Category Archives: Tumor Suppressor Genes

Ubiquitin specific protease 7 – a good target for cancer therapy

Ubiquitin specific protease 7 (USP7) is a deubiquitinase, an enzyme that removes ubiquitin a 76 amino acid protein that is added onto lysines in the target protein. Proteins that are mono, or poly (up to 10 residues), ubiquitinated are taken to the proteasome for destruction. Continue reading

CLEC12A – a novel target for AML and MDS

CLEC12 (C-Type Lectin Domain Family 12 Member A) is negative regulator of granulocyte and monocyte functioning. It is a member of the C-type lectin/C-type lectin-like domain (CTL/CTLD) superfamily. It is also known as Myeloid Inhibitory C-Type Lectin-Like Receptor and Dendritic Cell-Associated Lectin. CLEC12 is a cell surface receptor that modulates signaling cascades and mediates tyrosine phosphorylation of target MAP kinases. Continue reading

MDM2 and MDMX inhibitor restores p53 functioning in cancers with wild-type p53

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

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

Inhibition of Nuclear Export Protein XPO1 in Cancer

Selinexor (KPT-33) is a drug that inhibits exportin 1 (XPO1 and CRM1), a nuclear transport protein that shuttles nuclear proteins through the nuclear pore and is responsible for the removal of proteins from the nucleus: Continue reading

PD-L1 Inhibitor, avelumab, approved for Merkel cell carcinoma

Avelumab (Bavencio) is a PD-L1 inhibitor that was approved for the treatment of patients with metastatic Merkel cell carcinoma (MCC). Continue reading

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

The Roles of P53, BRCA1, and PTEN in Hereditary Cancers – Lauren Fitzgerald, Contributor

Cancer results from accumulated mutations in the cancer cell’s genome. These mutations can occur spontaneously in any cell throughout an individual’s lifetime, often increasing with age or exposure to carcinogenic or mutagenic compounds. These are called somatic mutations that do not exist in every cell, and cannot be passed along from one generation to the next. However, in approximately 5 to 10% of all cancer cases, mutations are passed along through the germ line and can predispose an individual to various types of cancers. 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

Biomarkers for Wnt activation Predict For HER-2(-) Breast Cancer and NSCLC Response to Vantictumab

OncoMed is developing several compounds that target Wnt and Notch pathways, which are important in cancer and cancer stem cell maintenance, survival, and proliferation. Biomarkers for response of Her-2-negative breast cancer and non-small cell lung cancer (NSCLC) following treatment with Vantictumab, anti-Wnt monoclonal antibody, have been developed. Continue reading