Category: Breast Cancer

Lapatinib is a Potent Inhibitor of the ErbB-2 and EGFR Tyrosine Kinase Domains

Growth factors and their transmembrane receptor tyrosine kinase play important roles in cell proliferation, survival, migration, and differentiation. Additionally, Epidermal growth factor (EGF)-like proteins stimulates cells to divide by activating members of the EGF receptor (EGFR) family. Many types of human tumor cells growth and development are related to the...

LTX-315 is an Oncolytic Peptide with Potent Anticancer Activity

Oncolytic peptides offer yet a new therapeutic modality. Their membranolytic mode of action includes the release of danger-associated molecular pattern molecules (DAMPs) and tumor antigens from cancer cells. Therefore, it results in regression of solid tumors and systemic tumor-specific immune responses. Consequently, the development of oncolytic peptides into novel...

Vistusertib (AZD2014) is an ATP Competitive mTOR Inhibitor

mTOR is an atypical serine threonine kinase involved in regulating major cellular functions, such as nutrients sensing, growth, and proliferation. mTOR is part of the multiprotein complexes mTORC1 and mTORC2. mTORC1 and mTORC2 have been shown to play critical yet functionally distinct roles in the regulation of cellular processes....

Epothilone B is a Microtubule Stabilizer

Microtubules are polymers of tubulin, which is one of several members of a small family of globular proteins. The tubulin superfamily includes five distinct families, the α-, β-, γ-, δ-, and ε-tubulins and a sixth family which is present only in kinetoplastid protozoa. The most common members α-tubulin and...

Splitomicin is a cell-permeable, potent SIR2 Inhibitor

The class III histone deacetylases (HDAC) are also known as the sirtuins. They are a member of the sirtuin family of proteins (SIRT1~7) and homologs of Sir2 (Sir2p) in yeast. SIRT1 shares a domain of about 275 amino acids with other sirtuins. It uses NAD+ to mediate the deacetylation...

GNE-149 is an Orally Active Estrogen Receptor α Antagonist

Estrogen receptor α (ERα) and β (ERβ) is a nuclear transcription factors involved in regulating many complex human physiological processes. Moreover, these proteins play a role in the nucleus and regulate the transcription of specific target genes by binding with relevant DNA regulatory sequences. The interaction between ligands, receptors,...