Delanzomib

**Semantic type:** Pharmacologic Substance

**Definition:** An orally bioavailable synthetic P2 threonine boronic acid inhibitor of the chymotrypsin-like activity of the proteasome, with potential antineoplastic activity. Delanzomib represses the proteasomal degradation of a variety of proteins, including inhibitory kappaBalpha (IkappaBalpha), resulting in the cytoplasmic sequestration of the transcription factor NF-kappaB; inhibition of NF-kappaB nuclear translocation and transcriptional up-regulation of a variety of cell growth-promoting factors; and apoptotic cell death in susceptible tumor cell populations. In vitro studies indicate that this agent exhibits a favorable cytotoxicity profile toward normal human epithelial cells, bone marrow progenitors, and bone marrow-derived stromal cells relative to the proteasome inhibitor bortezomib. The intracellular protein IkappaBalpha functions as a primary inhibitor of the proinflammatory transcription factor NF-kappaB.

**Synonyms:** - ((1R)-1-((2S,3R)-3-hydroxy-2-(6-phenylpyridine-2-carboxamido)butanamido)-3-methylbutyl)boronic Acid - CEP 18770 - CEP-18770 - CT-47098 - DELANZOMIB - NPH-007098 - NPH007098 - Proteasome Inhibitor CEP 18770