Sameer A. Greenall
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Impact of pembrolizumab on health outcomes and productivity in earlier-stage cancers within the US Medicare population Open
Perioperative/adjuvant pembrolizumab in earlier-stage cancers can meaningfully improve clinical outcomes for Medicare patients and reduce caregiver productivity losses. Sustained investment and access to pembrolizumab are critical to fully…
Impact on health outcomes and productive work of adding anti-PD-1 agents to treat early-stage cancers in the United Kingdom: a modelling study Open
Background Anti-PD-1 agents are recommended in adjuvant or perioperative settings in some early-stage cancers. The health and productivity benefits of anti-PD-1 use on a population level, however, are unknown. Methods A decision model was …
VHL-independent degradation of hepatitis B virus e antigen (HBeAg) by VHL-binding chimeric small molecules Open
Chimeric small molecule LH-3, designed to recruit the VHL E3 ligase, degrades HBV protein HBeAg through a largely VHL-independent mechanism. Virological assessment reveals enhanced efficacy against an inhibitor-resistant strain of the viru…
Most clinical anti-EGFR antibodies do not neutralize both wtEGFR and EGFRvIII activation in glioma Open
Background Although epidermal growth factor receptor (EGFR) and its truncated, autoactive mutant EGFR variant (v)III are bona fide drivers of tumorigenesis in some gliomas, therapeutic antibodies developed to neutralize this axis have not …
DDIS-19. CT-179: AN INHIBITOR OF THE OLIG2 TRANSCRIPTION FACTOR WITH POTENT ANTI-TUMOUR ACTIVITY IN BRAIN CANCER Open
High Grade Glioma (HGG) is incurable and has a median survival of less than 5% at five years, highlighting a desperate need for new therapeutic strategies. OLIG2 is a basic helix-loop-helix (bHLH) transcription factor that is expressed in …
Activation of ERBB4 in Glioblastoma Can Contribute to Increased Tumorigenicity and Influence Therapeutic Response Open
Glioblastoma (GBM) is often resistant to conventional and targeted therapeutics. ErbB2 Receptor Tyrosine Kinase 4 (ERBB4) is expressed throughout normal brain and is an oncogene in several pediatric brain cancers; therefore, we investigate…
Activation of ERBB4 in glioblastoma can contribute to increased tumorigenicity and influence therapeutic response Open
Glioblastoma (GBM) is often resistant to conventional and targeted therapeutics. ERBB4 is expressed throughout normal brain and is an oncogene in several pediatric brain cancers; therefore, we investigated ERBB4 as a prognostic marker and …
EAPH-16. DISCOVERY OF CT-179: A SMALL MOLECULE INHIBITOR OF THE OLIG2 TRANSCRIPTION FACTOR WITH POTENT ANTI-TUMOR IN PEDIATRIC BRAIN CANCER Open
OLIG2 is a protein transcription factor (TF) expressed exclusively in progenitor cells in the brain and spinal cord during development and is re-expressed in most adult and pediatric brain cancers. Expression of OLIG2 drives the growth, in…
View article: P08.21 Discovery of CT-179--a small molecule inhibitor of the transcription factor OLIG2 with potent anti-tumour activity in high-grade glioma
P08.21 Discovery of CT-179--a small molecule inhibitor of the transcription factor OLIG2 with potent anti-tumour activity in high-grade glioma Open
OLIG2 is a protein transcription factor that is expressed exclusively in progenitor cells in the brain and spinal cord during development. Typically, OLIG2 is not active in the adult brain and is not found outside the central nervous syste…
EXTH-17. CDK7 IS A NOVEL THERAPEUTIC TARGET IN HIGH GRADE GLIOMA Open
Cyclin dependent kinase 7 (CDK7), is a kinase that facilitates cell cycle progression and stabilises RNA polymerase II-based transcription. THZ1 is a novel irreversible inhibitor of CDK7 whose mechanism(s) of action are largely unknown. We…
Incomplete target neutralization by the anti-cancer antibody rilotumumab Open
The antibody rilotumumab, which has been tested in multiple Phase 2 and Phase 3 trials, has been reported to neutralize hepatocyte growth factor (HGF), the ligand for the oncogene MET. However, we report that rilotumumab does not prevent H…