title: Tyropeptins, proteasome inhibitors produced by Kitasatospora sp. MK993-dF2.
abstract: Tyropeptins are new proteasome inhibitors isolated from the culture broth of Kitasatospora sp. MK993-dF2. Tyropeptins permeate cell membranes, inhibit intracellular proteasomes and reduce the degradation of ubiquitinated proteins in mammalian cells. We performed structure-based drug design and structure-activity relationship studies on tyropeptin derivatives to obtain valuable information of derivatives. Among the synthesized tyropeptin derivatives, some boronic acid derivatives exhibited potent antitumor effects against human multiple myeloma. In this review, we summarize the discovery of tyropeptins and the development of tyropeptin derivatives.
authors.affiliation: Institute of Microbial Chemistry (BIKAKEN), Shizuoka, Japan.
authors.forename: Isao
authors.initials: I
authors.lastname: Momose
authors.affiliation: Institute of Microbial Chemistry (BIKAKEN), Tokyo, Japan.
authors.forename: Takumi
authors.initials: T
authors.lastname: Watanabe
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D004151:Dipeptides / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D015195:Drug Design; D006801:Humans; D046988:Proteasome Endopeptidase Complex; D061988:Proteasome Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D013306:Streptomycetaceae / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D004151:Dipeptides; D061988:Proteasome Inhibitors; C449021:tyropeptin A; C449020:tyropeptin B; D046988:Proteasome Endopeptidase Complex