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Darren A E Cross

Explore the profile of Darren A E Cross including associated specialties, affiliations and a list of published articles. Areas
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Articles 21
Citations 1797
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Recent Articles
11.
Hennessy E, Chuaqui C, Ashton S, Colclough N, Cross D, Debreczeni J, et al.
ACS Med Chem Lett . 2016 May; 7(5):514-9. PMID: 27190603
A novel series of covalent inhibitors of EGFR (epidermal growth factor receptor) kinase was discovered through a combination of subset screening and structure-based design. These compounds preferentially inhibit mutant forms...
12.
Eberlein C, Stetson D, Markovets A, Al-Kadhimi K, Lai Z, Fisher P, et al.
Cancer Res . 2015 Apr; 75(12):2489-500. PMID: 25870145
Resistance to targeted EGFR inhibitors is likely to develop in EGFR-mutant lung cancers. Early identification of innate or acquired resistance mechanisms to these agents is essential to direct development of...
13.
Meador C, Jin H, de Stanchina E, Nebhan C, Pirazzoli V, Wang L, et al.
Mol Cancer Ther . 2014 Dec; 14(2):542-52. PMID: 25477325
Metastatic EGFR-mutant lung cancers are sensitive to the first- and second-generation EGFR tyrosine kinase inhibitors (TKIs) gefitinib, erlotinib, and afatinib, but resistance develops. Acquired resistance to gefitinib or erlotinib occurs...
14.
Finlay M, Anderton M, Ashton S, Ballard P, Bethel P, Box M, et al.
J Med Chem . 2014 Oct; 57(20):8249-67. PMID: 25271963
Epidermal growth factor receptor (EGFR) inhibitors have been used clinically in the treatment of non-small-cell lung cancer (NSCLC) patients harboring sensitizing (or activating) mutations for a number of years. Despite...
15.
Cross D, Ashton S, Ghiorghiu S, Eberlein C, Nebhan C, Spitzler P, et al.
Cancer Discov . 2014 Jun; 4(9):1046-61. PMID: 24893891
Unlabelled: First-generation EGFR tyrosine kinase inhibitors (EGFR TKI) provide significant clinical benefit in patients with advanced EGFR-mutant (EGFRm(+)) non-small cell lung cancer (NSCLC). Patients ultimately develop disease progression, often driven...
16.
Ward R, Anderton M, Ashton S, Bethel P, Box M, Butterworth S, et al.
J Med Chem . 2013 Aug; 56(17):7025-48. PMID: 23930994
A novel series of small-molecule inhibitors has been developed to target the double mutant form of the epidermal growth factor receptor (EGFR) tyrosine kinase, which is resistant to treatment with...
17.
Delouvrie B, Al-Kadhimi K, Arnould J, Barry S, Cross D, Didelot M, et al.
Bioorg Med Chem Lett . 2012 May; 22(12):4111-6. PMID: 22575869
Potent antagonists of the integrin α(5)β(1), which are RGD mimetics built from tyrosine are described. This letter describes the optimization of in vitro potency obtained by variation of two parts...
18.
Delouvrie B, Al-Kadhimi K, Arnould J, Barry S, Cross D, Didelot M, et al.
Bioorg Med Chem Lett . 2012 May; 22(12):4117-21. PMID: 22572578
Potent antagonists of the integrin α(5)β(1), which are RGD mimetics built from tyrosine are described. This paper describes the optimization of in vitro potency obtained by variation of two parts...
19.
Roberts O, Holmes K, Muller J, Cross D, Cross M
J Cell Sci . 2010 Aug; 123(Pt 18):3189-200. PMID: 20736307
Extracellular signal-regulated kinase 5 (ERK5) is activated in response to environmental stress and growth factors. Gene ablation of Erk5 in mice is embryonically lethal as a result of disruption of...
20.
Roberts O, Holmes K, Muller J, Cross D, Cross M
Biochem Soc Trans . 2009 Nov; 37(Pt 6):1254-9. PMID: 19909257
ERK5 (extracellular-signal-regulated kinase 5), also termed BMK1 [big MAPK1 (mitogen-activated protein kinase 1)], is the most recently discovered member of the MAPK family. It is expressed in a variety of...