• Corpus ID: 10673654

Antitumor activity of a spicamycin derivative, KRN5500, and its active metabolite in tumor cells.

  title={Antitumor activity of a spicamycin derivative, KRN5500, and its active metabolite in tumor cells.},
  author={Masaru Kamishohara and Hiroyuki Kawai and Teruyuki Sakai and Toshiyuki Isoe and Kiyoshi Hasegawa and Junichiro Mochizuki and Takeshi Uchida and Shiro Kataoka and Hidehiko Yamaki and Takashi Tsuruo},
  journal={Oncology research},
  volume={6 8},
KRN5500, (6-[4-Deoxy-4-(2E,4E)-tetradecadienoylglycyl]amino-L-glycero - beta-L-mannoheptopyranosyl]amino-9H-purine), was semi-synthesized in an attempt to increase the therapeutic effects of spicamycin analogues. The present study evaluated the antitumor activity of KRN5500 against murine tumors and human tumor xenografts. KRN5500 prolonged the survival of P388 leukemia- and B16 melanoma-bearing mice but was marginally effective on colon adenocarcinoma 26. The antitumor activity of KRN5500 (4… 
Antiproliferative activity in vitro and in vivo of the spicamycin analogue KRN5500 with altered glycoprotein expression in vitro.
  • A. Burger, G. Kaur, E. Sausville
  • Biology, Chemistry
    Clinical cancer research : an official journal of the American Association for Cancer Research
  • 1997
These effects are consistent with a prominent early effect of SPA on the enzymatic machinery or organelles important for proper glycoprotein processing and emphasize the novelty of this agent's likely mechanism of action.
Inhibitory effect of a spicamycin derivative, KRN5500, on the growth of hepatic metastasis of human colon cancer-producing tissue polypeptide antigen
The chemotherapeutic efficacy of KRN5500 against experimental hepatic metastasis indicates that it may be a useful drug for the treatment of patients with hepatic cancers and the usefulness of TPA as a tumor marker in an experimental xenograft model is suggested.
In vitro interactions of a new derivative of spicamycin, KRN5500, and other anticancer drugs using a three-dimensional model
Purpose: KRN5500 is a new derivative of spicamycin produced by Streptomyces alanosinicus and is known to have a wide range of antitumor activities against human cancer cell lines. Because of its
Phase I and pharmacokinetic study of KRN5500, a spicamycin derivative, for patients with advanced solid tumors.
KRN5500, a structurally novel protein synthesis inhibitor, warrants further investigation to overcome these toxicity profiles and improve its efficacy.
Mechanism of action of aragusterol a (YTA0040), a potent anti‐tumor marine steroid targeting the G1 phase of the cell cycle
Findings indicated that YTA0040 arrested human NSCLC cells in late G1 phase of the cell cycle through inhibition of pRb phosphorylation.
The Novel Anticancer Drug KRN5500 Interacts with, but is Hardly Transported by, Human P‐Glycoprotein
The interaction of the novel anticancer drug KRN5500 with human Pglycoprotein (P‐gp) was analyzed from the viewpoint of cellular pharmacokinetics, and it was demonstrated that KRN 5500 interacted with, but was hardly transported via, P‐gp.
Reduction of the Side Effects of an Antitumor Agent, KRN5500, by Incorporation of the Drug into Polymeric Micelles
It is expected that KRN/m will be superior to KRN5500 for clinical use and that the methodology of polymeric micelle drug carrier systems can be applied to other water‐insoluble drugs.
A Phase I Clinical Trial of Spicamycin Derivative KRN5500 (NSC 650426) Using a Phase I Accelerated Titration “2B” Design
The spicamycin derivative KRN5500 was considered as a potential anti-cancer agent based on in vitro and preclinical studies, and clearance did not decrease significantly over the dose range 0.8–8.4 mg/m2/d × 5 days, and significant correlation was observed between plasma levels and toxicity.
KRN5500, a spicamycin derivative, exerts anti‐myeloma effects through impairing both myeloma cells and osteoclasts
The results suggest that KRN5500 exerts anti‐MM effects through impairing both MM cells and osteoclasts, which might be a useful therapeutic option in patients with MM.
KRN5500, a novel antitumor agent, induces apoptosis or cell differentiation in HL-60 cells.
It is anticipated that KRN5500 will be used clinically as an anti-leukemic agent, and its mechanism of antitumor action is to induce apoptosis or cell differentiation.