AJ (WOS:000407918100012) 2017; 24 Zhang, R (WOS:000471039200023) 2019; 25 McIntyre, PJ (WOS:000416204500026) 2017; 12 Bavetsias, V (WOS:000366811500001) 2015; 5 Murray, S (WOS:000309149400008) 2012; 38 Zhou, HY (WOS:000076231300023) 1998; 20 Ehrlichova, M (WOS:000322848500004) 2013; 102 Nair, JS (WOS:000375679600086) 2016; 7 Ehm, P (WOS:001028537900001) 2023; 12 Bayliss, R (WOS:000186196100010) 2003; 12 Lee, JK (WOS:000373854600016) 2016; 29 Do, TV (WOS:000406717200010) 2017; 8 Lu, SY (WOS:000343826600005) 2014; 34 D'Assoro, AB (WOS:000406742000001) 2016; 5 Marumoto, T (WOS:000187206300114) 2003; 278 Lassus, H (WOS:000285824800003) 2011; 120 Carmena, M (WOS:000186359800013) 2003; 4 Lin, Y (WOS:000310790900005) 2012; 107 Fu, JY (WOS:000243845800001) 2007; 5 Shah, KN (WOS:000455027700029) 2019; 25 van Gijn, SE (WOS:000458006300007) 2019; 38 Stallwood, Y (WOS:000238926500015) 2006; 177 Fang, ZZ (WOS:000314008000007) 2013; 8 Spartà, AM (WOS:000340272100015) 2014; 13 Kufer, TA (WOS:000177649900003) 2002; 158 Gustafson, WC (WOS:000341873800013) 2014; 26 Sarvagalla, S (WOS:000357942000003) 2015; 15 Bird, AW (WOS:000258274900009) 2008; 182 Asteriti, IA (WOS:000285658400011) 2010; 1806 Janecek, M (WOS:000378412200001) 2016; 6 Ochi, T (WOS:000272787300003) 2009; 13 Goldberg, Stuart L (MEDLINE:25068104) 2014; 3 Girdler, F (WOS:000240383500019) 2006; 119 Matthews, HK (WOS:000694780200001) 2022; 23 Groom, CR (WOS:000373989900003) 2016; 72 Kivinummi, K (WOS:000418562100018) 2017; 7 Damodaran, AP (WOS:000405902300003) 2017; 38 Li, DH (WOS:000181430400010) 2003; 9 Zhang, JM (WOS:000273981100042) 2010; 463 |
| References_xml | – ident: ref3/cit3 doi: 10.1016/j.ygyno.2010.09.003 – ident: ref50/cit50 doi: 10.1074/jbc.M306275200 – ident: ref7/cit7 doi: 10.3389/fonc.2015.00295 – ident: ref23/cit23 doi: 10.1242/jcs.075457 – ident: ref72/cit72 doi: 10.1093/protein/gzx017 – ident: ref18/cit18 doi: 10.3389/fonc.2015.00285 – ident: ref48/cit48 doi: 10.1158/2159-8290.CD-18-0469 – ident: ref58/cit58 doi: 10.1007/s00280-011-1618-8 – ident: ref21/cit21 doi: 10.1083/jcb.200204155 – ident: ref41/cit41 doi: 10.1038/nature08675 – ident: ref65/cit65 doi: 10.1038/cdd.2012.169 – ident: ref13/cit13 doi: 10.1016/S1535-6108(02)00235-0 – ident: ref47/cit47 doi: 10.1038/nrc1502 – ident: ref55/cit55 doi: 10.3390/cells12131798 – ident: ref63/cit63 doi: 10.1158/1535-7163.MCT-12-1232 – ident: ref67/cit67 doi: 10.1016/j.ygeno.2013.03.005 – ident: ref36/cit36 doi: 10.1016/j.ccr.2014.07.015 – ident: ref70/cit70 doi: 10.1016/j.biotechadv.2014.10.011 – ident: ref14/cit14 doi: 10.1016/j.lrr.2014.06.003 – ident: ref37/cit37 doi: 10.1038/srep28528 – ident: ref15/cit15 doi: 10.1517/14728220903307483 – ident: ref45/cit45 doi: 10.1107/S2052520616003954 – ident: ref33/cit33 doi: 10.18632/oncotarget.16738 – volume: 9 start-page: 991 issue: 3 year: 2003 ident: ref5/cit5 publication-title: Clin. Cancer Res. – ident: ref17/cit17 doi: 10.3389/fonc.2015.00278 – ident: ref2/cit2 doi: 10.1158/1541-7786.MCR-06-0208 – ident: ref71/cit71 doi: 10.1002/med.21317 – ident: ref11/cit11 doi: 10.1038/s41591-018-0264-7 – ident: ref42/cit42 doi: 10.1016/j.ccell.2016.03.001 – ident: ref40/cit40 doi: 10.1016/j.chembiol.2017.07.009 – ident: ref38/cit38 doi: 10.1021/cb300663j – volume: 3 start-page: 404 issue: 4 year: 2004 ident: ref46/cit46 publication-title: Cell Cycle doi: 10.4161/cc.3.4.777 – ident: ref8/cit8 doi: 10.1038/s41388-018-0470-2 – ident: ref22/cit22 doi: 10.3389/fonc.2016.00088 – ident: ref26/cit26 doi: 10.1177/1947601912473306 – ident: ref20/cit20 doi: 10.1083/jcb.200802005 – ident: ref35/cit35 doi: 10.1002/chem.201900815 – ident: ref54/cit54 doi: 10.4161/cc.29267 – ident: ref62/cit62 doi: 10.18632/oncotarget.7335 – ident: ref28/cit28 doi: 10.1038/nrc.2016.138 – ident: ref60/cit60 doi: 10.1158/1078-0432.CCR-12-0571 – ident: ref19/cit19 doi: 10.1016/j.tips.2017.05.003 – ident: ref56/cit56 doi: 10.1111/j.1399-3038.2008.00843.x – ident: ref69/cit69 doi: 10.1530/ERC-17-0120 – ident: ref29/cit29 doi: 10.2174/1568009615666150421110401 – ident: ref53/cit53 doi: 10.1158/1535-7163.MCT-09-0323 – ident: ref30/cit30 doi: 10.1038/nrm1245 – ident: ref68/cit68 doi: 10.1016/j.ctrv.2012.02.011 – ident: ref25/cit25 doi: 10.1038/ncb936 – ident: ref32/cit32 doi: 10.1158/1078-0432.CCR-11-1536 – ident: ref57/cit57 doi: 10.4049/jimmunol.177.2.885 – ident: ref59/cit59 doi: 10.1158/1078-0432.CCR-12-0589 – ident: ref10/cit10 doi: 10.1038/s41598-017-18210-3 – ident: ref44/cit44 doi: 10.1073/pnas.1610626113 – ident: ref4/cit4 doi: 10.1158/0008-5472.CAN-05-2796 – ident: ref9/cit9 doi: 10.18632/oncotarget.18970 – ident: ref27/cit27 doi: 10.1038/onc.2014.14 – ident: ref51/cit51 doi: 10.1158/0008-5472.CAN-10-1030 – volume: 20 start-page: 1414 issue: 6 year: 2015 ident: ref12/cit12 publication-title: J. BUON – ident: ref31/cit31 doi: 10.1016/j.critrevonc.2017.09.006 – ident: ref16/cit16 doi: 10.1016/j.blre.2016.02.001 – ident: ref49/cit49 doi: 10.1242/jcs.03145 – ident: ref34/cit34 doi: 10.1021/acschembio.7b00537 – ident: ref61/cit61 doi: 10.1083/jcb.152.4.669 – ident: ref1/cit1 doi: 10.1016/j.bbcan.2010.08.001 – ident: ref39/cit39 doi: 10.1016/j.pharmthera.2015.10.002 – ident: ref24/cit24 doi: 10.1016/S1097-2765(03)00392-7 – ident: ref52/cit52 doi: 10.1158/1535-7163.MCT-10-0299 – ident: ref6/cit6 doi: 10.1038/2496 – ident: ref64/cit64 doi: 10.1007/s00280-013-2305-8 – ident: ref66/cit66 doi: 10.1038/bjc.2012.450 – ident: ref43/cit43 doi: 10.1021/acschembio.6b00709 – volume: 5 start-page: 1 year: 2007 ident: WOS:000243845800001 article-title: Roles of aurora kinases in mitosis and tumorigenesis publication-title: MOLECULAR CANCER RESEARCH doi: 10.1158/1541-7786.MCR-06-0208 – volume: 3 start-page: 51 year: 2003 ident: WOS:000180630600008 article-title: AURORA-A amplification overrides the mitotic spindle assembly checkpoint, inducing resistance to Taxol publication-title: CANCER CELL – volume: 20 start-page: 1414 year: 2015 ident: WOS:000369355100004 article-title: Aurora A overexpression in breast cancer patients induces taxane resistance and results in worse prognosis publication-title: JOURNAL OF BUON – volume: 9 start-page: 2844 year: 2010 ident: WOS:000282724600019 article-title: Phase I Study of the Selective Aurora A Kinase Inhibitor MLN8054 in Patients with Advanced Solid Tumors: Safety, Pharmacokinetics, and Pharmacodynamics publication-title: MOLECULAR CANCER THERAPEUTICS doi: 10.1158/1535-7163.MCT-10-0299 – volume: 102 start-page: 96 year: 2013 ident: WOS:000322848500004 article-title: The association of taxane resistance genes with the clinical course of ovarian carcinoma publication-title: GENOMICS doi: 10.1016/j.ygeno.2013.03.005 – volume: 463 start-page: 501 year: 2010 ident: WOS:000273981100042 article-title: Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors publication-title: NATURE doi: 10.1038/nature08675 – volume: 72 start-page: 1255 year: 2013 ident: WOS:000327387000010 article-title: Preclinical pharmacokinetic/pharmacodynamic/efficacy relationships for alisertib, an investigational small-molecule inhibitor of Aurora A kinase publication-title: CANCER CHEMOTHERAPY AND PHARMACOLOGY doi: 10.1007/s00280-013-2305-8 – volume: 26 start-page: 414 year: 2014 ident: WOS:000341873800013 article-title: Drugging MYCN through an Allosteric Transition in Aurora Kinase A publication-title: CANCER CELL doi: 10.1016/j.ccr.2014.07.015 – volume: 25 start-page: 111 year: 2019 ident: WOS:000455027700029 article-title: Aurora kinase A drives the evolution of resistance to third-generation EGFR inhibitors in lung cancer publication-title: NATURE MEDICINE doi: 10.1038/s41591-018-0264-7 – volume: 119 start-page: 3664 year: 2006 ident: WOS:000240383500019 article-title: Validating Aurora B as an anti-cancer drug target publication-title: JOURNAL OF CELL SCIENCE doi: 10.1242/jcs.03145 – volume: 20 start-page: 624 year: 2009 ident: WOS:000270662700003 article-title: The regulatory function of umbilical cord blood CD4+CD25+ T cells stimulated with anti-CD3/anti-CD28 and exogenous interleukin (IL)-2 or IL-15 publication-title: PEDIATRIC ALLERGY AND IMMUNOLOGY doi: 10.1111/j.1399-3038.2008.00843.x – volume: 29 start-page: 536 year: 2016 ident: WOS:000373854600016 article-title: N-Myc Drives Neuroendocrine Prostate Cancer Initiated from Human Prostate Epithelial Cells publication-title: CANCER CELL doi: 10.1016/j.ccell.2016.03.001 – volume: 158 start-page: 617 year: 2002 ident: WOS:000177649900003 article-title: Human TPX2 is required for targeting Aurora-A kinase to the spindle publication-title: JOURNAL OF CELL BIOLOGY doi: 10.1083/jcb.200204155 – volume: 278 start-page: 51786 year: 2003 ident: WOS:000187206300114 article-title: Aurora-a kinase maintains the fidelity of early and late mitotic events in HeLa cells publication-title: JOURNAL OF BIOLOGICAL CHEMISTRY doi: 10.1074/jbc.M306275200 – volume: 124 start-page: 113 year: 2011 ident: WOS:000285242200013 article-title: Control of Aurora-A stability through interaction with TPX2 publication-title: JOURNAL OF CELL SCIENCE doi: 10.1242/jcs.075457 – volume: 8 start-page: 58 year: 2013 ident: WOS:000314008000007 article-title: Strategies for the Selective Regulation of Kinases with Allosteric Modulators: Exploiting Exclusive Structural Features publication-title: ACS CHEMICAL BIOLOGY doi: 10.1021/cb300663j – volume: 7 start-page: 12893 year: 2016 ident: WOS:000375679600086 article-title: MLN-8237: A dual inhibitor of aurora A and B in soft tissue sarcomas publication-title: ONCOTARGET – volume: 24 start-page: 1017 year: 2017 ident: WOS:000407918100012 article-title: Modulating Protein-Protein Interactions of the Mitotic Polo-like Kinases to Target Mutant KRAS publication-title: CELL CHEMICAL BIOLOGY doi: 10.1016/j.chembiol.2017.07.009 – volume: 113 start-page: 13726 year: 2016 ident: WOS:000388835700063 article-title: Structural basis of N-Myc binding by Aurora-A and its destabilization by kinase inhibitors publication-title: PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA doi: 10.1073/pnas.1610626113 – volume: 15 start-page: 375 year: 2015 ident: WOS:000357942000003 article-title: Structural Biology Insight for the Design of Sub-type Selective Aurora Kinase Inhibitors publication-title: CURRENT CANCER DRUG TARGETS – volume: 71 start-page: 675 year: 2011 ident: WOS:000286830300008 article-title: Phase I Assessment of New Mechanism-Based Pharmacodynamic Biomarkers for MLN8054, a Small-Molecule Inhibitor of Aurora A Kinase publication-title: CANCER RESEARCH doi: 10.1158/0008-5472.CAN-10-1030 – volume: 9 start-page: 248 year: 2019 ident: WOS:000458154500013 article-title: Aurora A Kinase Inhibition Is Synthetic Lethal with Loss of the RB1 Tumor Suppressor Gene publication-title: CANCER DISCOVERY doi: 10.1158/2159-8290.CD-18-0469 – volume: 6 start-page: ARTN 28528 year: 2016 ident: WOS:000378412200001 article-title: Allosteric modulation of AURKA kinase activity by a small-molecule inhibitor of its protein-protein interaction with TPX2 publication-title: SCIENTIFIC REPORTS doi: 10.1038/srep28528 – volume: 6 start-page: ARTN 88 year: 2016 ident: WOS:000374216300001 article-title: Non-centrosomal TPX2-Dependent Regulation of the Aurora A Kinase: Functional Implications for Healthy and Pathological Cell Division publication-title: FRONTIERS IN ONCOLOGY doi: 10.3389/fonc.2016.00088 – volume: 3 start-page: 721 year: 2012 ident: MEDLINE:23634259 article-title: Mitotic Stress and Chromosomal Instability in Cancer: The Case for TPX2. publication-title: Genes & cancer doi: 10.1177/1947601912473306 – volume: 38 start-page: 687 year: 2017 ident: WOS:000405902300003 article-title: Aurora A Kinase Is a Priority Pharmaceutical Target for the Treatment of Cancers publication-title: TRENDS IN PHARMACOLOGICAL SCIENCES doi: 10.1016/j.tips.2017.05.003 – volume: 24 start-page: T107 year: 2017 ident: WOS:000408115800013 article-title: Fighting tubulin-targeting anticancer drug toxicity and resistance publication-title: ENDOCRINE-RELATED CANCER doi: 10.1530/ERC-17-0120 – volume: 12 start-page: 2906 year: 2017 ident: WOS:000416204500026 article-title: Characterization of Three Druggable Hot-Spots in the Aurora-A/TPX2 Interaction Using Biochemical, Biophysical, and Fragment-Based Approaches publication-title: ACS CHEMICAL BIOLOGY doi: 10.1021/acschembio.7b00537 – volume: 8 start-page: 2046 year: 2009 ident: WOS:000268005700033 article-title: Determinants for the efficiency of anticancer drugs targeting either Aurora-A or Aurora-B kinases in human colon carcinoma cells publication-title: MOLECULAR CANCER THERAPEUTICS doi: 10.1158/1535-7163.MCT-09-0323 – volume: 177 start-page: 885 year: 2006 ident: WOS:000238926500015 article-title: Small interfering RNA-mediated knockdown of notch ligands in primary CD4+ T cells and dendritic cells enhances cytokine production publication-title: JOURNAL OF IMMUNOLOGY – volume: 156 start-page: 59 year: 2015 ident: WOS:000366952600006 article-title: Allosteric small-molecule kinase inhibitors publication-title: PHARMACOLOGY & THERAPEUTICS doi: 10.1016/j.pharmthera.2015.10.002 – volume: 34 start-page: 1242 year: 2014 ident: WOS:000343826600005 article-title: Harnessing Allostery: A Novel Approach to Drug Discovery publication-title: MEDICINAL RESEARCH REVIEWS doi: 10.1002/med.21317 – volume: 11 start-page: 3400 year: 2016 ident: WOS:000390179700024 article-title: Chemical Proteomics and Structural Biology Define EPHA2 Inhibition by Clinical Kinase Drugs publication-title: ACS CHEMICAL BIOLOGY doi: 10.1021/acschembio.6b00709 – volume: 12 start-page: 851 year: 2003 ident: WOS:000186196100010 article-title: Structural basis of Aurora-A activation by TPX2 at the mitotic spindle publication-title: MOLECULAR CELL – volume: 72 start-page: 171 year: 2016 ident: WOS:000373989900003 article-title: The Cambridge Structural Database publication-title: ACTA CRYSTALLOGRAPHICA SECTION B-STRUCTURAL SCIENCE CRYSTAL ENGINEERING AND MATERIALS doi: 10.1107/S2052520616003954 – volume: 5 start-page: 242 year: 2003 ident: WOS:000181322500018 article-title: A Ran signalling pathway mediated by the mitotic kinase Aurora A in spindle assembly publication-title: NATURE CELL BIOLOGY doi: 10.1038/ncb936 – volume: 13 start-page: 122 year: 2014 ident: WOS:000329815200013 article-title: Response to MLN8237 in Pancreatic Cancer Is Not Dependent on RalA Phosphorylation publication-title: MOLECULAR CANCER THERAPEUTICS doi: 10.1158/1535-7163.MCT-12-1232 – volume: 30 start-page: 419 year: 2017 ident: WOS:000404476100002 article-title: Development of a multipurpose scaffold for the display of peptide loops publication-title: PROTEIN ENGINEERING DESIGN & SELECTION doi: 10.1093/protein/gzx017 – volume: 3 start-page: 58 year: 2014 ident: MEDLINE:25068104 article-title: An exploratory phase 2 study of investigational Aurora A kinase inhibitor alisertib (MLN8237) in acute myelogenous leukemia and myelodysplastic syndromes. publication-title: Leukemia research reports doi: 10.1016/j.lrr.2014.06.003 – volume: 34 start-page: 537 year: 2015 ident: WOS:000348853500001 article-title: The aurora kinases in cell cycle and leukemia publication-title: ONCOGENE doi: 10.1038/onc.2014.14 – volume: 8 start-page: 32117 year: 2017 ident: WOS:000401003200118 article-title: Identification of small molecule inhibitors of the Aurora-A/TPX2 complex publication-title: ONCOTARGET doi: 10.18632/oncotarget.16738 – volume: 12 start-page: ARTN 1798 year: 2023 ident: WOS:001028537900001 article-title: SHIP1 Is Present but Strongly Downregulated in T-ALL, and after Restoration Suppresses Leukemia Growth in a T-ALL Xenotransplantation Mouse Model publication-title: CELLS doi: 10.3390/cells12131798 – volume: 1806 start-page: 230 year: 2010 ident: WOS:000285658400011 article-title: The Aurora-A/TPX2 complex: A novel oncogenic holoenzyme? publication-title: BIOCHIMICA ET BIOPHYSICA ACTA-REVIEWS ON CANCER doi: 10.1016/j.bbcan.2010.08.001 – volume: 38 start-page: 852 year: 2019 ident: WOS:000458006300007 article-title: TPX2/Aurora kinase A signaling as a potential therapeutic target in genomically unstable cancer cells publication-title: ONCOGENE doi: 10.1038/s41388-018-0470-2 – volume: 3 start-page: 404 year: 2004 ident: WOS:000222361700006 article-title: Determinants for Aurora-A activation and Aurora-B discrimination by TPX2 publication-title: CELL CYCLE – volume: 9 start-page: 991 year: 2003 ident: WOS:000181430400010 article-title: Overexpression of oncogenic STK15/BTAK/aurora A kinase in human pancreatic cancer publication-title: CLINICAL CANCER RESEARCH – volume: 66 start-page: 4996 year: 2006 ident: WOS:000237679900004 article-title: Targeting aurora kinases for the treatment of prostate cancer publication-title: CANCER RESEARCH doi: 10.1158/0008-5472.CAN-05-2796 – volume: 38 start-page: 890 year: 2012 ident: WOS:000309149400008 article-title: Taxane resistance in breast cancer: Mechanisms, predictive biomarkers and circumvention strategies publication-title: CANCER TREATMENT REVIEWS doi: 10.1016/j.ctrv.2012.02.011 – volume: 20 start-page: 189 year: 1998 ident: WOS:000076231300023 article-title: Tumour amplified kinase STK15/BTAK induces centrosome amplification, aneuploidy and transformation publication-title: NATURE GENETICS – volume: 25 start-page: 6831 year: 2019 ident: WOS:000471039200023 article-title: Construction of a Shape-Diverse Fragment Set: Design, Synthesis and Screen against Aurora-A Kinase publication-title: CHEMISTRY-A EUROPEAN JOURNAL doi: 10.1002/chem.201900815 – volume: 4 start-page: 927 year: 2004 ident: WOS:000225454300011 article-title: Aurora-kinase inhibitors as anticancer agents publication-title: NATURE REVIEWS CANCER doi: 10.1038/nrc1502 – volume: 7 start-page: ARTN 17978 year: 2017 ident: WOS:000418562100018 article-title: The expression of AURKA is androgen regulated in castration-resistant prostate cancer publication-title: SCIENTIFIC REPORTS doi: 10.1038/s41598-017-18210-3 – volume: 33 start-page: 224 year: 2015 ident: WOS:000351321400017 article-title: Nanoscale drug delivery for taxanes based on the mechanism of multidrug resistance of cancer publication-title: BIOTECHNOLOGY ADVANCES doi: 10.1016/j.biotechadv.2014.10.011 – volume: 30 start-page: 275 year: 2016 ident: WOS:000381172200004 article-title: Update on rational targeted therapy in AML publication-title: BLOOD REVIEWS doi: 10.1016/j.blre.2016.02.001 – volume: 120 start-page: 11 year: 2011 ident: WOS:000285824800003 article-title: Aurora-A overexpression and aneuploidy predict poor outcome in serous ovarian carcinoma publication-title: GYNECOLOGIC ONCOLOGY doi: 10.1016/j.ygyno.2010.09.003 – volume: 119 start-page: 59 year: 2017 ident: WOS:000415392100008 article-title: Critical risk-benefit assessment of the novel anti-cancer aurora a kinase inhibitor alisertib (MLN8237): A comprehensive review of the clinical data publication-title: CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY doi: 10.1016/j.critrevonc.2017.09.006 – volume: 182 start-page: 289 year: 2008 ident: WOS:000258274900009 article-title: Building a spindle of the correct length in human cells requires the interaction between TPX2 and Aurora A publication-title: JOURNAL OF CELL BIOLOGY – volume: 4 start-page: 842 year: 2003 ident: WOS:000186359800013 article-title: The cellular geography of aurora kinases publication-title: NATURE REVIEWS MOLECULAR CELL BIOLOGY doi: 10.1038/nrm1245 – volume: 107 start-page: 1692 year: 2012 ident: WOS:000310790900005 article-title: Paclitaxel and CYC3, an aurora kinase A inhibitor, synergise in pancreatic cancer cells but not bone marrow precursor cells publication-title: BRITISH JOURNAL OF CANCER doi: 10.1038/bjc.2012.450 – volume: 13 start-page: 1399 year: 2009 ident: WOS:000272787300003 article-title: Aurora-A kinase: a novel target both for cellular immunotherapy and molecular target therapy against human leukemia publication-title: EXPERT OPINION ON THERAPEUTIC TARGETS doi: 10.1517/14728220903307483 – volume: 18 start-page: 4764 year: 2012 ident: WOS:000309964500031 article-title: Phase I Pharmacokinetic/Pharmacodynamic Study of MLN8237, an Investigational, Oral, Selective Aurora A Kinase Inhibitor, in Patients with Advanced Solid Tumors publication-title: CLINICAL CANCER RESEARCH doi: 10.1158/1078-0432.CCR-12-0571 – volume: 5 start-page: ARTN 295 year: 2016 ident: WOS:000406742000001 article-title: Aurora-A Kinase as a Promising Therapeutic Target in Cancer publication-title: FRONTIERS IN ONCOLOGY doi: 10.3389/fonc.2015.00295 – volume: 68 start-page: 1291 year: 2011 ident: WOS:000297124400022 article-title: Efficacy and pharmacokinetic/pharmacodynamic evaluation of the Aurora kinase A inhibitor MLN8237 against preclinical models of pediatric cancer publication-title: CANCER CHEMOTHERAPY AND PHARMACOLOGY doi: 10.1007/s00280-011-1618-8 – volume: 13 start-page: 2237 year: 2014 ident: WOS:000340272100015 article-title: Therapeutic targeting of Polo-like kinase-1 and Aurora kinases in T-cell acute lymphoblastic leukemia publication-title: CELL CYCLE doi: 10.4161/cc.29267 – volume: 18 start-page: 4775 year: 2012 ident: WOS:000309964500032 article-title: Phase I Study of Aurora A Kinase Inhibitor MLN8237 in Advanced Solid Tumors: Safety, Pharmacokinetics, Pharmacodynamics, and Bioavailability of Two Oral Formulations publication-title: CLINICAL CANCER RESEARCH doi: 10.1158/1078-0432.CCR-12-0589 – volume: 8 start-page: 50376 year: 2017 ident: WOS:000406717200010 article-title: Aurora A kinase regulates non-homologous end-joining and poly(ADP-ribose) polymerase function in ovarian carcinoma cells publication-title: ONCOTARGET doi: 10.18632/oncotarget.18970 – volume: 152 start-page: 669 year: 2001 ident: WOS:000167114800004 article-title: Drosophila Aurora B kinase is required for histone H3 phosphorylation and condensin recruitment during chromosome condensation and to organize the central spindle during cytokinesis publication-title: JOURNAL OF CELL BIOLOGY – volume: 20 start-page: 721 year: 2013 ident: WOS:000317264800006 article-title: USP7 and Daxx regulate mitosis progression and taxane sensitivity by affecting stability of Aurora-A kinase publication-title: CELL DEATH AND DIFFERENTIATION doi: 10.1038/cdd.2012.169 – volume: 23 start-page: 74 year: 2022 ident: WOS:000694780200001 article-title: Cell cycle control in cancer publication-title: NATURE REVIEWS MOLECULAR CELL BIOLOGY doi: 10.1038/s41580-021-00404-3 – volume: 5 start-page: ARTN 285 year: 2015 ident: WOS:000366811700001 article-title: A Cell Biologist's Field Guide to Aurora Kinase Inhibitors publication-title: FRONTIERS IN ONCOLOGY doi: 10.3389/fonc.2015.00285 – volume: 5 start-page: ARTN 278 year: 2015 ident: WOS:000366811500001 article-title: Aurora Kinase inhibitors: Current Status and Outlook publication-title: FRONTIERS IN ONCOLOGY doi: 10.3389/fonc.2015.00278 – volume: 17 start-page: 7614 year: 2011 ident: WOS:000298410300013 article-title: Characterization of Alisertib (MLN8237), an Investigational Small-Molecule Inhibitor of Aurora A Kinase Using Novel In Vivo Pharmacodynamic Assays publication-title: CLINICAL CANCER RESEARCH doi: 10.1158/1078-0432.CCR-11-1536 |
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| Snippet | Aurora A kinase, a cell division regulator, is frequently overexpressed in various cancers, provoking genome instability and resistance to antimitotic... Aurora A kinase, a cell division regulator, is frequently overexpressed in various cancers, provoking genome instability and resistance to antimitotic... |
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| SubjectTerms | Animals Antimitotic Agents - chemistry Antimitotic Agents - pharmacology Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Aurora Kinase A - antagonists & inhibitors Aurora Kinase A - metabolism Cell Cycle Proteins - antagonists & inhibitors Cell Cycle Proteins - metabolism Cell Line, Tumor Chemistry, Medicinal Humans Life Sciences & Biomedicine Mice Mice, Nude Microtubule-Associated Proteins - metabolism Nuclear Proteins - antagonists & inhibitors Nuclear Proteins - metabolism Paclitaxel - pharmacology Pharmacology & Pharmacy Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Science & Technology Structure-Activity Relationship Xenograft Model Antitumor Assays |
| Title | Selective Aurora A-TPX2 Interaction Inhibitors Have In Vivo Efficacy as Targeted Antimitotic Agents |
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