Category: Colon Cancer

SN-38 (NK012) is an Active Metabolite of the Topoisomerase I Inhibitor Irinotecan

DNA topoisomerase I (Top1) is a DNA unwinding protein and the specific target of the camptothecin class of chemotherapeutic drugs. Top1 binds supercoiled DNA, nicks a DNA strand allowing its rotation around the intact strand, and then relegates the DNA. Camptothecins bind and stabilize the Top1-DNA cleavage complexes, thus...

ML-00253764 is a Brain Penetrant Melanocortin Receptor 4 Antagonist

The involuntary weight loss that occurs as some diseases poses a serious medical problem. For example, sarcopenia, cancer cachexia, rheumatoid arthritis, and hip fractures can lead to involuntary weight loss. The melanocortin 4 receptor (MC4R) plays a key role in body weight regulation and energy homeostasis. The signaling of...

CXD101 is a Selective and Orally Active Class I HDAC Inhibitor

Aberrant expression of classical HDACs associates with a variety of malignancies, including solid and hematological tumors. HDACs have also been found broadly dysregulated in multiple myeloma (MM). In particular, the mechanisms that HDACs regulate tumorigenesis are quite diverse. HDACs induce a range of cellular and molecular effects through the...

NVS-CECR2-1 is a CECR2 BRD (non-BET Family) Inhibitor

A Bromodomain (BRD) is a protein domain of about 110 amino acids and is a “reader” of lysine acetylation. Specifically, BRDs recognize acetylated lysine residues, such as those on the N-terminal tail of histones. Besides, BRD is responsible for the transduction of signals carried by acetylated lysine residues and...

SAR-020106 is an ATP-Competitive and Selective CHK1 Inhibitor

Genotoxic antitumor drugs cause DNA damage and activate cell cycle checkpoints, which are required for DNA repair and the maintenance of genomic integrity. The transcription factor p53 is a critical checkpoint protein. As a result, in the presence of damaged DNA, p53 stabilized and activated, causes the upregulation of...

Tetrac is a Thyrointegrin Receptor Antagonist

In the angiogenesis process, integrins are members of a family of cell surface transmembrane receptors. They play a critical role particularly in blood vessel formation and the local release of vascular growth factors. Thyroid hormones such as T4 and T3 promote angiogenesis and tumor cell proliferation via integrin αvβ3...

CB-1158 is a Potent and Orally Active Arginase Inhibitor

Myeloid cells are an abundant leukocyte in many types of tumors and contribute to immune evasion. The major populations of tumor-infiltrating myeloid cells include tumor-associated macrophages (TAMs), myeloid-derived suppressor cells (MDSCs), and granulocytes. A feature common to all of these immunosuppressive cells is their expression of the enzyme arginase...