KRAS-specific inhibition using a DARPin binding to a site in the allosteric lobe
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P. Kolasinska-Zwierz | J. Breed | J. Debreczeni | R. Minter | T. Rabbitts | Ami Miller | C. Stubbs | R. Overman | C. Phillips | N. Bery | S. Legg | K. Embrey | N. Barrett | R. Marwood | J. Watson | J. Tart
[1] T. Rabbitts,et al. Bioluminescence Resonance Energy Transfer 2 (BRET2)‐Based RAS Biosensors to Characterize RAS Inhibitors , 2019, Current protocols in cell biology.
[2] S. Phillips,et al. Structure-based development of new RAS-effector inhibitors from a combination of active and inactive RAS-binding compounds , 2019, Proceedings of the National Academy of Sciences.
[3] I. Khan,et al. Targeting the α4-α5 dimerization interface of K-RAS inhibits tumor formation in vivo , 2018, Oncogene.
[4] Narcis Fernandez-Fuentes,et al. Small molecule inhibitors of RAS-effector protein interactions derived using an intracellular antibody fragment , 2018, Nature Communications.
[5] S. Phillips,et al. BRET-based RAS biosensors that show a novel small molecule is an inhibitor of RAS-effector protein-protein interactions , 2018, eLife.
[6] Haiyun Wang,et al. KRAS Dimerization Impacts MEK Inhibitor Sensitivity and Oncogenic Activity of Mutant KRAS , 2018, Cell.
[7] P. Zarrinkar,et al. Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor , 2018, Cell.
[8] M. Neal Waxham,et al. Spatiotemporal Analysis of K-Ras Plasma Membrane Interactions Reveals Multiple High Order Homo-oligomeric Complexes. , 2017, Journal of the American Chemical Society.
[9] Jing Zhang,et al. Structural and functional characterization of a DARPin which inhibits Ras nucleotide exchange , 2017, Nature Communications.
[10] P. Lyne,et al. Targeting KRAS-dependent tumors with AZD4785, a high-affinity therapeutic antisense oligonucleotide inhibitor of KRAS , 2017, Science Translational Medicine.
[11] Matthew E. Welsch,et al. Multivalent Small-Molecule Pan-RAS Inhibitors , 2017, Cell.
[12] Wei Chen,et al. Computational and biochemical characterization of two partially overlapping interfaces and multiple weak-affinity K-Ras dimers , 2017, Scientific Reports.
[13] Marc Therrien,et al. Inhibition of RAS function through targeting an allosteric regulatory site. , 2017, Nature chemical biology.
[14] Ozlem Keskin,et al. Membrane-associated Ras dimers are isoform-specific: K-Ras dimers differ from H-Ras dimers. , 2016, The Biochemical journal.
[15] C. Der,et al. RAS isoforms and mutations in cancer at a glance , 2016, Journal of Cell Science.
[16] F. McCormick. K-Ras protein as a drug target , 2016, Journal of Molecular Medicine.
[17] Frank McCormick,et al. K-Ras protein as a drug target , 2016, Journal of Molecular Medicine.
[18] Yi Liu,et al. Selective Inhibition of Oncogenic KRAS Output with Small Molecules Targeting the Inactive State. , 2016, Cancer discovery.
[19] Neal Rosen,et al. Allele-specific inhibitors inactivate mutant KRAS G12C by a trapping mechanism , 2016, Science.
[20] Ozlem Keskin,et al. GTP-Dependent K-Ras Dimerization. , 2015, Structure.
[21] Xiaolin Nan,et al. Ras-GTP dimers activate the Mitogen-Activated Protein Kinase (MAPK) pathway , 2015, Proceedings of the National Academy of Sciences.
[22] Mitsuhiko Ikura,et al. Oncogenic and RASopathy-associated K-RAS mutations relieve membrane-dependent occlusion of the effector-binding site , 2015, Proceedings of the National Academy of Sciences.
[23] S. Fesik,et al. Drugging the undruggable RAS: Mission Possible? , 2014, Nature Reviews Drug Discovery.
[24] D. Esposito,et al. Dragging ras back in the ring. , 2014, Cancer cell.
[25] A. Breeze,et al. 1H, 13C and 15N resonance assignment for the human K-Ras at physiological pH , 2013, Biomolecular NMR assignments.
[26] M. Therrien,et al. Inhibitors that stabilize a closed RAF kinase domain conformation induce dimerization , 2013, Nature chemical biology.
[27] I. Mellman,et al. Small-molecule ligands bind to a distinct pocket in Ras and inhibit SOS-mediated nucleotide exchange activity , 2012, Proceedings of the National Academy of Sciences.
[28] Dima Kozakov,et al. Analysis of binding site hot spots on the surface of Ras GTPase. , 2011, Journal of molecular biology.
[29] Harrison J. Hocker,et al. Novel Allosteric Sites on Ras for Lead Generation , 2011, PloS one.
[30] Julian Downward,et al. RAS Interaction with PI3K: More Than Just Another Effector Pathway. , 2011, Genes & cancer.
[31] Michel Bouvier,et al. Multiplexing of multicolor bioluminescence resonance energy transfer. , 2010, Biophysical journal.
[32] B. Vanhaesebroeck,et al. The emerging mechanisms of isoform-specific PI3K signalling , 2010, Nature Reviews Molecular Cell Biology.
[33] M. García-Díaz,et al. Structure of the dominant negative S17N mutant of Ras. , 2010, Biochemistry.
[34] I. Prior,et al. Ras isoform abundance and signalling in human cancer cell lines , 2008, Oncogene.
[35] Roger L. Williams,et al. Tumour prevention by a single antibody domain targeting the interaction of signal transduction proteins with RAS , 2007, The EMBO journal.
[36] Andreas Plückthun,et al. Signal sequences directing cotranslational translocation expand the range of proteins amenable to phage display , 2006, Nature Biotechnology.
[37] M. Groves,et al. Affinity maturation of phage display antibody populations using ribosome display. , 2006, Journal of immunological methods.
[38] John Kuriyan,et al. The structural basis of the activation of Ras by Sos , 1998, Nature.