Salinosporamide A: A Superior Proteasome Inhibitor
Significantly more potent than other commercially available proteasome inhibitors; IC50 values in the low to mid nM range. 3-log specificity for the inhibition of proteasome proteolytic activities as compared to other proteases such as chymotrypsin, trypsin, catharsis A, and catharsis B. Well-characterized mechanism of binding and action. Easily configured for sale as an individual reagent or within a kit.
Marine organisms are a rich source of natural products with unique structures and potent biological activities. UC researchers have isolated and characterized one such product, Salinosporamide A (Sal A), which was discovered as a fermentation product from the marine actinomycete Salinispora tropica. By forming an irreversible, covalent adduct with the active site threonine of the 20S subunit of the proteasome, Sal A is able to potently and selectively inhibit all catalytic functions of the proteasome and thus represents a new biochemical tool that can be used to study basic cell biology or can be used as a standard for drug discovery programs targeting proteasome inhibition.
Patent Number: US7179834B2
Application Number: US2003600854A
Inventor: Fenical, William | Jensen, Paul | Mincer, Tracy | Feling, Robert H. R.
Priority Date: 24 Jun 2002
Priority Number: US7179834B2
Application Date: 20 Jun 2003
Publication Date: 20 Feb 2007
IPC Current: A61K0031407 | A61K0031397 | A61K0031424 | A61K003143 | C07D049104 | C12P001718 | C07D0491044
US Class: 514421 | 548453
Assignee Applicant: The Regents of the University of California
Title: Salinosporamides and methods for use thereof
Usefulness: Salinosporamides and methods for use thereof
Summary: Used for inhibiting proliferation of hyperproliferative cells, for treating cell proliferative disorders, particularly neoplasms comprising mammary, small-cell lung, non-small-cell lung, colorectal, leukemia, melanoma, pancreatic adenocarcinoma, central nervous system, ovarian, prostate, sarccff of soft tissue or bone, head and neck, gastric including thyroid and non-Hodgkin's disease, stomach, myeloma, bladder, renal, neuroendocrine including thyroid and non Hodgkin's disease and Hodgkin's disease neoplasms (all claimed).
Novelty: New salinosporamide derivatives used for treating proliferative disorders e.g. neoplasms in small-cell lung and non-small cell lung
Disease Diagnostic/Treatment
Cancer/Tumor
7179834
Intellectual Property Info U.S. issued patents include 7,179,834 and 7,176,232. Foreign rights also available. The field of use of “drug discovery and therapeutics” is not available for licensing. Related Cases SD2006-203 and SD2001-022 Related Materials Additional Technologies by these Inventors Tech ID/UC Case 21336/2001-208-0 Related Cases 2001-208-0, 2006-203-1, 2006-203-2, 2001-022-1, 2001-022-2, 2001-022-3, 2001-022-4, 2001-022-5, 2001-022-6
USA
