XZ739 is a PROTAC BCL-XL Degrader
PROTAC is an emerging therapeutic modality. PROTAC is a feasible solution to reduce platelet toxicity associated with BCL-XL inhibition. BCL-XL plays a key role in tumorigenesis and cancer chemotherapy resistance.…
PROTAC is an emerging therapeutic modality. PROTAC is a feasible solution to reduce platelet toxicity associated with BCL-XL inhibition. BCL-XL plays a key role in tumorigenesis and cancer chemotherapy resistance.…
In this article, we will introduce a potent, selective, and well-tolerated eIF4A inhibitor, Zotatifin. It promotes eIF4A binding to specific mRNA sequences with recognition motifs in the 5’-UTRs (IC50=2 nM). Zotatifin…
Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase. ALK is an attractive target for cancer therapies not only for its prominent role in a number of malignancies but also…
Mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALT1), a positive regulator of NF-κB, is amongst the top highly induced genes. In lymphocytes, MALT1 regulates NF-κB signaling through a scaffold function…
Protein arginine methyltransferases are a class of enzymes. They transfer a methyl group from the cofactor S-adenosylmethionine (SAM) onto the arginine omega nitrogens of substrate proteins, including histones. There are three…
Research from Jeffrey R. Jackson, et al. discovered and identified an indolocarbazole inhibitor of human checkpoint Kinase (Chk1) SB-218078. SB-218078 is an ATP Competitive and Reversible Chk1 Inhibitor The regulation…
Protein phosphorylation plays a fundamental role in the regulation of a variety of cellular processes. Casein kinase I (CK1) is a cyclic nucleotide independent kinase. It is highly purified from…
Interleukin-1 receptor-associated kinase 4 (IRAK4) is the most upstream kinase in Toll/Interleukin-1 receptor (TIR) signaling. Toll-like receptor (TLR) and interleukin-1 receptor (IL-1R) signaling in a variety of myeloid and lymphoid…
As we have written in the article “SD-36 is a Selective PROTAC STAT3 Degrader”, proteolysis targeting chimera (PROTAC) technology has been a type of therapeutics that induces targeted protein degradation.…
Proteolysis targeting chimera (PROTAC) technology has been a type of therapeutics that induces targeted protein degradation. Signal transducer and activator of transcription 3 (STAT3) is an attractive cancer therapeutic target.…