• Publications
  • Influence
Identification of Ras farnesyltransferase inhibitors by microbial screening.
TLDR
Kinetic analyses of the inhibition suggest that UCF1-C shows significant activity to inhibit the growth of Ki-ras-transformed fibrosarcoma, raising the possibility of its use as an antitumor drug.
Calphostins (UCN-1028), novel and specific inhibitors of protein kinase C. I. Fermentation, isolation, physico-chemical properties and biological activities.
TLDR
A novel complex of calphostin (UCN-1028), which specifically inhibits protein kinase C (PKC) has been isolated from the culture broth of a fungi Cladosporium cladosporioides, showing cytotoxic activities against various tumor cells.
Potent and Specific Inhibitors of Protein Kinase C of Microbial Origin
Potent and specific inhibitors of protein kinase C have been found in streptomyces and fungi: Staurosporine, an alkaloid from Streptomyces sp., is the most potent inhibitor of protein kinases with an
Chemical biology of natural indolocarbazole products: 30 years since the discovery of staurosporine
TLDR
Staurosporine was discovered at the Kitasato Institute in 1977 while screening for microbial alkaloids using chemical detection methods and was shown to be nanomolar inhibitors of protein kinases in 1986, viewed as forerunners of today’s crop of novel anticancer drugs.
Inhibition of protein kinase C by calphostin C is light-dependent.
Interaction of radicicol with members of the heat shock protein 90 family of molecular chaperones.
TLDR
The radicicol-binding site appears to be specific to and is conserved in all members of the Hsp90 family of molecular chaperones from bacteria to mammals, but is not present in other molecular chapers with nucleotide-binding domains.
Targeting AMAP1 and cortactin binding bearing an atypical src homology 3/proline interface for prevention of breast cancer invasion and metastasis.
TLDR
It is proposed that the AMAP1/cortactin complex, which is not detected in normal mammary epithelial cells, is an excellent drug target for cancer therapeutics.
Staurosporine inhibits tyrosine-specific protein kinase activity of Rous sarcoma virus transforming protein p60.
TLDR
The novel closure structure takes advantage of the vacuum force in the container to maintain a gas-proof, hermetic seal, reduces the thickness required of the closure to maintain the hermetic Seal and is easier to assemble in an air evacuated container.
...
...