Category: Cancer

SBI-581 is An Orally Active Serine-Threonine Kinase TAO3 Inhibitor

TAO3 is a STE20-like kinase of the GCK subfamily. Specifically, TAO3 is overexpressed in many human cancers. Besides, it regulates the formation of invasive pseudopodia in melanoma, breast cancer, and bladder cancer. Both TAO3 and CBK1 are components of the RAM signal network, which regulate cell separation and polarization...

CQ211 is a Potent and Selective RIOK2 Inhibitor

RIOK2 is a typical kinase implicated in multiple human cancers. The right open reading frame (RIO) kinases belong to the atypical kinases family. RIO kinases contain a C-terminal RIO domain that is structurally homologous to typical protein kinases. However, RIOKs lack the key motifs which can convert the enzyme from...

Rebeccamycin, an Antitumor Antibiotic, Inhibits DNA Topoisomerase I

Rebeccamycin, a yellow crystalline product, is isolated from the mycelium. It has activity against P388 leukemia, L1210 leukemia, and B16 melanoma implanted in mice. Rebeccamycin is also an antitumor antibiotic produced by the actinomycete Saccharotrix aerocolonigenes with activity against several human tumor cell lines, including A549 (lung adenocarcinoma), HCT-116...

DS17701585 is a Highly Selective, Orally Active EP300 and CBP Inhibitor

DS17701585 (Compound 11) is a highly selective, orally active EP300 and CBP inhibitor with IC50 values of 0.15, 0.040, 0.45 and 0.70 µM against CBP, EP300, H3K27 and SOX2. Besides, DS17701585 has the potential for the research of cancer. EP300 and its paralog CBP play an important role in post-translational modification as...

Actinomycin D Inhibits DNA Repair and Induces Autophagy

Actinomycin D is isolated from Streptomyces species, containing a phenoxazine chromophore and two cyclic pentapeptide lactone rings. Besides, Actinomycin D can inhibit DNA repair, DNA-directed RNA synthesis, or DNA synthesis via binding to double-stranded DNA and the phenoxazine chromophore inserting DNA bases. Therefore, it acts as a DNA intercalator and...

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...