Andrew J Massey
Affiliation: Granta Park
- A novel, small molecule inhibitor of Hsc70/Hsp70 potentiates Hsp90 inhibitor induced apoptosis in HCT116 colon carcinoma cellsAndrew J Massey
Vernalis R and D Ltd, Granta Park, Cambridge, CB21 6GB, UK
Cancer Chemother Pharmacol 66:535-45. 2010....
- Context-dependent cell cycle checkpoint abrogation by a novel kinase inhibitorAndrew J Massey
Vernalis R and D Ltd, Granta Park, Cambridge, United Kingdom
PLoS ONE 5:e13123. 2010..We have identified a novel inhibitor of these kinases and utilized this molecule to probe the functional interplay between these two checkpoints...
- γH2AX and Chk1 phosphorylation as predictive pharmacodynamic biomarkers of Chk1 inhibitor-chemotherapy combination treatmentsRebecca Rawlinson
Vernalis R and D Ltd, Granta Park, Cambridge, UK CB21 6GB
BMC Cancer 14:483. 2014..Utilizing pharmacodynamic biomarkers to optimize drug dose and scheduling in these trials could greatly enhance the likelihood of clinical success...
- Inhibition of the checkpoint kinase Chk1 induces DNA damage and cell death in human Leukemia and Lymphoma cellsChristopher Bryant
Vernalis R and D Ltd, Granta Park, Cambridge CB21 6GB, UK
Mol Cancer 13:147. 2014..Recent evidence suggests that Chk1 inhibitors may demonstrate significant single agent activity in tumors with specific DNA repair defects, a constitutively activated DNA damage response or oncogene induced replicative stress...
- NVP-AUY922: a small molecule HSP90 inhibitor with potent antitumor activity in preclinical breast cancer modelsMichael Rugaard Jensen
Novartis Institutes for BioMedical Research, Oncology Research, Klybeckstrasse 141, CH 4057 Basel, Switzerland
Breast Cancer Res 10:R33. 2008..HSP90 has emerged in recent years as a promising new target for anticancer therapies...
- Adenosine-derived inhibitors of 78 kDa glucose regulated protein (Grp78) ATPase: insights into isoform selectivityAlba T Macias
Vernalis R and D Ltd, Granta Park, Great Abington, Cambridge, CB21 6GB, UK
J Med Chem 54:4034-41. 2011..X-ray crystal structures of Grp78 bound to ATP, ADPnP, and adenosine derivative 10 revealed differences in the binding site between Grp78 and homologous proteins...
- Novel adenosine-derived inhibitors of 70 kDa heat shock protein, discovered through structure-based designDouglas S Williamson
Vernalis R and D Ltd, Granta Park, Great Abington, Cambridge CB21 6GB, United Kingdom
J Med Chem 52:1510-3. 2009..Exposure of compound 12 to HCT116 cells caused significant reduction in cellular levels of Raf-1 and Her2 at concentrations similar to that which caused cell growth arrest...
- Knockdown of PAK4 or PAK1 inhibits the proliferation of mutant KRAS colon cancer cells independently of RAF/MEK/ERK and PI3K/AKT signalingHana Tabusa
Department of Oncology, Vernalis R and D Ltd, Granta Park, Cambridge, CB21 6GB, United Kingdom
Mol Cancer Res 11:109-21. 2013..These results support a role for the PAKs in the proliferation of mutant KRAS-driven colorectal carcinoma cells via pathways not involving RAF/MEK/ERK and PI3K/AKT signaling...