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Items: 22

1.

A Synergistic Anticancer FAK and HDAC Inhibitor Combination Discovered by a Novel Chemical-Genetic High-Content Phenotypic Screen.

Dawson JC, Serrels B, Byron A, Muir MT, Makda A, García-Muñoz A, von Kriegsheim A, Lietha D, Carragher NO, Frame MC.

Mol Cancer Ther. 2019 Nov 29. doi: 10.1158/1535-7163.MCT-19-0330. [Epub ahead of print]

PMID:
31784455
2.

Structural and mechanistic insights into mechanoactivation of focal adhesion kinase.

Bauer MS, Baumann F, Daday C, Redondo P, Durner E, Jobst MA, Milles LF, Mercadante D, Pippig DA, Gaub HE, Gräter F, Lietha D.

Proc Natl Acad Sci U S A. 2019 Apr 2;116(14):6766-6774. doi: 10.1073/pnas.1820567116. Epub 2019 Mar 15.

3.

Structure-Based Design, Synthesis, and Characterization of the First Irreversible Inhibitor of Focal Adhesion Kinase.

Yen-Pon E, Li B, Acebrón-Garcia-de-Eulate M, Tomkiewicz-Raulet C, Dawson J, Lietha D, Frame MC, Coumoul X, Garbay C, Etheve-Quelquejeu M, Chen H.

ACS Chem Biol. 2018 Aug 17;13(8):2067-2073. doi: 10.1021/acschembio.8b00250. Epub 2018 Jun 22.

4.

Exome Sequencing of Plasma DNA Portrays the Mutation Landscape of Colorectal Cancer and Discovers Mutated VEGFR2 Receptors as Modulators of Antiangiogenic Therapies.

Toledo RA, Garralda E, Mitsi M, Pons T, Monsech J, Vega E, Otero Á, Albarran MI, Baños N, Durán Y, Bonilla V, Sarno F, Camacho-Artacho M, Sanchez-Perez T, Perea S, Álvarez R, De Martino A, Lietha D, Blanco-Aparicio C, Cubillo A, Domínguez O, Martínez-Torrecuadrada JL, Hidalgo M.

Clin Cancer Res. 2018 Aug 1;24(15):3550-3559. doi: 10.1158/1078-0432.CCR-18-0103. Epub 2018 Mar 27.

5.

Structural basis for interdomain communication in SHIP2 providing high phosphatase activity.

Le Coq J, Camacho-Artacho M, Velázquez JV, Santiveri CM, Gallego LH, Campos-Olivas R, Dölker N, Lietha D.

Elife. 2017 Aug 9;6. pii: e26640. doi: 10.7554/eLife.26640.

6.

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. 2017 Apr 15;27(8):1727-1730. doi: 10.1016/j.bmcl.2017.02.072. Epub 2017 Feb 28.

PMID:
28284808
7.

Forcing FAK into Transcriptional Activity.

Lietha D.

Structure. 2016 Aug 2;24(8):1223-1225. doi: 10.1016/j.str.2016.07.004.

8.

Expression, Purification, Crystallisation and X-ray Crystallographic Analysis of a Truncated Form of Human Src Homology 2 Containing Inositol 5-Phosphatase 2.

Le Coq J, Heredia Gallego L, Lietha D.

Protein J. 2016 Jun;35(3):225-30. doi: 10.1007/s10930-016-9665-y.

PMID:
27170292
9.

Alternative Activation Mechanisms of Protein Kinase B Trigger Distinct Downstream Signaling Responses.

Balzano D, Fawal MA, Velázquez JV, Santiveri CM, Yang J, Pastor J, Campos-Olivas R, Djouder N, Lietha D.

J Biol Chem. 2015 Oct 9;290(41):24975-85. doi: 10.1074/jbc.M115.651570. Epub 2015 Aug 18.

10.

Allosteric regulation of focal adhesion kinase by PIP₂ and ATP.

Zhou J, Bronowska A, Le Coq J, Lietha D, Gräter F.

Biophys J. 2015 Feb 3;108(3):698-705. doi: 10.1016/j.bpj.2014.11.3454.

11.

Design, synthesis, and evaluation of novel imidazo[1,2-a][1,3,5]triazines and their derivatives as focal adhesion kinase inhibitors with antitumor activity.

Dao P, Smith N, Tomkiewicz-Raulet C, Yen-Pon E, Camacho-Artacho M, Lietha D, Herbeuval JP, Coumoul X, Garbay C, Chen H.

J Med Chem. 2015 Jan 8;58(1):237-51. doi: 10.1021/jm500784e. Epub 2014 Sep 11.

PMID:
25180654
12.

Phosphatidylinositol 4,5-bisphosphate triggers activation of focal adhesion kinase by inducing clustering and conformational changes.

Goñi GM, Epifano C, Boskovic J, Camacho-Artacho M, Zhou J, Bronowska A, Martín MT, Eck MJ, Kremer L, Gräter F, Gervasio FL, Perez-Moreno M, Lietha D.

Proc Natl Acad Sci U S A. 2014 Aug 5;111(31):E3177-86. doi: 10.1073/pnas.1317022111. Epub 2014 Jul 21.

13.

Inhibition of both focal adhesion kinase and fibroblast growth factor receptor 2 pathways induces anti-tumor and anti-angiogenic activities.

Dao P, Jarray R, Smith N, Lepelletier Y, Le Coq J, Lietha D, Hadj-Slimane R, Herbeuval JP, Garbay C, Raynaud F, Chen H.

Cancer Lett. 2014 Jun 28;348(1-2):88-99. doi: 10.1016/j.canlet.2014.03.007. Epub 2014 Mar 19.

PMID:
24657306
14.

Synthesis of novel diarylamino-1,3,5-triazine derivatives as FAK inhibitors with anti-angiogenic activity.

Dao P, Jarray R, Le Coq J, Lietha D, Loukaci A, Lepelletier Y, Hadj-Slimane R, Garbay C, Raynaud F, Chen H.

Bioorg Med Chem Lett. 2013 Aug 15;23(16):4552-6. doi: 10.1016/j.bmcl.2013.06.038. Epub 2013 Jun 24.

PMID:
23845217
15.

Tyrosine phosphorylation of Rac1: a role in regulation of cell spreading.

Chang F, Lemmon C, Lietha D, Eck M, Romer L.

PLoS One. 2011;6(12):e28587. doi: 10.1371/journal.pone.0028587. Epub 2011 Dec 6.

16.

The FERM domain: organizing the structure and function of FAK.

Frame MC, Patel H, Serrels B, Lietha D, Eck MJ.

Nat Rev Mol Cell Biol. 2010 Nov;11(11):802-14. doi: 10.1038/nrm2996. Review.

PMID:
20966971
17.
18.

Spatial and temporal regulation of focal adhesion kinase activity in living cells.

Cai X, Lietha D, Ceccarelli DF, Karginov AV, Rajfur Z, Jacobson K, Hahn KM, Eck MJ, Schaller MD.

Mol Cell Biol. 2008 Jan;28(1):201-14. Epub 2007 Oct 29.

19.

Structural basis for the autoinhibition of focal adhesion kinase.

Lietha D, Cai X, Ceccarelli DF, Li Y, Schaller MD, Eck MJ.

Cell. 2007 Jun 15;129(6):1177-87.

21.

A new crystal form of the NK1 splice variant of HGF/SF demonstrates extensive hinge movement and suggests that the NK1 dimer originates by domain swapping.

Watanabe K, Chirgadze DY, Lietha D, de Jonge H, Blundell TL, Gherardi E.

J Mol Biol. 2002 May 31;319(2):283-8.

PMID:
12051906
22.

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