About: The value of proteasome inhibition in cancer. Can the old drug, disulfiram, have a bright new future as a novel proteasome inhibitor?     Goto   Sponge   NotDistinct   Permalink

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  • Hlavní přístup ve vývoji protinádorových léčiv zahrnuje hledání nových sloučen, účinných proti malignitám, které nejsou doposud klinicky využívány. Tato strategie je časově náročná a nákladná. Recentní studie odhalily překvapivou, ale mechanisticky konzistentní aktivitu disulfiramu (antabus), léčiva využívaného přes 50 let v léčbě alkoholismu. Disulfiram byl s úspěchem použit k potlačení jaterních metastáz pocházejících z okulárního melanomu. Farmakokinetika disulfiramu a jeho farmakologický profil v nádorových liniích získaných z pacientů jsou dobře známy. Disulfiram je běžně dostupná a levná sloučenina, jejíž vedlejší účinky jsou zanedbatelné ve srovnání s klasickými cytostatiky. Navíc inhibiční účinnost disulfiramu proti proteasomu je v souladu se současnou protinádorovou strategií a představuje nový, slibný přístup k inhibici proteasomu. (cs)
  • The major approach to the development of anticancer drugs involves searching for new compounds, efficient against malignancies, which are not, as yet, used clinically. This strategy is time-consuming and expensive. Recent studies have disclosed a surprising, but mechanistically consistent, anticancer activity of disulfiram (antabuse), a drug used for about 50 years in the treatment of alcoholism. Disulfiram has been successfully used to suppress hepatic metastases originating from ocular melanoma. The pharmacokinetics of disulfiram and its pharmacological profile in cancer cell lines and in cancer cells obtained from patients is well known. Disulfiram is a readily available and inexpensive substance whose adverse effects are negligible, compared to classical cancerostatics. In addition, the inhibitory potency of disulfiram against the proteasome conforms to current anticancer strategies and represents a new, promising approach to proteasome inhibition.
  • The major approach to the development of anticancer drugs involves searching for new compounds, efficient against malignancies, which are not, as yet, used clinically. This strategy is time-consuming and expensive. Recent studies have disclosed a surprising, but mechanistically consistent, anticancer activity of disulfiram (antabuse), a drug used for about 50 years in the treatment of alcoholism. Disulfiram has been successfully used to suppress hepatic metastases originating from ocular melanoma. The pharmacokinetics of disulfiram and its pharmacological profile in cancer cell lines and in cancer cells obtained from patients is well known. Disulfiram is a readily available and inexpensive substance whose adverse effects are negligible, compared to classical cancerostatics. In addition, the inhibitory potency of disulfiram against the proteasome conforms to current anticancer strategies and represents a new, promising approach to proteasome inhibition. (en)
Title
  • The value of proteasome inhibition in cancer. Can the old drug, disulfiram, have a bright new future as a novel proteasome inhibitor?
  • Význam inhibice proteasomu v rakovině: Může staré léčivo, disulfiram, mít zářivou novou budoucnost jako nový inhibitor proteasomu? (cs)
  • The value of proteasome inhibition in cancer. Can the old drug, disulfiram, have a bright new future as a novel proteasome inhibitor? (en)
skos:prefLabel
  • The value of proteasome inhibition in cancer. Can the old drug, disulfiram, have a bright new future as a novel proteasome inhibitor?
  • Význam inhibice proteasomu v rakovině: Může staré léčivo, disulfiram, mít zářivou novou budoucnost jako nový inhibitor proteasomu? (cs)
  • The value of proteasome inhibition in cancer. Can the old drug, disulfiram, have a bright new future as a novel proteasome inhibitor? (en)
skos:notation
  • RIV/61989592:15310/08:00005338!RIV09-MSM-15310___
http://linked.open...avai/riv/aktivita
http://linked.open...avai/riv/aktivity
  • P(GP303/08/P137), Z(MSM6198959216)
http://linked.open...iv/cisloPeriodika
  • 15-16
http://linked.open...vai/riv/dodaniDat
http://linked.open...aciTvurceVysledku
http://linked.open.../riv/druhVysledku
http://linked.open...iv/duvernostUdaju
http://linked.open...titaPredkladatele
http://linked.open...dnocenehoVysledku
  • 402247
http://linked.open...ai/riv/idVysledku
  • RIV/61989592:15310/08:00005338
http://linked.open...riv/jazykVysledku
http://linked.open.../riv/klicovaSlova
  • Proteasome; nuclear factor-kappaB; disulfiram; bortezomib; cancer (en)
http://linked.open.../riv/klicoveSlovo
http://linked.open...odStatuVydavatele
  • GB - Spojené království Velké Británie a Severního Irska
http://linked.open...ontrolniKodProRIV
  • [6FDF7BA15C48]
http://linked.open...i/riv/nazevZdroje
  • Drug Discovery Today
http://linked.open...in/vavai/riv/obor
http://linked.open...ichTvurcuVysledku
http://linked.open...cetTvurcuVysledku
http://linked.open...vavai/riv/projekt
http://linked.open...UplatneniVysledku
http://linked.open...v/svazekPeriodika
  • 13
http://linked.open...iv/tvurceVysledku
  • Cvek, Boris
  • Dvořák, Zdeněk
http://linked.open...n/vavai/riv/zamer
issn
  • 1359-6446
number of pages
http://localhost/t...ganizacniJednotka
  • 15310
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