1mp8 › Citations

Structures of the cancer-related Aurora-A, FAK, and EphA2 protein kinases from nanovolume crystallography.

Nowakowski J, Cronin CN, McRee DE, Knuth MW, Nelson CG, Pavletich NP, Rogers J, Sang BC, Scheibe DN, Swanson RV, Thompson DA
Structure 10 1659-67 (2002)
Related entries: 1mq4, 1mqb

Cited: 111 times
EuropePMC logo PMID: 12467573

Abstract

Protein kinases are important drug targets in human cancers, inflammation, and metabolic diseases. This report presents the structures of kinase domains for three cancer-associated protein kinases: ephrin receptor A2 (EphA2), focal adhesion kinase (FAK), and Aurora-A. The expression profiles of EphA2, FAK, and Aurora-A in carcinomas suggest that inhibitors of these kinases may have inherent potential as therapeutic agents. The structures were determined from crystals grown in nanovolume droplets, which produced high-resolution diffraction data at 1.7, 1.9, and 2.3 A for FAK, Aurora-A, and EphA2, respectively. The FAK and Aurora-A structures are the first determined within two unique subfamilies of human kinases, and all three structures provide new insights into kinase regulation and the design of selective inhibitors.

Articles - 1mp8 mentioned but not cited (15)

  1. Structural basis for the autoinhibition of focal adhesion kinase. Lietha D, Cai X, Ceccarelli DF, Li Y, Schaller MD, Eck MJ. Cell 129 1177-1187 (2007)
  2. Sequence and structural analyses of nuclear export signals in the NESdb database. Xu D, Farmer A, Collett G, Grishin NV, Chook YM. Mol Biol Cell 23 3677-3693 (2012)
  3. Structural characterization of proline-rich tyrosine kinase 2 (PYK2) reveals a unique (DFG-out) conformation and enables inhibitor design. Han S, Mistry A, Chang JS, Cunningham D, Griffor M, Bonnette PC, Wang H, Chrunyk BA, Aspnes GE, Walker DP, Brosius AD, Buckbinder L. J. Biol. Chem. 284 13193-13201 (2009)
  4. Structural protein-ligand interaction fingerprints (SPLIF) for structure-based virtual screening: method and benchmark study. Da C, Kireev D. J Chem Inf Model 54 2555-2561 (2014)
  5. Crystal structures of the FAK kinase in complex with TAE226 and related bis-anilino pyrimidine inhibitors reveal a helical DFG conformation. Lietha D, Eck MJ. PLoS ONE 3 e3800 (2008)
  6. Structure of a pseudokinase-domain switch that controls oncogenic activation of Jak kinases. Toms AV, Deshpande A, McNally R, Jeong Y, Rogers JM, Kim CU, Gruner SM, Ficarro SB, Marto JA, Sattler M, Griffin JD, Eck MJ. Nat. Struct. Mol. Biol. 20 1221-1223 (2013)
  7. Structural basis of Focal Adhesion Kinase activation on lipid membranes. Acebrón I, Righetto RD, Schoenherr C, de Buhr S, Redondo P, Culley J, Rodríguez CF, Daday C, Biyani N, Llorca O, Byron A, Chami M, Gräter F, Boskovic J, Frame MC, Stahlberg H, Lietha D. EMBO J 39 e104743 (2020)
  8. Analysis of the calcium-dependent regulation of proline-rich tyrosine kinase 2 by gonadotropin-releasing hormone. Xie J, Allen KH, Marguet A, Berghorn KA, Bliss SP, Navratil AM, Guan JL, Roberson MS. Mol. Endocrinol. 22 2322-2335 (2008)
  9. Disulfide conformation and design at helix N-termini. Indu S, Kumar ST, Thakurela S, Gupta M, Bhaskara RM, Ramakrishnan C, Varadarajan R. Proteins 78 1228-1242 (2010)
  10. Relating the shape of protein binding sites to binding affinity profiles: is there an association? Simon Z, Vigh-Smeller M, Peragovics A, Csukly G, Zahoránszky-Kohalmi G, Rauscher AA, Jelinek B, Hári P, Bitter I, Málnási-Csizmadia A, Czobor P. BMC Struct Biol 10 32 (2010)
  11. Mapping RNAPII CTD Phosphorylation Reveals That the Identity and Modification of Seventh Heptad Residues Direct Tyr1 Phosphorylation. Burkholder NT, Sipe SN, Escobar EE, Venkatramani M, Irani S, Yang W, Wu H, Matthews WM, Brodbelt JS, Zhang Y. ACS Chem Biol 14 2264-2275 (2019)
  12. An in silico high-throughput screen identifies potential selective inhibitors for the non-receptor tyrosine kinase Pyk2. Meirson T, Samson AO, Gil-Henn H. Drug Des Devel Ther 11 1535-1557 (2017)
  13. Artocarpin Targets Focal Adhesion Kinase-Dependent Epithelial to Mesenchymal Transition and Suppresses Migratory-Associated Integrins in Lung Cancer Cells. Nonpanya N, Sanookpan K, Sriratanasak N, Vinayanuwattikun C, Wichadakul D, Sritularak B, Chanvorachote P. Pharmaceutics 13 554 (2021)
  14. A Triazaspirane Derivative Inhibits Migration and Invasion in PC3 Prostate Cancer Cells. Vasconcelos-Ulloa JJ, García-González V, Valdez-Salas B, Vázquez-Jiménez JG, Rivero-Espejel I, Díaz-Molina R, Galindo-Hernández O. Molecules 28 4524 (2023)
  15. Dissecting the molecular mechanism of cepharanthine against COVID-19, based on a network pharmacology strategy combined with RNA-sequencing analysis, molecular docking, and molecular dynamics simulation. Liu J, Sun T, Liu S, Liu J, Fang S, Tan S, Zeng Y, Zhang B, Li W. Comput Biol Med 151 106298 (2022)


Reviews citing this publication (25)

  1. Focal adhesion kinase: in command and control of cell motility. Mitra SK, Hanson DA, Schlaepfer DD. Nat. Rev. Mol. Cell Biol. 6 56-68 (2005)
  2. The cellular geography of aurora kinases. Carmena M, Earnshaw WC. Nat. Rev. Mol. Cell Biol. 4 842-854 (2003)
  3. Regulation of protein kinases; controlling activity through activation segment conformation. Nolen B, Taylor S, Ghosh G. Mol. Cell 15 661-675 (2004)
  4. Targeting polo-like kinase 1 for cancer therapy. Strebhardt K, Ullrich A. Nat. Rev. Cancer 6 321-330 (2006)
  5. Multiple connections link FAK to cell motility and invasion. Schlaepfer DD, Mitra SK. Curr. Opin. Genet. Dev. 14 92-101 (2004)
  6. Aurora A kinase (AURKA) in normal and pathological cell division. Nikonova AS, Astsaturov I, Serebriiskii IG, Dunbrack RL, Golemis EA. Cell. Mol. Life Sci. 70 661-687 (2013)
  7. Eph receptor-ephrin bidirectional signals that target Ras and Rho proteins. Noren NK, Pasquale EB. Cell. Signal. 16 655-666 (2004)
  8. Targeting FAK in human cancer: from finding to first clinical trials. Golubovskaya VM. Front Biosci (Landmark Ed) 19 687-706 (2014)
  9. Aurora A and B kinases as targets for cancer: will they be selective for tumors? Matthews N, Visintin C, Hartzoulakis B, Jarvis A, Selwood DL. Expert Rev Anticancer Ther 6 109-120 (2006)
  10. Focal adhesion kinase and p53 signal transduction pathways in cancer. Golubovskaya VM, Cance W. Front Biosci (Landmark Ed) 15 901-912 (2010)
  11. How focal adhesion kinase achieves regulation by linking ligand binding, localization and action. Arold ST. Curr. Opin. Struct. Biol. 21 808-813 (2011)
  12. Focal adhesion kinase -- the basis of local hypertrophic signaling domains. Franchini KG. J. Mol. Cell. Cardiol. 52 485-492 (2012)
  13. FAK and paxillin, two potential targets in pancreatic cancer. Kanteti R, Batra SK, Lennon FE, Salgia R. Oncotarget 7 31586-31601 (2016)
  14. The target discovery process. Egner U, Krätzschmar J, Kreft B, Pohlenz HD, Schneider M. Chembiochem 6 468-479 (2005)
  15. The role of Eph receptors in lens function and disease. Son AI, Park JE, Zhou R. Sci China Life Sci 55 434-443 (2012)
  16. Tie2 and Eph receptor tyrosine kinase activation and signaling. Barton WA, Dalton AC, Seegar TC, Himanen JP, Nikolov DB. Cold Spring Harb Perspect Biol 6 (2014)
  17. FAK Structure and Regulation by Membrane Interactions and Force in Focal Adhesions. Tapial Martínez P, López Navajas P, Lietha D. Biomolecules 10 (2020)
  18. Switching Aurora-A kinase on and off at an allosteric site. Bayliss R, Burgess SG, McIntyre PJ. FEBS J. 284 2947-2954 (2017)
  19. Adaptability in protein structures: structural dynamics and implications in ligand design. Maity A, Majumdar S, Priya P, De P, Saha S, Ghosh Dastidar S. J. Biomol. Struct. Dyn. 33 298-321 (2015)
  20. The multifaceted allosteric regulation of Aurora kinase A. Levinson NM. Biochem. J. 475 2025-2042 (2018)
  21. Looking lively: emerging principles of pseudokinase signaling. Sheetz JB, Lemmon MA. Trends Biochem Sci 47 875-891 (2022)
  22. Mechanosensing dysregulation in the fibroblast: A hallmark of the aging heart. Angelini A, Trial J, Ortiz-Urbina J, Cieslik KA. Ageing Res Rev 63 101150 (2020)
  23. Mitotic protein kinase-driven crosstalk of machineries for mitosis and metastasis. Kim CH, Kim DE, Kim DH, Min GH, Park JW, Kim YB, Sung CK, Yim H. Exp Mol Med 54 414-425 (2022)
  24. Recent advances in synthetic strategies and SAR of thiazolidin-4-one containing molecules in cancer therapeutics. Sharma A, Sharma D, Saini N, Sharma SV, Thakur VK, Goyal RK, Sharma PC. Cancer Metastasis Rev (2023)
  25. The Development of FAK Inhibitors: A Five-Year Update. Spallarossa A, Tasso B, Russo E, Villa C, Brullo C. Int J Mol Sci 23 6381 (2022)

Articles citing this publication (71)

  1. Structural basis of Aurora-A activation by TPX2 at the mitotic spindle. Bayliss R, Sardon T, Vernos I, Conti E. Mol. Cell 12 851-862 (2003)
  2. Mechanism of Aurora B activation by INCENP and inhibition by hesperadin. Sessa F, Mapelli M, Ciferri C, Tarricone C, Areces LB, Schneider TR, Stukenberg PT, Musacchio A. Mol. Cell 18 379-391 (2005)
  3. Drosophila Aurora-A kinase inhibits neuroblast self-renewal by regulating aPKC/Numb cortical polarity and spindle orientation. Lee CY, Andersen RO, Cabernard C, Manning L, Tran KD, Lanskey MJ, Bashirullah A, Doe CQ. Genes Dev. 20 3464-3474 (2006)
  4. Regulation of focal adhesion kinase by its amino-terminal domain through an autoinhibitory interaction. Cooper LA, Shen TL, Guan JL. Mol. Cell. Biol. 23 8030-8041 (2003)
  5. Crystal structure of the ALK (anaplastic lymphoma kinase) catalytic domain. Lee CC, Jia Y, Li N, Sun X, Ng K, Ambing E, Gao MY, Hua S, Chen C, Kim S, Michellys PY, Lesley SA, Harris JL, Spraggon G. Biochem. J. 430 425-437 (2010)
  6. C-terminal truncation and Parkinson's disease-associated mutations down-regulate the protein serine/threonine kinase activity of PTEN-induced kinase-1. Sim CH, Lio DS, Mok SS, Masters CL, Hill AF, Culvenor JG, Cheng HC. Hum. Mol. Genet. 15 3251-3262 (2006)
  7. Direct association with inner centromere protein (INCENP) activates the novel chromosomal passenger protein, Aurora-C. Li X, Sakashita G, Matsuzaki H, Sugimoto K, Kimura K, Hanaoka F, Taniguchi H, Furukawa K, Urano T. J. Biol. Chem. 279 47201-47211 (2004)
  8. EPHA2 is associated with age-related cortical cataract in mice and humans. Jun G, Guo H, Klein BE, Klein R, Wang JJ, Mitchell P, Miao H, Lee KE, Joshi T, Buck M, Chugha P, Bardenstein D, Klein AP, Bailey-Wilson JE, Gong X, Spector TD, Andrew T, Hammond CJ, Elston RC, Iyengar SK, Wang B. PLoS Genet. 5 e1000584 (2009)
  9. Crystal structure of the FERM domain of focal adhesion kinase. Ceccarelli DF, Song HK, Poy F, Schaller MD, Eck MJ. J Biol Chem 281 252-259 (2006)
  10. Phospho-regulation of human protein kinase Aurora-A: analysis using anti-phospho-Thr288 monoclonal antibodies. Ohashi S, Sakashita G, Ban R, Nagasawa M, Matsuzaki H, Murata Y, Taniguchi H, Shima H, Furukawa K, Urano T. Oncogene 25 7691-7702 (2006)
  11. SAR and inhibitor complex structure determination of a novel class of potent and specific Aurora kinase inhibitors. Heron NM, Anderson M, Blowers DP, Breed J, Eden JM, Green S, Hill GB, Johnson T, Jung FH, McMiken HH, Mortlock AA, Pannifer AD, Pauptit RA, Pink J, Roberts NJ, Rowsell S. Bioorg. Med. Chem. Lett. 16 1320-1323 (2006)
  12. Structures of rhodopsin kinase in different ligand states reveal key elements involved in G protein-coupled receptor kinase activation. Singh P, Wang B, Maeda T, Palczewski K, Tesmer JJ. J. Biol. Chem. 283 14053-14062 (2008)
  13. Crystal structure of the catalytic domain of human atypical protein kinase C-iota reveals interaction mode of phosphorylation site in turn motif. Messerschmidt A, Macieira S, Velarde M, Bädeker M, Benda C, Jestel A, Brandstetter H, Neuefeind T, Blaesse M. J. Mol. Biol. 352 918-931 (2005)
  14. A change in conformational dynamics underlies the activation of Eph receptor tyrosine kinases. Wiesner S, Wybenga-Groot LE, Warner N, Lin H, Pawson T, Forman-Kay JD, Sicheri F. EMBO J. 25 4686-4696 (2006)
  15. Structure and inhibition of the human cell cycle checkpoint kinase, Wee1A kinase: an atypical tyrosine kinase with a key role in CDK1 regulation. Squire CJ, Dickson JM, Ivanovic I, Baker EN. Structure 13 541-550 (2005)
  16. Autoregulation by the juxtamembrane region of the human ephrin receptor tyrosine kinase A3 (EphA3). Davis TL, Walker JR, Loppnau P, Butler-Cole C, Allali-Hassani A, Dhe-Paganon S. Structure 16 873-884 (2008)
  17. Modulation of kinase-inhibitor interactions by auxiliary protein binding: crystallography studies on Aurora A interactions with VX-680 and with TPX2. Zhao B, Smallwood A, Yang J, Koretke K, Nurse K, Calamari A, Kirkpatrick RB, Lai Z. Protein Sci. 17 1791-1797 (2008)
  18. Crystal structures of active SRC kinase domain complexes. Breitenlechner CB, Kairies NA, Honold K, Scheiblich S, Koll H, Greiter E, Koch S, Schäfer W, Huber R, Engh RA. J. Mol. Biol. 353 222-231 (2005)
  19. Molecular distinctions between Aurora A and B: a single residue change transforms Aurora A into correctly localized and functional Aurora B. Hans F, Skoufias DA, Dimitrov S, Margolis RL. Mol. Biol. Cell 20 3491-3502 (2009)
  20. Organization and post-transcriptional processing of focal adhesion kinase gene. Corsi JM, Rouer E, Girault JA, Enslen H. BMC Genomics 7 198 (2006)
  21. A pentacyclic triterpene natural product, ursolic acid and its prodrug US597 inhibit targets within cell adhesion pathway and prevent cancer metastasis. Xiang L, Chi T, Tang Q, Yang X, Ou M, Chen X, Yu X, Chen J, Ho RJ, Shao J, Jia L. Oncotarget 6 9295-9312 (2015)
  22. Crystal structure of human aurora B in complex with INCENP and VX-680. Elkins JM, Santaguida S, Musacchio A, Knapp S. J. Med. Chem. 55 7841-7848 (2012)
  23. Discovery of an Aurora kinase inhibitor through site-specific dynamic combinatorial chemistry. Cancilla MT, He MM, Viswanathan N, Simmons RL, Taylor M, Fung AD, Cao K, Erlanson DA. Bioorg. Med. Chem. Lett. 18 3978-3981 (2008)
  24. Automated sample mounting and alignment system for biological crystallography at a synchrotron source. Snell G, Cork C, Nordmeyer R, Cornell E, Meigs G, Yegian D, Jaklevic J, Jin J, Stevens RC, Earnest T. Structure 12 537-545 (2004)
  25. Crystal structures of the N-terminal kinase domain of human RSK1 bound to three different ligands: Implications for the design of RSK1 specific inhibitors. Ikuta M, Kornienko M, Byrne N, Reid JC, Mizuarai S, Kotani H, Munshi SK. Protein Sci. 16 2626-2635 (2007)
  26. Giardia lamblia aurora kinase: a regulator of mitosis in a binucleate parasite. Davids BJ, Williams S, Lauwaet T, Palanca T, Gillin FD. Int. J. Parasitol. 38 353-369 (2008)
  27. A Cell Biologist's Field Guide to Aurora Kinase Inhibitors. de Groot CO, Hsia JE, Anzola JV, Motamedi A, Yoon M, Wong YL, Jenkins D, Lee HJ, Martinez MB, Davis RL, Gahman TC, Desai A, Shiau AK. Front Oncol 5 285 (2015)
  28. A water-mediated allosteric network governs activation of Aurora kinase A. Cyphers S, Ruff EF, Behr JM, Chodera JD, Levinson NM. Nat. Chem. Biol. 13 402-408 (2017)
  29. Production of selenomethionyl-derivatized proteins in baculovirus-infected insect cells. Cronin CN, Lim KB, Rogers J. Protein Sci. 16 2023-2029 (2007)
  30. Structural model for p75(NTR)-TrkA intracellular domain interaction: a combined FRET and bioinformatics study. Iacaruso MF, Galli S, Martí M, Villalta JI, Estrin DA, Jares-Erijman EA, Pietrasanta LI. J. Mol. Biol. 414 681-698 (2011)
  31. Structural basis for the inhibition of Aurora A kinase by a novel class of high affinity disubstituted pyrimidine inhibitors. Tari LW, Hoffman ID, Bensen DC, Hunter MJ, Nix J, Nelson KJ, McRee DE, Swanson RV. Bioorg. Med. Chem. Lett. 17 688-691 (2007)
  32. Two TPX2-dependent switches control the activity of Aurora A. Xu X, Wang X, Xiao Z, Li Y, Wang Y. PLoS ONE 6 e16757 (2011)
  33. Crystal structure of the EphA4 protein tyrosine kinase domain in the apo- and dasatinib-bound state. Farenc C, Celie PH, Tensen CP, de Esch IJ, Siegal G. FEBS Lett. 585 3593-3599 (2011)
  34. Identification of a Novel and Selective Series of Itk Inhibitors via a Template-Hopping Strategy. Alder CM, Ambler M, Campbell AJ, Champigny AC, Deakin AM, Harling JD, Harris CA, Longstaff T, Lynn S, Maxwell AC, Mooney CJ, Scullion C, Singh OM, Smith IE, Somers DO, Tame CJ, Wayne G, Wilson C, Woolven JM. ACS Med Chem Lett 4 948-952 (2013)
  35. Dynamics of protein kinases: insights from nuclear magnetic resonance. Xiao Y, Liddle JC, Pardi A, Ahn NG. Acc. Chem. Res. 48 1106-1114 (2015)
  36. SERS and MD simulation studies of a kinase inhibitor demonstrate the emergence of a potential drug discovery tool. Karthigeyan D, Siddhanta S, Kishore AH, Perumal SS, Ågren H, Sudevan S, Bhat AV, Balasubramanyam K, Subbegowda RK, Kundu TK, Narayana C. Proc. Natl. Acad. Sci. U.S.A. 111 10416-10421 (2014)
  37. Small-molecule inhibition of Aurora kinases triggers spindle checkpoint-independent apoptosis in cancer cells. Sun L, Li D, Dong X, Yu H, Dong JT, Zhang C, Lu X, Zhou J. Biochem. Pharmacol. 75 1027-1034 (2008)
  38. A FRET biosensor reveals spatiotemporal activation and functions of aurora kinase A in living cells. Bertolin G, Sizaire F, Herbomel G, Reboutier D, Prigent C, Tramier M. Nat Commun 7 12674 (2016)
  39. Discovery and characterization of novel allosteric FAK inhibitors. Iwatani M, Iwata H, Okabe A, Skene RJ, Tomita N, Hayashi Y, Aramaki Y, Hosfield DJ, Hori A, Baba A, Miki H. Eur J Med Chem 61 49-60 (2013)
  40. Discovery of a dual-targeting organometallic ruthenium complex with high activity inducing early stage apoptosis of cancer cells. Du J, Zhang E, Zhao Y, Zheng W, Zhang Y, Lin Y, Wang Z, Luo Q, Wu K, Wang F. Metallomics 7 1573-1583 (2015)
  41. Mouse Aurora A: expression in Escherichia coli and purification. Elling RA, Tangonan BT, Penny DM, Smith JT, Vincent DE, Hansen SK, O'Brien T, Romanowski MJ. Protein Expr. Purif. 54 139-146 (2007)
  42. Structure-based design of nitrogen-linked macrocyclic kinase inhibitors leading to the clinical candidate SB1317/TG02, a potent inhibitor of cyclin dependant kinases (CDKs), Janus kinase 2 (JAK2), and Fms-like tyrosine kinase-3 (FLT3). Poulsen A, William A, Blanchard S, Nagaraj H, Williams M, Wang H, Lee A, Sun E, Teo EL, Tan E, Goh KC, Dymock B. J Mol Model 19 119-130 (2013)
  43. Aurora kinase targeted therapeutics in oncology: past, present and future. Mahadevan D, Beeck S. Expert Opin Drug Discov 2 1011-1026 (2007)
  44. Computational investigation of cancer-associated molecular mechanism in Aurora A (S155R) mutation. Kumar A, Rajendran V, Sethumadhavan R, Purohit R. Cell Biochem. Biophys. 66 787-796 (2013)
  45. Structural studies of B-type Aurora kinase inhibitors using computational methods. Neaz M, Muddassar M, Pasha F, Cho SJ. Acta Pharmacol. Sin. 31 244-258 (2010)
  46. Structure-based design of Aurora A & B inhibitors. Poulsen A, William A, Lee A, Blanchard S, Teo E, Deng W, Tu N, Tan E, Sun E, Goh KL, Ong WC, Ng CP, Goh KC, Bonday Z. J. Comput. Aided Mol. Des. 22 897-906 (2008)
  47. Computational and Experimental Characterization of Patient Derived Mutations Reveal an Unusual Mode of Regulatory Spine Assembly and Drug Sensitivity in EGFR Kinase. Ruan Z, Katiyar S, Kannan N. Biochemistry 56 22-32 (2017)
  48. The noni anthraquinone damnacanthal is a multi-kinase inhibitor with potent anti-angiogenic effects. García-Vilas JA, Pino-Ángeles A, Martínez-Poveda B, Quesada AR, Medina MÁ. Cancer Lett. 385 1-11 (2017)
  49. Comparison of LanthaScreen Eu kinase binding assay and surface plasmon resonance method in elucidating the binding kinetics of focal adhesion kinase inhibitors. Mason JL, Spais C, Husten J, Prouty E, Albom MS, Meyer SL, Ator MA, Angeles TS. Assay Drug Dev Technol 10 468-475 (2012)
  50. Dynamics of human protein kinase Aurora A linked to drug selectivity. Pitsawong W, Buosi V, Otten R, Agafonov RV, Zorba A, Kern N, Kutter S, Kern G, Pádua RA, Meniche X, Kern D. Elife 7 (2018)
  51. Interactions of the EphA2 Kinase Domain with PIPs in Membranes: Implications for Receptor Function. Chavent M, Karia D, Kalli AC, Domański J, Duncan AL, Hedger G, Stansfeld PJ, Seiradake E, Jones EY, Sansom MSP. Structure 26 1025-1034.e2 (2018)
  52. RIPK1-dependent cell death: a novel target of the Aurora kinase inhibitor Tozasertib (VX-680). Martens S, Goossens V, Devisscher L, Hofmans S, Claeys P, Vuylsteke M, Takahashi N, Augustyns K, Vandenabeele P. Cell Death Dis 9 211 (2018)
  53. Regulation of Focal Adhesion Kinase through a Direct Interaction with an Endogenous Inhibitor. Zak TJ, Koshman YE, Samarel AM, Robia SL. Biochemistry 56 4722-4731 (2017)
  54. Structure activity relationships of quinoxalin-2-one derivatives as platelet-derived growth factor-beta receptor (PDGFbeta R) inhibitors, derived from molecular modeling. Mori Y, Hirokawa T, Aoki K, Satomi H, Takeda S, Aburada M, Miyamoto K. Chem. Pharm. Bull. 56 682-687 (2008)
  55. Structures of an Eph receptor tyrosine kinase and its potential activation mechanism. Wei Q, Liu J, Wang N, Zhang X, Jin J, Chin-Sang I, Zheng J, Jia Z. Acta Crystallogr. D Biol. Crystallogr. 70 3135-3143 (2014)
  56. 4-Substituted quinazoline derivatives as novel EphA2 receptor tyrosine kinase inhibitors. Lim CJ, Oh KS, Ha JD, Lee JH, Seo HW, Chae CH, Kim DG, Lee MJ, Lee BH. Bioorg. Med. Chem. Lett. 24 4080-4083 (2014)
  57. Synthesis of novel 1,2,4-triazine scaffold as FAK inhibitors with antitumor activity. Dao P, Lietha D, Etheve-Quelquejeu M, Garbay C, Chen H. Bioorg. Med. Chem. Lett. 27 1727-1730 (2017)
  58. Towards simple kinetic models of functional dynamics for a kinase subfamily. Sultan MM, Kiss G, Pande VS. Nat Chem 10 903-909 (2018)
  59. Using LongSAGE to Detect Biomarkers of Cervical Cancer Potentially Amenable to Optical Contrast Agent Labelling. Kneller JM, Ehlen T, Matisic JP, Miller D, Van Niekerk D, Lam WL, Marra M, Richards-Kortum R, Follen M, Macaulay C, Jones SJ. Biomark Insights 2 447-461 (2007)
  60. A Dual Non-ATP Analogue Inhibitor of Aurora Kinases A and B, Derived from Resorcinol with a Mixed Mode of Inhibition. Karthigeyan D, Surabhi S, Mizar P, Soumik S, Banerjee A, Sinha SH, Dasgupta D, Narayana C, Kundu TK. Chem Biol Drug Des 87 958-967 (2016)
  61. Expression and Purification of EPHA2 Tyrosine Kinase Domain for Crystallographic and NMR Studies. Gande SL, Saxena K, Sreeramulu S, Linhard V, Kudlinzki D, Heinzlmeir S, Reichert AJ, Skerra A, Kuster B, Schwalbe H. Chembiochem 17 2257-2263 (2016)
  62. Platinum(II) Terpyridine Anticancer Complexes Possessing Multiple Mode of DNA Interaction and EGFR Inhibiting Activity. Li C, Xu F, Zhao Y, Zheng W, Zeng W, Luo Q, Wang Z, Wu K, Du J, Wang F. Front Chem 8 210 (2020)
  63. SOCS2 Binds to and Regulates EphA2 through Multiple Mechanisms. Pilling C, Cooper JA. Sci Rep 7 10838 (2017)
  64. A computational and laboratory approach for the investigation of interactions of peptide conjugated natural terpenes with EpHA2 receptor. Goncalves BG, Banerjee IA. J Mol Model 29 204 (2023)
  65. Aurora kinase protein family in Trypanosoma cruzi: Novel role of an AUK-B homologue in kinetoplast replication. Fassolari M, Alonso GD. PLoS Negl Trop Dis 13 e0007256 (2019)
  66. Exploring the mechanistic insights of Cas scaffolding protein family member 4 with protein tyrosine kinase 2 in Alzheimer's disease by evaluating protein interactions through molecular docking and dynamic simulations. Hassan M, Shahzadi S, Alashwal H, Zaki N, Seo SY, Moustafa AA, Moustafa AA. Neurol. Sci. 39 1361-1374 (2018)
  67. Identification of FAK substrate peptides via colorimetric screening of a one-bead one-peptide combinatorial library. Witucki LA, Borowicz LS, Pedley AM, Curtis-Fisk J, Kuszpit EG. J. Pept. Sci. 21 302-311 (2015)
  68. Molecular Docking, Molecular Dynamics Simulations, and Free Energy Calculation Insights into the Binding Mechanism between VS-4718 and Focal Adhesion Kinase. Shi M, Chen T, Wei S, Zhao C, Zhang X, Li X, Tang X, Liu Y, Yang Z, Chen L. ACS Omega 7 32442-32456 (2022)
  69. New type of interaction between the SARAH domain of the tumour suppressor RASSF1A and its mitotic kinase Aurora A. Szimler T, Gráczer É, Györffy D, Végh B, Szilágyi A, Hajdú I, Závodszky P, Vas M. Sci Rep 9 5550 (2019)
  70. Oxethazaine inhibits esophageal squamous cell carcinoma proliferation and metastasis by targeting aurora kinase A. Bao Z, Li A, Lu X, Wang Z, Yu Y, Wu W, Zhao L, Li B, Wu X, Laster KV, Zhang C, Jiang Y, Dong Z, Liu K. Cell Death Dis 13 189 (2022)
  71. Phosphorylation, Mg-ADP, and Inhibitors Differentially Shape the Conformational Dynamics of the A-Loop of Aurora-A. Musavizadeh Z, Grottesi A, Guarguaglini G, Paiardini A. Biomolecules 11 567 (2021)


Quick links