Specificity and mechanism of action of EHT 1864, a novel small molecule inhibitor of Rac family small GTPases
Open accessAbstract
There is now considerable experimental evidence that aberrant activation of Rho family small GTPases promotes the uncontrolled proliferation, invasion, and metastatic properties of human cancer cells. Therefore, there is considerable interest in the development of small molecule inhibitors of Rho GTPase function. However, to date, most efforts have focused on inhibitors that indirectly block Rho GTPase function, by targeting either enzymes involved in post-translational processing or downstream protein kinase effectors. We recently determined that the EHT 1864 small molecule can inhibit Rac function in vivo. In this study, we evaluated the biological and biochemical specificities and biochemical mechanism of action of EHT 1864. We determined that EHT 1864 specifically inhibited Rac1-dependent platelet-derived growth factor-induced lamellipodia formation. Furthermore, our biochemical analyses with recombinant Rac proteins found that EHT 1864 possesses high affinity binding to Rac1, as well as the related Rac1b, Rac2, and Rac3 isoforms, and this association promoted the loss of bound nucleotide, inhibiting both guanine nucleotide association and Tiam1 Rac guanine nucleotide exchange factor-stimulated exchange factor activity in vitro. EHT 1864 therefore places Rac in an inert and inactive state, preventing its engagement with downstream effectors. Finally, we evaluated the ability of EHT 1864 to block Rac-dependent growth transformation, and we determined that EHT 1864 potently blocked transformation caused by constitutively activated Rac1, as well as Rac-dependent transformation caused by Tiam1 or Ras. Taken together, our results suggest that EHT 1864 selectively inhibits Rac downstream signaling and transformation by a novel mechanism involving guanine nucleotide displacement.
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Cites
Ridley, A. J., & Hall, A. (1992) · Cell · doi:10.1016/0092-8674(92)90163-7 · Cited by 4,469 · see citing works
The small GTP-binding protein rac regulates growth factor-induced membrane ruffling
Ridley, A. J., Paterson, H. F., Johnston, C. L., Diekmann, D., & Hall, A. (1992) · Cell · doi:10.1016/0092-8674(92)90164-8 · Cited by 3,651 · see citing works
Hansen, M., Nielsen, S. E., & Berg, K. (1989) · Journal of Immunological Methods · doi:10.1016/0022-1759(89)90397-9 · Cited by 3,526 · see citing works
RHO GTPASES: Biochemistry and Biology
Jaffe, A. B., & Hall, A. (2005) · Annual Review of Cell and Developmental Biology · doi:10.1146/annurev.cellbio.21.020604.150721 · Cited by 3,009 · see citing works
Rho GTPases and their effector proteins
Bishop, A. L., & Hall, A. (2000) · Biochemical Journal · doi:10.1042/bj3480241 · Cited by 2,040 · see citing works
RAS oncogenes: the first 30 years
Malumbres, M., & Barbacid, M. (2003) · Nature Reviews Cancer · doi:10.1038/nrc1097 · Cited by 1,902 · see citing works
The Ras superfamily at a glance
Wennerberg, K., Rossman, K. L., & Der, C. J. (2005) · Journal of Cell Science · doi:10.1242/jcs.01660 · Cited by 1,549 · see citing works
Self-citationSahai, E. A., & Marshall, C. J. (2002) · Nature reviews. Cancer · doi:10.1038/nrc725 · Cited by 1,398 · see citing works
Rho GTPases and actin dynamics in membrane protrusions and vesicle trafficking
Ridley, A. J. (2006) · Trends in Cell Biology · doi:10.1016/j.tcb.2006.08.006 · Cited by 1,180 · see citing works
Rational design and characterization of a Rac GTPase-specific small molecule inhibitor
Gao, Y., Dickerson, J. B., Guo, F., Zheng, J., & Zheng, Y. (2004) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0307512101 · Cited by 1,091 · see citing works
Kozma, R., Ahmed, S., Best, A., & Lim, L. (1995) · Molecular and Cellular Biology · doi:10.1128/mcb.15.4.1942 · Cited by 1,021 · see citing works
An essential role for Rac in Ras transformation
Qiu, R., Chen, J., Kirn, D. H., McCormick, F. P., & Symons, M. H. (1995) · Nature · doi:10.1038/374457a0 · Cited by 883 · see citing works
Bar‐Sagi, D., & Hall, A. (2000) · Cell · doi:10.1016/s0092-8674(00)00115-x · Cited by 778 · see citing works
Activation of Rac1, RhoA, and mitogen-activated protein kinases is required for Ras transformation
Khosravi-Far, R., Solski, P. A., Clark, G. J., Kinch, M. S., & Der, C. J. (1995) · Molecular and Cellular Biology · doi:10.1128/mcb.15.11.6443 · Cited by 683 · see citing works
Self-citationDifferential Localization of Rho Gtpases in Live Cells
Michaelson, D., Silletti, J., Murphy, G., D'Eustachio, P., Rush, M., & Philips, M. R. (2001) · The Journal of Cell Biology · doi:10.1083/jcb.152.1.111 · Cited by 679 · see citing works
Rho-family GTPases: it's not only Rac and Rho (and I like it)
Wennerberg, K., & Der, C. J. (2004) · Journal of Cell Science · doi:10.1242/jcs.01118 · Cited by 615 · see citing works
Self-citationA role for Rac in Tiaml-induced membrane ruffling and invasion
Michiels, F., Habets, G. G. M., Stam, J. C., van der Kammen, R. A., & Collard, J. G. (1995) · Nature · doi:10.1038/375338a0 · Cited by 556 · see citing works
Westwick, J. K., Lambert, Q. T., Clark, G. J., Symons, M. H., Aelst, L. V., Pestell, R. G., & Der, C. J. (1997) · Molecular and Cellular Biology · doi:10.1128/mcb.17.3.1324 · Cited by 436 · see citing works
Self-citationTools of the trade: use of dominant-inhibitory mutants of Ras-family GTPases
Feig, L. (1999) · Nature Cell Biology · doi:10.1038/10018 · Cited by 433 · see citing works
Schnelzer, A., Prechtel, D., Knaus, U. G., Dehne, K., Gerhard, M., Graeff, H., Harbeck, N., Schmitt, M., & Lengyel, E. R. (2000) · Oncogene · doi:10.1038/sj.onc.1203621 · Cited by 411 · see citing works
Crystal structure of Rac1 in complex with the guanine nucleotide exchange region of Tiam1
Worthylake, D. K., Rossman, K. L., & Sondek, J. (2000) · Nature · doi:10.1038/35047014 · Cited by 355 · see citing works
Khosravi‐Far, R., White, M. A., Westwick, J. K., Solski, P. A., Chrzanowska‐Wodnicka, M., Aelst, L. V., Wigler, M. H., & Der, C. J. (1996) · Molecular and Cellular Biology · doi:10.1128/mcb.16.7.3923 · Cited by 343 · see citing works
Self-citationTiam1 mediates Ras activation of Rac by a PI(3)K-independent mechanism
Lambert, J. M., Lambert, Q. T., Reuther, G. W., Malliri, A., Siderovski, D. P., Sondek, J., Collard, J. G., & Der, C. J. (2002) · Nature Cell Biology · doi:10.1038/ncb833 · Cited by 326 · see citing works
Self-citationGAP control: regulating the regulators of small GTPases
Bernards, A., & Settleman, J. E. (2004) · Trends in Cell Biology · doi:10.1016/j.tcb.2004.05.003 · Cited by 310 · see citing works
Thematic review series: Lipid Posttranslational Modifications. Farnesyl transferase inhibitors
Basso, A. D., Kirschmeier, P. T., & Bishop, W. R. (2005) · Journal of Lipid Research · doi:10.1194/jlr.r500012-jlr200 · Cited by 297 · see citing works
Sebti, S. M., & Hamilton, A. D. (2000) · Oncogene · doi:10.1038/sj.onc.1204146 · Cited by 278 · see citing works
Reid, T. S., Terry, K. L., Casey, P. J., & Beese, L. S. (2004) · Journal of Molecular Biology · doi:10.1016/j.jmb.2004.08.056 · Cited by 264 · see citing works
Cloning of a novel human Rac1b splice variant with increased expression in colorectal tumors
Jordan, P., Brazão, R., Boavida, M. G., Gespach, C. P., & Chastre, E. (1999) · Oncogene · doi:10.1038/sj.onc.1203233 · Cited by 253 · see citing works
Roles of the Rac1 and Rac3 GTPases in human tumor cell invasion
Chan, A. Y., Coniglio, S. J., Chuang, Y.-Y., Michaelson, D., Knaus, U. G., Philips, M. R., & Symons, M. H. (2005) · Oncogene · doi:10.1038/sj.onc.1208909 · Cited by 247 · see citing works
The role of Rho GTPases in disease development
Boettner, B., & Van Aelst, L. (2002) · Gene · doi:10.1016/s0378-1119(02)00426-2 · Cited by 229 · see citing works
Ectopic expression of VAV1 reveals an unexpected role in pancreatic cancer tumorigenesis
Fernández-Zapico, M. E., Gonzalez-Paz, N. C., Weiss, E. A., Savoy, D. N., Molina, J. R., Fonseca, R., Smyrk, T. C., Chari, S. T., Urrutia, R. A., & Billadeau, D. D. (2005) · Cancer Cell · doi:10.1016/j.ccr.2004.11.024 · Cited by 221 · see citing works
Ridley, A. J. (2004) · Breast Cancer Research and Treatment · doi:10.1023/b:brea.0000018423.47497.c6 · Cited by 189 · see citing works
Singh, A., Karnoub, A. E., Palmby, T. R., Lengyel, E. R., Sondek, J., & Der, C. J. (2004) · Oncogene · doi:10.1038/sj.onc.1208182 · Cited by 174 · see citing works
Self-citationThe RhoGAP Protein DLC-1 Functions as a Metastasis Suppressor in Breast Cancer Cells
Steve Goodison, B., Yuan, J., Sloan, D. D., Kim, R. S., Li, C., Popescu, N. C., & Urquidi, V. (2005) · Cancer Research · doi:10.1158/0008-5472.can-04-3043 · Cited by 157 · see citing works
Alternative Splicing of Rac1 Generates Rac1b, a Self-activating GTPase
Fiegen, D., Haeusler, L. C., Blumenstein, L., Herbrand, U., Dvorský, R., Vetter, I. R., & Ahmadian, M. R. (2004) · Journal of Biological Chemistry · doi:10.1074/jbc.m310281200 · Cited by 148 · see citing works
Ando, S., Kaibuchi, K., Sasaki, T., Hiraoka, K., Nishiyama, T., Mizuno, T., Asada, M., Nunoi, H., Matsuda, I., & Matsuura, Y. (1992) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(18)35665-5 · Cited by 145 · see citing works
Désiré, L., Bourdin, J., Loiseau, N., Peillon, H., Picard, V., Oliveira, C. D., Bachelot, F., Leblond, B., Taverne, T., Beausoleil, E., et al. (2005) · Journal of Biological Chemistry · doi:10.1074/jbc.m507913200 · Cited by 134 · see citing works
Self-citationPro-metastatic signaling by c-Met through RAC-1 and reactive oxygen species (ROS)
Ferraro, D. A., Corso, S., Fasano, E., Panieri, E., Santangelo, R., Borrello, S., Giordano, S., Pani, G., & Galeotti, T. (2006) · Oncogene · doi:10.1038/sj.onc.1209409 · Cited by 131 · see citing works
Matos, P., Collard, J. G., & Jordan, P. (2003) · Journal of Biological Chemistry · doi:10.1074/jbc.m308215200 · Cited by 129 · see citing works
Chuang, T., Xu, X., Knaus, U. G., Hart, M. J., & Bokoch, G. (1993) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(18)54000-x · Cited by 124 · see citing works
EphrinA1 inactivates integrin-mediated vascular smooth muscle cell spreading via the Rac/PAK pathway
Deroanne, C., Vouret‐Craviari, V., Wang, B., & Pouysségur, J. (2003) · Journal of Cell Science · doi:10.1242/jcs.00308 · Cited by 124 · see citing works
Oncogenic activity of Tiam1 and Rac1 in NIH3T3 cells.
van Leeuwen, F. N., van der Kammen, R. A., Habets, G. G. M., & Collard, J. G. (1995) · PubMed · Cited by 120 · see citing works
Kleer, C. G., Griffith, K. A., Sabel, M. S., Gallagher, G., van Golen, K. L., Wu, Z.-F., & Merajver, S. D. (2005) · Breast Cancer Research and Treatment · doi:10.1007/s10549-005-4170-6 · Cited by 116 · see citing works
Hiraoka, K., Kaibuchi, K., Ando, S., Musha, T., Takaishi, K., Mizuno, T., Asada, M., Ménard, L., Tomhave, E. D., Didsbury, J. R., et al. (1992) · Biochemical and Biophysical Research Communications · doi:10.1016/0006-291x(92)91820-g · Cited by 114 · see citing works
RhoG Signals in Parallel with Rac1 and Cdc42
Wennerberg, K., Ellerbroek, S. M., Liu, R.-Y., Karnoub, A. E., Burridge, K., & Der, C. J. (2002) · Journal of Biological Chemistry · doi:10.1074/jbc.m203816200 · Cited by 106 · see citing works
Self-citationMolecular basis for Rac1 recognition by guanine nucleotide exchange factors.
(2001) · Nature Structural Biology · doi:10.1038/nsb719 · Cited by 93 · see citing works
Self-citationMas Oncogene Signaling and Transformation Require the Small GTP-Binding Protein Rac
Zohn, I. E., Symons, M. H., Chrzanowska‐Wodnicka, M., Westwick, J. K., & Der, C. J. (1998) · Molecular and Cellular Biology · doi:10.1128/mcb.18.3.1225 · Cited by 84 · see citing works
Self-citationConsequences of weak interaction of rho GDI with the GTP-bound forms of rho p21 and rac p21.
Sasaki, T., Kato, M., & Takai, Y. (1993) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(20)80478-5 · Cited by 73 · see citing works
Rac is required for v-Abl tyrosine kinase to activate mitogenesis
Renshaw, M. W., Lea-Chou, E., & Wang, J. Y. J. (1996) · Current Biology · doi:10.1016/s0960-9822(02)00424-4 · Cited by 73 · see citing works
Chen, S. Y., Huff, S. Y., Lai, C., Der, C. J., & Powers, S. (1994) · PubMed · Cited by 70 · see citing works
Self-citationManne, V., Yamazaki, S., & Kung, H. F. (1984) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.81.22.6953 · Cited by 66 · see citing works
Joyce, P. L., & Cox, A. D. (2003) · PubMed · Cited by 61 · see citing works
The Mechanism of Ras GTPase Activation by Neurofibromin
Phillips, R. A., Hunter, J. L., Eccleston, J. F., & Webb, M. R. (2003) · Biochemistry · doi:10.1021/bi027316z · Cited by 60 · see citing works
Purification and characterization of c-Ki-ras p21 from bovine brain crude membranes.
Yamashita, T., Yamamoto, K., Kikuchi, A., Kawata, M., Kondo, J. D. M., HISHIDA, T., Teranishi, Y., Shiku, H., & Takai, Y. (1988) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(18)37515-x · Cited by 41 · see citing works
Structural and Biophysical Insights into the Role of the Insert Region in Rac1 Function
Thapar, R., Karnoub, A. E., & Campbell, S. L. (2002) · Biochemistry · doi:10.1021/bi0120087 · Cited by 31 · see citing works
Purification and Biochemical Properties of Rac1, 2, 3 and the Splice Variant Rac1b
Haeusler, L. C., Hemsath, L., Fiegen, D., Blumenstein, L., Herbrand, U., Stege, P., Dvorský, R., & Ahmadian, M. R. (2006) · Methods in enzymology on CD-ROM/Methods in enzymology · doi:10.1016/s0076-6879(06)06001-0 · Cited by 30 · see citing works
Expression of Rac3 in human brain tumors
Hwang, S., Chang, J.-H., Cheng, T.-S., Sy, W.-D., Lieu, A., Lin, C., Lee, K., Howng, S., & Hong, Y. (2005) · Journal of Clinical Neuroscience · doi:10.1016/j.jocn.2004.08.013 · Cited by 25 · see citing works
VAV1: A new target in pancreatic cancer?
DeNicol, G., & Tuveson, D. A. (2005) · Cancer Biology & Therapy · doi:10.4161/cbt.4.5.1781 · Cited by 20 · see citing works
Shutes, A., Phillips, R. A., Corrie, J. E. T., & Webb, M. R. (2002) · Biochemistry · doi:10.1021/bi0119464 · Cited by 17 · see citing works
Self-citationOnozawa, T., Danjoh, I., & Fujiyama, A. (1995) · Yeast · doi:10.1002/yea.320110902 · Cited by 17 · see citing works
[14] Ras-Cdc25 and Rho-Dbl binding assays: Complex formation in vitro
Hart, M. J., & Powers, S. (1995) · Methods in enzymology on CD-ROM/Methods in enzymology · doi:10.1016/s0076-6879(95)55016-x · Cited by 14 · see citing works
Introduction: Identification, analysis, and characterization of fungal prions
Masison, D. C. (2006) · Methods · doi:10.1016/j.ymeth.2006.05.001 · Cited by 8 · see citing works
Flagged first, then by citations
Research works printed but not linked: 2
- Gao, Y., Dickerson, J. B., Guo, F., Zheng, J., and Zheng, Y. (2004) Proc. Natl. Acad. Sci. U. S. A. 101, 7618 -7623
- Manne, V., Yamazaki, S., and Kung, H. F. (1984) Proc. Natl. Acad. Sci.
Cited by
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Maurer, T., Garrenton, L. S., Oh, A., Pitts, K., Anderson, D. J., Skelton, N. J., Fauber, B. P., Pan, B., Malek, S., Stokoe, D., et al. (2012) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1116510109 · Cited by 618 · see citing works
PI3K signaling in cancer: beyond AKT
Lien, E. C., Dibble, C. C., & Toker, A. (2017) · Current Opinion in Cell Biology · doi:10.1016/j.ceb.2017.02.007 · Cited by 446 · see citing works
Phosphatidylserine receptor BAI1 and apoptotic cells as new promoters of myoblast fusion
Hochreiter, A. E., Lee, C. S., Kinchen, J. M., Sokolowski, J. D., Arandjelovic, S., Call, J. A., Klibanov, A. L., Yan, Z., Mandell, J. W., & Ravichandran, K. S. (2013) · Nature · doi:10.1038/nature12135 · Cited by 286 · see citing works
Apoptotic cell clearance by bronchial epithelial cells critically influences airway inflammation
Juncadella, I. J., Kadl, A., Sharma, A. K., Shim, Y. M., Hochreiter, A. E., Borish, L., & Ravichandran, K. S. (2012) · Nature · doi:10.1038/nature11714 · Cited by 287 · see citing works
RAC1: An Emerging Therapeutic Option for Targeting Cancer Angiogenesis and Metastasis
Bid, H. K., Roberts, R. D., Manchanda, P. K., & Houghton, P. J. (2013) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-13-0164 · Cited by 265 · see citing works
Characterization of EHop-016, Novel Small Molecule Inhibitor of Rac GTPase
Montalvo-Ortiz, B. L., Castillo‐Pichardo, L., O'Farril, E. H., Humphries‐Bickley, T., Mota‐Peynado, A. D. L., Cubano, L. A., Vlaar, C. P., & Dharmawardhane, S. (2012) · Journal of Biological Chemistry · doi:10.1074/jbc.m111.334524 · Cited by 240 · see citing works
Targeting Rac and Cdc42 GTPases in Cancer
Maldonado, M. D. M., & Dharmawardhane, S. (2018) · Cancer Research · doi:10.1158/0008-5472.can-18-0619 · Cited by 236 · see citing works
Approach for targeting Ras with small molecules that activate SOS-mediated nucleotide exchange
Burns, M. C., Sun, Q., Daniels, R. N., Camper, D., Kennedy, J. P., Phan, J., Olejniczak, E. T., Lee, T., Waterson, A. G., Rossanese, O. W., et al. (2014) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1315798111 · Cited by 199 · see citing works
Neuronal Growth Cone Retraction Relies on Proneurotrophin Receptor Signaling Through Rac
Deinhardt, K., Kim, T., Spellman, D. S., Mains, R. E., Eipper, B. A., Neubert, T. A., Chao, M. V., & Hempstead, B. L. (2011) · Science Signaling · doi:10.1126/scisignal.2002060 · Cited by 183 · see citing works
Nieborowska-Skorska, M., Kopinski, P. K., Ray, R., Hoser, G., Ngaba, D., Flis, S., Cramer, K., Reddy, M. M., Koptyra, M., Penserga, T., et al. (2012) · Blood · doi:10.1182/blood-2011-10-385658 · Cited by 190 · see citing works
Overmeyer, J. H., Young, A. M., Bhanot, H., & Maltese, W. A. (2011) · Molecular Cancer · doi:10.1186/1476-4598-10-69 · Cited by 172 · see citing works
Rac1 in human diseases: The therapeutic potential of targeting Rac1 signaling regulatory mechanisms
Marei, H., & Malliri, A. (2016) · Small GTPases · doi:10.1080/21541248.2016.1211398 · Cited by 168 · see citing works
Paving the Rho in cancer metastasis: Rho GTPases and beyond
Jansen, S. R., Gosens, R., Wieland, T., & Schmidt, M. (2017) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2017.09.002 · Cited by 169 · see citing works
Recruitment of Actin Modifiers to TrkA Endosomes Governs Retrograde NGF Signaling and Survival
Harrington, A., Hillaire, C. S., Zweifel, L. S., Glebova, N. O., Philippidou, P., Halegoua, S., & Ginty, D. D. (2011) · Cell · doi:10.1016/j.cell.2011.07.008 · Cited by 147 · see citing works
Approaches of targeting Rho GTPases in cancer drug discovery
Lin, Y., & Zheng, Y. (2015) · Expert Opinion on Drug Discovery · doi:10.1517/17460441.2015.1058775 · Cited by 133 · see citing works
The role of small GTPases of the Rho/Rac family in TGF‐β‐induced EMT and cell motility in cancer
Ungefroren, H., Witte, D. P., & Lehnert, H. (2017) · Developmental Dynamics · doi:10.1002/dvdy.24505 · Cited by 127 · see citing works
Comprehensive Survey of Chemical Libraries for Drug Discovery and Chemical Biology: 2007
Dolle, R. E., Bourdonnec, B. L., Goodman, A. J., Morales, G. A., Thomas, C. J., & Zhang, W. (2008) · Journal of Combinatorial Chemistry · doi:10.1021/cc800119z · Cited by 127 · see citing works
Characterization of EHT 1864, a novel small molecule inhibitor of Rac family small GTPases
(2008) · Methods in Enzymology · doi:10.1016/s0076-6879(07)00409-0 · Cited by 126 · see citing works
Self-citationWinter, J., Anderson, M., Blades, K., Brassington, C., Breeze, A. L., Chresta, C. M., Embrey, K. J., Fairley, G., Faulder, P., Finlay, M. R. V., et al. (2015) · Journal of Medicinal Chemistry · doi:10.1021/jm501660t · Cited by 126 · see citing works
Sabra, H., Brunner, M., Mandati, V., Wehrle‐Haller, B., Lallemand, D., Ribba, A., Chevalier, G., Guardiola, P., Block, M. R., & Bouvard, D. (2017) · Journal of Biological Chemistry · doi:10.1074/jbc.m117.808063 · Cited by 121 · see citing works
Rac2 Modulates Atherosclerotic Calcification by Regulating Macrophage Interleukin-1β Production
Ceneri, N. M., Zhao, L., Young, B. D., Healy, A. L., Coşkun, S., Vasavada, H. H., Yarovinsky, T. O., Ike, K., Pardi, R., Qin, L., et al. (2016) · Arteriosclerosis Thrombosis and Vascular Biology · doi:10.1161/atvbaha.116.308507 · Cited by 122 · see citing works
Reciprocal Activation within a Kinase-Effector Complex Underlying Persistence of Structural LTP
Saneyoshi, T., Matsuno, H., Suzuki, A., Murakoshi, H., Hedrick, N. G., Agnello, E., O’Connell, R., Stratton, M. M., Yasuda, R., & Hayashi, Y. (2019) · Neuron · doi:10.1016/j.neuron.2019.04.012 · Cited by 119 · see citing works
Shank3 Deficiency Induces NMDA Receptor Hypofunction via an Actin-Dependent Mechanism
Duffney, L. J., Wei, J., Cheng, J., Liu, W., Smith, K. R., Kittler, J. T., & Yan, Z. (2013) · The Journal of Neuroscience · doi:10.1523/jneurosci.1175-13.2013 · Cited by 115 · see citing works
Targeting R ho‐ GTP ases in immune cell migration and inflammation
Biro, M., Munoz, M. A., & Weninger, W. (2014) · British Journal of Pharmacology · doi:10.1111/bph.12658 · Cited by 115 · see citing works
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Liang, J., Oyang, L., Rao, S., Han, Y., Luo, X., Yi, P., Lin, J., Xia, L., Hu, J., Tan, S., et al. (2021) · Frontiers in Oncology · doi:10.3389/fonc.2021.674426 · Cited by 112 · see citing works
Rho GTPases as therapeutic targets in cancer (Review)
Cardama, G. A., González, N., Maggio, J., Menna, P. L., & Gomez, D. E. (2017) · International Journal of Oncology · doi:10.3892/ijo.2017.4093 · Cited by 107 · see citing works
Characterization of a Dual Rac/Cdc42 Inhibitor MBQ-167 in Metastatic Cancer
Humphries‐Bickley, T., Castillo‐Pichardo, L., O'Farril, E. H., Borrero-García, L. D., Forestier-Román, I., Gerena, Y., Blanco, M., Rivera-Robles, M. J., Rodríguez-Medina, J. R., Cubano, L. A., et al. (2017) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-16-0442 · Cited by 105 · see citing works
Aksamitiene, E., Achanta, S., Kölch, W., Kholodenko, B. Ν., Hoek, J. B., & Kiyatkin, A. B. (2011) · Cellular Signalling · doi:10.1016/j.cellsig.2011.06.014 · Cited by 103 · see citing works
Kawarazaki, W., Nagase, M., Yoshida, S., Takeuchi, M., Ishizawa, K., Ayuzawa, N., Ueda, K., & Fujita, T. (2012) · Journal of the American Society of Nephrology · doi:10.1681/asn.2011070734 · Cited by 102 · see citing works
Androgen-Induced Cell Migration: Role of Androgen Receptor/Filamin A Association
Castoria, G., D’Amato, L., Ciociola, A., Giovannelli, P., Giraldi, T., Sepe, L., Paolella, G., Barone, M. V., Migliaccio, A., & Auricchio, F. (2011) · PLoS ONE · doi:10.1371/journal.pone.0017218 · Cited by 102 · see citing works
Guanine nucleotide exchange factors for RhoGTPases: Good therapeutic targets for cancer therapy?
Lazer, G., & Katzav, S. (2010) · Cellular Signalling · doi:10.1016/j.cellsig.2010.10.022 · Cited by 100 · see citing works
A Cell Active Chemical GEF Inhibitor Selectively Targets the Trio/RhoG/Rac1 Signaling Pathway
Bouquier, N., Vignal, E., Charrasse, S., Weill, M., Schmidt, S., Léonetti, J., Blangy, A., & Fort, P. (2009) · Chemistry & Biology · doi:10.1016/j.chembiol.2009.04.012 · Cited by 101 · see citing works
Olson, M. F. (2016) · Small GTPases · doi:10.1080/21541248.2016.1218407 · Cited by 100 · see citing works
Induction of Nonapoptotic Cell Death by Activated Ras Requires Inverse Regulation of Rac1 and Arf6
Bhanot, H., Young, A. M., Overmeyer, J. H., & Maltese, W. A. (2010) · Molecular Cancer Research · doi:10.1158/1541-7786.mcr-10-0090 · Cited by 99 · see citing works
Gastonguay, A. J., Berg, T. J., Hauser, A. D., Schuld, N. J., Lorimer, E., & Williams, C. L. (2012) · Cancer Biology & Therapy · doi:10.4161/cbt.20082 · Cited by 99 · see citing works
Rho GTPases in hepatocellular carcinoma
Grise, F., Bidaud-Meynard, A., & Moreau, V. (2009) · Biochimica et Biophysica Acta (BBA) - Reviews on Cancer · doi:10.1016/j.bbcan.2008.12.003 · Cited by 98 · see citing works
Mehner, C., Miller, E. E., Nassar, A., Bamlet, W. R., Radisky, E. S., & Radisky, D. C. (2015) · Genes & Cancer · doi:10.18632/genesandcancer.90 · Cited by 97 · see citing works
Dütting, S., Heidenreich, J. F., Cherpokova, D., Amin, E., Zhang, S.-C., Ahmadian, M. R., Brakebusch, C., & Nieswandt, B. (2015) · Journal of Thrombosis and Haemostasis · doi:10.1111/jth.12861 · Cited by 94 · see citing works
Cheng, S., Ramachandran, B., Behrmann, A., Shao, J.-S., Mead, M., Smith, C., Krchma, K., Arredondo, Y. B., Kovács, A., Kapoor, K., et al. (2015) · Circulation Research · doi:10.1161/circresaha.117.306712 · Cited by 93 · see citing works
Focal-adhesion targeting links caveolin-1 to a Rac1-degradation pathway
Nethe, M., Anthony, E. C., Fernandez‐Borja, M., Dee, R., Geerts, D., Hensbergen, P. J., Deelder, A. M., Schmidt, G., & Hordijk, P. L. (2010) · Journal of Cell Science · doi:10.1242/jcs.062919 · Cited by 91 · see citing works
Secretion-mediated STAT3 activation promotes self-renewal of glioma stem-like cells during hypoxia
Bonnin, D. A. A., Havrda, M. C., Lee, M. C., Liu, H., Zhang, Z., Nguyen, L., Harrington, L. X., Hassanpour, S., Cheng, C., & Israel, M. A. (2017) · Oncogene · doi:10.1038/onc.2017.404 · Cited by 91 · see citing works
The Rac Inhibitor EHop-016 Inhibits Mammary Tumor Growth and Metastasis in a Nude Mouse Model
Castillo‐Pichardo, L., Humphries‐Bickley, T., de la Parra, C., Forestier-Román, I., Martínez‐Ferrer, M., O'Farril, E. H., Vlaar, C. P., Ferrer‐Acosta, Y., Washington, A. V., Cubano, L. A., et al. (2014) · Translational Oncology · doi:10.1016/j.tranon.2014.07.004 · Cited by 90 · see citing works
The F-BAR domain protein PACSIN2 associates with Rac1 and regulates cell spreading and migration
de Kreuk, B.-J., Nethe, M., Fernandez‐Borja, M., Anthony, E. C., Hensbergen, P. J., Deelder, A. M., Plomann, M., & Hordijk, P. L. (2011) · Journal of Cell Science · doi:10.1242/jcs.080630 · Cited by 88 · see citing works
Pollitt, A. Y., Grygielska, B., Leblond, B., Désiré, L., Eble, J. A., & Watson, S. P. (2010) · Blood · doi:10.1182/blood-2009-12-257212 · Cited by 88 · see citing works
Self-citationA Competitive Nucleotide Binding Inhibitor: In Vitro Characterization of Rab7 GTPase Inhibition
Agola, J. O., Lin, H., Surviladze, Z., Ursu, O., Waller, A., Strouse, J. J., Simpson, D. S., Schroeder, C. E., Oprea, T. I., Golden, J. E., et al. (2012) · ACS Chemical Biology · doi:10.1021/cb3001099 · Cited by 86 · see citing works
Zhu, G.-F., Fan, Z., Ding, M., Zhang, H.-B., Mu, L., Ding, Y., Zhang, Y., Jia, B., Chen, L., Chang, Z., et al. (2015) · Oncogene · doi:10.1038/onc.2015.45 · Cited by 86 · see citing works
Drugging the Small GTPase Pathways in Cancer Treatment: Promises and Challenges
Prieto‐Domínguez, N., Parnell, C., & Teng, Y. (2019) · Cells · doi:10.3390/cells8030255 · Cited by 85 · see citing works
Kunschmann, T., Puder, S., Fischer, T., Steffen, A., Rottner, K., & Mierke, C. T. (2019) · Scientific Reports · doi:10.1038/s41598-019-43975-0 · Cited by 85 · see citing works
Targeting small GTPases: emerging grasps on previously untamable targets, pioneered by KRAS
Yin, G., Huang, J., Petela, J., Jiang, H., Zhang, Y., Gong, S., Wu, J., Liu, B., Shi, J., & Gao, Y. (2023) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-023-01441-4 · Cited by 87 · see citing works
The small GTPase Rac1 is a novel binding partner of Bcl-2 and stabilizes its antiapoptotic activity
Velaithan, R., Kang, J., Hirpara, J. L., Loh, T. K. S., Goh, B. C., Bras, M. L., Brenner, C., Clement, M., & Pervaiz, S. (2011) · Blood · doi:10.1182/blood-2010-08-301283 · Cited by 84 · see citing works
Adherens junction regulates cryptic lamellipodia formation for epithelial cell migration
Ozawa, M., Hiver, S., Yamamoto, T., Shibata, T., Upadhyayula, S., Mimori‐Kiyosue, Y., & Takeichi, M. (2020) · The Journal of Cell Biology · doi:10.1083/jcb.202006196 · Cited by 84 · see citing works
Cardama, G. A., Comin, M. J., Hornos, L., González, N., Defelipe, L. A., Turjanski, A. G., Alonso, D. F., Gomez, D. E., & Menna, P. L. (2013) · Anti-Cancer Agents in Medicinal Chemistry · doi:10.2174/18715206113136660334 · Cited by 84 · see citing works
Macropinocytosis drives T cell growth by sustaining the activation of mTORC1
Charpentier, J. C., Chen, D., Lapinski, P. E., Turner, J. S., Grigorova, I., Swanson, J. A., & King, P. D. (2020) · Nature Communications · doi:10.1038/s41467-019-13997-3 · Cited by 83 · see citing works
Rap1-Rac1 Circuits Potentiate Platelet Activation
Stefanini, L., Boulaftali, Y., Ouellette, T. D., Holinstat, M. A., Désiré, L., Leblond, B., André, P., Conley, P. B., & Bergmeier, W. (2011) · Arteriosclerosis Thrombosis and Vascular Biology · doi:10.1161/atvbaha.111.239194 · Cited by 82 · see citing works
Self-citationBlockade of Inflammatory Responses by a Small-Molecule Inhibitor of the Rac Activator DOCK2
Nishikimi, A., Uruno, T., Duan, X., Cao, Q., Okamura, Y., Saitoh, T., Saito, N., Sakaoka, S., Du, Y., Suenaga, A., et al. (2012) · Chemistry & Biology · doi:10.1016/j.chembiol.2012.03.008 · Cited by 83 · see citing works
Function of the Nucleotide Exchange Activity of Vav1 in T Cell Development and Activation
Saveliev, A., Vanes, L., Ksionda, O., Rapley, J., Smerdon, S. J., Rittinger, K., & Tybulewicz, V. L. J. (2009) · Science Signaling · doi:10.1126/scisignal.2000420 · Cited by 81 · see citing works
Patel, S. P., Tang, J., Overstreet, J. M., Anorga, S., Lian, F., Arnouk, A., Goldschmeding, R., Higgins, P. J., & Samarakoon, R. (2019) · The FASEB Journal · doi:10.1096/fj.201802489rr · Cited by 77 · see citing works
Direct Modulation of Small GTPase Activity and Function
Cromm, P. M., Spiegel, J., Grossmann, T. N., & Waldmann, H. (2015) · Angewandte Chemie International Edition · doi:10.1002/anie.201504357 · Cited by 78 · see citing works
Modulation of actin dynamics by Rac1 to target cognitive function
Tejada‐Simon, M. V. (2015) · Journal of Neurochemistry · doi:10.1111/jnc.13100 · Cited by 76 · see citing works
Racchetti, G., D’Alessandro, R., & Meldolesi, J. (2011) · Glia · doi:10.1002/glia.22280 · Cited by 75 · see citing works
Seljeset, S., & Siehler, S. (2012) · Journal of Receptors and Signal Transduction · doi:10.3109/10799893.2012.692118 · Cited by 74 · see citing works
The VEGF/Rho GTPase signalling pathway: A promising target for anti-angiogenic/anti-invasion therapy
van der Meel, R., Symons, M. H., Kudernatsch, R., Kok, R. J., Schiffelers, R. M., Storm, G., Gallagher, W. M., & Byrne, A. T. (2011) · Drug Discovery Today · doi:10.1016/j.drudis.2011.01.005 · Cited by 73 · see citing works
Martinez, L. A., & Tejada-Simon, M. V. (2011) · Neuropharmacology · doi:10.1016/j.neuropharm.2011.04.017 · Cited by 72 · see citing works
The small GTPase RhoG mediates glioblastoma cell invasion
Kwiatkowska, A., Didier, S., Ensign, S. P. F., Chuang, Y.-Y., White, T. G., Berens, M. E., Rushing, E. J., Eschbacher, J., Tran, N. L., Chan, A. Y., et al. (2012) · Molecular Cancer · doi:10.1186/1476-4598-11-65 · Cited by 70 · see citing works
Attacking the supply wagons to starve cancer cells to death
Selwan, E. M., Finicle, B. T., Kim, S. M., & Edinger, A. L. (2016) · FEBS Letters · doi:10.1002/1873-3468.12121 · Cited by 70 · see citing works
mTOR Signalling in Head and Neck Cancer: Heads Up
Tan, F. H., Bai, Y., Saintigny, P., & Darido, C. (2019) · Cells · doi:10.3390/cells8040333 · Cited by 66 · see citing works
RAC1B: A Rho GTPase with Versatile Functions in Malignant Transformation and Tumor Progression
Melzer, C., Hass, R., Lehnert, H., & Ungefroren, H. (2019) · Cells · doi:10.3390/cells8010021 · Cited by 69 · see citing works
GIT1 and βPIX Are Essential for GABAA Receptor Synaptic Stability and Inhibitory Neurotransmission
Smith, K. R., Davenport, E. C., Wei, J., Li, X., Pathania, M., Vaccaro, V., Yan, Z., & Kittler, J. T. (2014) · Cell Reports · doi:10.1016/j.celrep.2014.08.061 · Cited by 65 · see citing works
Hodakoski, C., Hopkins, B. D., Zhang, G., Su, T., Cheng, Z., Morris, R., Rhee, K. Y., Goncalves, M. D., & Cantley, L. C. (2019) · Cancers · doi:10.3390/cancers11010037 · Cited by 67 · see citing works
Death pathways triggered by activated Ras in cancer cells
Jean, H. O. (2010) · Frontiers in bioscience · doi:10.2741/3814 · Cited by 68 · see citing works
Surviladze, Z., Waller, A., Wu, Y., Romero, E., Edwards, B. S., Wandinger‐Ness, A., & Sklar, L. A. (2009) · SLAS DISCOVERY · doi:10.1177/1087057109352240 · Cited by 66 · see citing works
Goka, E. T., & Lippman, M. E. (2015) · Oncogene · doi:10.1038/onc.2014.468 · Cited by 65 · see citing works
RAC1 as a Therapeutic Target in Malignant Melanoma
Cannon, A. C., Uribe‐Alvarez, C., & Chernoff, J. (2020) · Trends in cancer · doi:10.1016/j.trecan.2020.02.021 · Cited by 65 · see citing works
Targeting the cytoskeleton against metastatic dissemination
Ruggiero, C., & Lalli, E. (2021) · Cancer and Metastasis Reviews · doi:10.1007/s10555-020-09936-0 · Cited by 64 · see citing works
Targeting of Rac GTPases blocks the spread of intact human breast cancer
Katz, E., Sims, A. H., Sproul, D., Caldwell, H., Dixon, J. M., Meehan, R. R., & Harrison, D. J. (2012) · Oncotarget · doi:10.18632/oncotarget.520 · Cited by 62 · see citing works
Rnd3/RhoE Is down-regulated in hepatocellular carcinoma and controls cellular invasion
Grise, F., Sena, S., Bidaud-Meynard, A., Baud, J., Hiriart, J., Makki, K., Dugot‐Senant, N., Staedel, C., Bioulac‐Sage, P., Zucman‐Rossi, J., et al. (2012) · Hepatology · doi:10.1002/hep.25568 · Cited by 62 · see citing works
The physiological regulation of macropinocytosis during Dictyostelium growth and development
Williams, T. D., & Kay, R. R. (2018) · Journal of Cell Science · doi:10.1242/jcs.213736 · Cited by 58 · see citing works
Rosenblatt, A. E., Garcia, M. I., Lyons, L. S., Xie, Y., Maiorino, C., Désiré, L., Slingerland, J., & Burnstein, K. L. (2010) · Endocrine Related Cancer · doi:10.1677/erc-10-0049 · Cited by 60 · see citing works
Essential role of endocytosis for Interleukin-4 receptor mediated JAK/STAT signalling
Kurgonaite, K., Gandhi, H., Kurth, T., Pautot, S., Schwille, P., Weidemann, T., & Bökel, C. (2015) · Journal of Cell Science · doi:10.1242/jcs.170969 · Cited by 61 · see citing works
Targeting Rho GTPase Signaling for Cancer Therapy
Mardilovich, K., Olson, M. F., & Baugh, M. D. (2012) · Future Oncology · doi:10.2217/fon.11.143 · Cited by 59 · see citing works
Pandey, D. B., Goyal, P., Dwivedi, S., & Siess, W. (2009) · Blood · doi:10.1182/blood-2008-10-183582 · Cited by 58 · see citing works
Lissanu, Y., Shi, Y., Rai, K., Nezi, L., Amin, S. B., Wu, C.-C., Akdemir, K. C., Mahdavi, M., Peng, Q., Chang, Q., et al. (2016) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1513801113 · Cited by 58 · see citing works
A Potent and Selective Inhibitor of Cdc42 GTPase
Surviladze, Z., Waller, A., Strouse, J. J., Bologa, C., Ursu, O., Salas, V. M., Parkinson, J. F., Phillips, G. K., Romero, E., Wandinger‐Ness, A., et al. (2010) · DigitalCommons-Cedarville (Cedarville University) · Cited by 57 · see citing works
G protein signaling in the parasite Entamoeba histolytica
Bosch, D. E., & Siderovski, D. P. (2013) · Experimental & Molecular Medicine · doi:10.1038/emm.2013.30 · Cited by 58 · see citing works
Pajic, M., Herrmann, D., Vennin, C., Conway, J. R. W., Chin, V. T., Johnsson, A., Welch, H. C. E., & Timpson, P. (2015) · Small GTPases · doi:10.4161/21541248.2014.973749 · Cited by 56 · see citing works
RHO GTPase family in hepatocellular carcinoma
Wang, T., Rao, D., Yu, C., Sheng, J., Luo, Y., Xia, L., & Huang, W. (2022) · Experimental Hematology and Oncology · doi:10.1186/s40164-022-00344-4 · Cited by 56 · see citing works
Cheng, W.-Y., Tong, H., Miller, E. W., Chang, C. J., Remington, S. J., Zucker, R. M., Bromberg, P. A., Samet, J. M., & Höfer, T. (2010) · Environmental Health Perspectives · doi:10.1289/ehp.0901811 · Cited by 56 · see citing works
The role of Rac in tumor susceptibility and disease progression: from biochemistry to the clinic
Casado‐Medrano, V., Baker, M. J., López‐Haber, C., Cooke, M., Wang, S., Caloca, M. J., & Kazanietz, M. G. (2018) · Biochemical Society Transactions · doi:10.1042/bst20170519 · Cited by 55 · see citing works
Regulation of Epithelial-Mesenchymal Transition in Breast Cancer Cells by Cell Contact and Adhesion
Cichon, M. A., Nelson, C. M., & Radisky, D. C. (2015) · Cancer Informatics · doi:10.4137/cin.s18965 · Cited by 55 · see citing works
Atherton, P., Lausecker, F., Harrison, A. J., & Ballestrem, C. (2017) · Journal of Cell Science · doi:10.1242/jcs.192781 · Cited by 55 · see citing works
Tiam1/Rac1 complex controls Il17a transcription and autoimmunity
Kurdi, A. T., Bassil, R., Olah, M., Wu, C., Xiao, S., Taga, M., Frangieh, M., Buttrick, T. S., Orent, W., Bradshaw, E., et al. (2016) · Nature Communications · doi:10.1038/ncomms13048 · Cited by 65 · see citing works
Padmanabhan, J., Chen, K., Sivaraj, D., Henn, D., Kuehlmann, B. A., Kussie, H. C., Zhao, E. T., Kahn, A., Bonham, C. A., Dohi, T., et al. (2023) · Nature Biomedical Engineering · doi:10.1038/s41551-023-01091-5 · Cited by 57 · see citing works
Walliser, C., Hermkes, E., Schade, A., Wiese, S., Deinzer, J., Zapatka, M., Désiré, L., Mertens, D., Stilgenbauer, S., & Gierschik, P. (2016) · Journal of Biological Chemistry · doi:10.1074/jbc.m116.746842 · Cited by 51 · see citing works
Dharmawardhane, S., O'Farril, E. H., & Vlaar, C. P. (2013) · The Enzymes · doi:10.1016/b978-0-12-416749-0.00006-3 · Cited by 51 · see citing works
Bu, F., Min, J., Munshi, Y., Lai, Y., Li, Q., Urayama, A., McCullough, L. D., & Li, J. (2019) · Experimental Neurology · doi:10.1016/j.expneurol.2019.113059 · Cited by 51 · see citing works
Cardama, G. A., Alonso, D. F., González, N., Maggio, J., Gomez, D. E., Rolfo, C. D., & Menna, P. L. (2018) · Critical Reviews in Oncology/Hematology · doi:10.1016/j.critrevonc.2018.01.012 · Cited by 49 · see citing works
RAC1b Overexpression Confers Resistance to Chemotherapy Treatment in Colorectal Cancer
Goka, E. T., Chaturvedi, P., Lopez, D. T. M., Garza, A. D. L., & Lippman, M. E. (2019) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-18-0955 · Cited by 49 · see citing works
Cross-talk between androgen receptor/filamin A and TrkA regulates neurite outgrowth in PC12 cells
Donato, M. D., Bilancio, A., D’Amato, L., Claudiani, P., Oliviero, M. A., Barone, M. V., Auricchio, A., Appella, E., Migliaccio, A., Auricchio, F., et al. (2015) · Molecular Biology of the Cell · doi:10.1091/mbc.e14-09-1352 · Cited by 48 · see citing works
Castoria, G., Giovannelli, P., Donato, M. D., Ciociola, A., Hayashi, R., Bernal, F., Appella, E., Auricchio, F., & Migliaccio, A. (2014) · Cell Death and Disease · doi:10.1038/cddis.2014.497 · Cited by 48 · see citing works
Evelyn, C. R., Ferng, T. T., Rojas, R. J., Larsen, M. J., Sondek, J., & Neubig, R. R. (2009) · SLAS DISCOVERY · doi:10.1177/1087057108328761 · Cited by 47 · see citing works
- Authors
- Shutes, A., Onesto, C., Picard, V., Leblond, B., Schweighoffer, F., & Der, C. J.
- Affiliations
- University of North Carolina at Chapel Hill (US)
- Corresponding author
- Der, Channing J.
- Venue
- Journal of Biological Chemistry
- Publisher
- Elsevier BV
- Published
- 2007-12
- Volume
- 282
- Issue
- 49
- Pages
- 35666-35678
- ISSN
- 0021-9258 (ISSN-L)
- OpenAlex
- W2124054733
- Cited by
- 336
- References
- 62
- Citations by year
- 2026: 14 · 2025: 18 · 2024: 22 · 2023: 16 · 2022: 18 · 2021: 21 · 2020: 22 · 2019: 20 · 2018: 16 · 2017: 22 · 2016: 20 · 2015: 21 · 2014: 7 · 2013: 27 · 2012: 25
- FWCI
- 3.98
- Type
- journal article
- Language
- en
- Open access
- hybrid
- doi.org
- Licence
- Locations
- Journal of Biological Chemistry (publishedVersion, cc-by)
- PubMed (publishedVersion)
- Carolina Digital Repository (University of North Carolina at Chapel Hill) (submittedVersion)
- UNC Libraries
- Funders
- Susan G. Komen for the Cure
- National Institutes of Health (CA063071, CA67771)
- National Cancer Institute (CA 92240, CA 063071, R01CA063071, CA 67771, R01CA092240, U19CA067771)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Kinase Regulation and GTPase Signaling
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cell Biology › Cellular transport and secretion
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Mechanisms of cancer metastasis
- Keywords
- Rac1, guanine nucleotide exchange factor, Tiam1, lamellipodia formation, platelet-derived growth factor, cell transformation, small molecule inhibitors, metastasis
- MeSH terms
- T-Lymphoma Invasion and Metastasis-inducing Protein 1, Animals, Cell Transformation, Neoplastic, Enzyme Activation, Humans, Neoplasm Invasiveness, Neoplasm Metastasis, Neoplasms, Protein Processing, Post-Translational, Pseudopodia, Pyrones, Quinolines, Signal Transduction, Guanine Nucleotide Exchange Factors, rac GTP-Binding Proteins, NIH 3T3 Cells, Cell Line, Tumor, Cell Proliferation, Mice
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