SLLN-15 Activates Autophagy in Triple-Negative Breast Cancer (TNBC)
As more active compounds found in Triple-negative breast cancer (TNBC), this kind of malignant tumor has received more and more attention. Our previous article “IITZ-01 as a Potent Lysosomotropic Autophagy Inhibitor” described the good efficacy of IITZ-01 in TNBC. Today, I would like to introduce another novel small molecule...
TD-428 is a Highly Specific BRD4 Degrader
Immunomodulatory drugs (IMiDs), including Thalidomide and its analogues, which possess pleiotropic anti-myeloma properties. These properties include immune-modulation, anti-angiogenic, anti-inflammatory and anti-proliferative effects. Thalidomide is an immunomodulatory drug, which is used mainly in the treatment of multiple myeloma. The proliferation of clonal plasma cells causes multiple myeloma. Multiple myeloma leads...
TAK-981, an Inhibitor For SUMOylation Enzymatic Cascade with Antineoplastic Activities
Recently, National Cancer Institute has reported a novel inhibitor TAK-981 for SUMOylation enzymatic cascade. This inhibitor showed potential immune-activating and antineoplastic activities. Firstly, TAK-981 targets and covalently binds to the small ubiquitin-like modifier (SUMO; small ubiquitin-related modifier) protein, forming an adduct with SUMO. This binding blocks the transfer of...
NRX-252262, an Enhancer of β-catenin:β-TrCP Interaction
To develop small molecules that modulate protein-protein interactions (PPIs) displays a significant therapeutic potential. However, rational design of small molecule enhancers of PPIs remains elusive. A study from Kyle R. Simonetta, et al. reported the potent small molecules that enhance the interaction between an oncogenic transcription factor, β-Catenin, and...
Borussertib, a Covalent-Allosteric Akt Inhibitor
Protein kinases inhibition is a common therapeutic strategy for many diseases, including cancers, inflammatory diseases, diabetes and neurodegenerative disorders. The Ser-/Thr-specific kinase Akt is also known as protein kinase B. It plays a key role in PKBPI3K/Akt/mTOR-pathway. Alterations and disorders in the PI3K/Akt signaling pathway relate to different types...
Y06137 is a Selective BET Inhibitor for Treatment of CRPC
Prostate cancer arises as an androgen driven disease. Therefore the mainstay of systemic therapy for patients with advanced disease is androgen deprivation therapy. Despite of significant responses, nearly all patients ultimately progress and castration resistance ensues. Castration resistant prostate cancer therefore represents a stage in the continuum of the...
BTR-1 Induces Cell Growth Inhibition Followed by Apoptosis
Leukemia is a kind of blood cancer, begins in the bone marrow and results in abnormal blood cells. It severely affects the patients. The need for more drugs with fewer side effects is increasing. Researchers synthesize a series of compounds to examine their biological activities. As a result, BTR-1...