P53 is a tumor suppressor gene that pauses cell division to allow for repair of gene damage, and triggers apoptosis if the damage is not reparable. Loss of p53 is a critical step in the evolution of cancer. Most frequently, p53 is mutated at its DNA binding domain; since p53 is a transcription factor, a diminished ability to bind to DNA significantly disrupts its functioning. Continue reading
Tag Archives: p53
Blocking Protein-Protein Interactions in Cancer
The last twenty years has been an unprecedented time in biology – in sequencing the genome and studying the functions of proteins, as well as in unraveling signal transduction pathways, the fundamental biology of normal and diseased cells has been elucidated to a great extent. Although many druggable targets have been identified, it has largely been impossible to target protein-protein interactions (PPI) in drug development. In fact, only ONE drug that targets a PPI has been approved. Continue reading
Hyperprogression on Checkpoint Inhibition Immunotherapy
Results with checkpoint inhibitors nivolumab (PD-1, Opdivo), pembrolizumab (PD-1, Keytruda), and atezolizumab (PD-L1, Tecentriq) are impressive. Some patients have experienced incredible and prolonged responses. These drugs are truly modern medical breakthroughs.
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Ublituximab, a novel anti-CD20 Monoclonal Antibody for CLL
TG Therapeutics is developing ublituximab, and anti-CD20 monoclonal antibody for patients with CLL (Chronic Lymphocytic Leukemia). In a phase 3 study in patients with relapsed disease, the combination of ublituximab and ibrutinib (Imbruvica) was superior to ibrutinib, alone – the overall response rates were 80% and 47%, respectively. Continue reading
Melanocytes Must Regain Primitive, Early Embryologic State to Develop Melanoma
Researchers working with the zebrafish melanoma model have determined that oncogene activation and crippling of tumor suppressors genes is not sufficient to transform melanocytes into melanoma cells. It is essential that the cells re-acquire primordial characteristics, as well. Continue reading
Why do elephants have lower rates of cancer than humans?
Why elephants do not get cancer is a famous conundrum that was posed by epidemiologist Richard Peto of the University of Oxford, UK, in the 1970’s. Peto noted that, in general, there is little relationship between cancer rates and the body size or age of animals. Continue reading
Ubiquitin Proteasome System Targeting for Cancer – Nurix and Celgene
Celgene and Nurix entered into a collaboration to develop small molecule treatments for cancer that target the ubiquitin proteasome system (UPS). Continue reading
Kevetrin – p53 Inducer by Cellceutix
Thioureidobutyronitrile (Kevetrin) is an intravenous drug currently in a Phase 1 study in patients with advanced solid malignancies. It acts by promoting apoptosis in several ways: Continue reading
Reprogramming Lung Cancer to Self-Destruct Using TRAIL and CDK9 Inhibitor
CANCER RESEARCH UK scientists have found a drug combination that can trigger the self-destruct process in lung cancer cells – paving the way for new treatments, according to research that will be presented at the National Cancer Research Institute (NCRI) Cancer Conference in Liverpool next week. This process is known as apoptosis. Continue reading