Matches in SemOpenAlex for { <https://semopenalex.org/work/W1569067568> ?p ?o ?g. }
- W1569067568 endingPage "514" @default.
- W1569067568 startingPage "489" @default.
- W1569067568 abstract "This chapter reviews the current status and new perspectives on the chemotherapy of Chagas disease, a chronic parasitosis caused by the kinetoplastid protozoon Trypanosoma cruzi, which is responsible for the largest parasitic disease burden in the American continent. The activity and limitations of currently available drugs (the nitroheterocyclic compounds nifurtimox and benznidazole) are discussed, as well as potential alternatives, focusing on ergosterol biosynthesis inhibitors (EBIs) – the most advanced candidates for new anti-T. cruzi treatments. Such compounds block the de novo production of 24-alkyl-sterols, which are essential for parasite survival. Among EBIs, the most promising compounds are new anti-fungal triazole derivatives that inhibit the parasite's sterol C14α-demethylase (CYP51): they have curative activity in animal models of acute and chronic Chagas disease, and are active against nifurtimox- and benznidazole-resistant T. cruzi strains, even if the hosts are immunosuppressed. The CYP51 inhibitors posaconazole and ravuconazole have recently entered phase II clinical trials in chronic Chagas disease. Other EBIs with potent and specific anti-T. cruzi activity include inhibitors of squalene synthase, lanosterol synthase, 24-methenyl transferase, and squalene epoxidase, as well as compounds with dual mechanisms of action (ergosterol biosynthesis inhibition and free radical generation), but their development is less advanced. The main potential advantages of EBIs over current therapies comprise higher potency in both acute and chronic infections, selectivity and improved safety profile. If safety and efficacy of this class of compounds are confirmed in clinical trials, a new era for the specific treatment of this long-neglected disease is expected." @default.
- W1569067568 created "2016-06-24" @default.
- W1569067568 creator A5014684114 @default.
- W1569067568 date "2013-04-04" @default.
- W1569067568 modified "2023-10-16" @default.
- W1569067568 title "Ergosterol Biosynthesis for the Specific Treatment of Chagas Disease: From Basic Science to Clinical Trials" @default.
- W1569067568 cites W1503504963 @default.
- W1569067568 cites W1531569394 @default.
- W1569067568 cites W1659005916 @default.
- W1569067568 cites W1957435804 @default.
- W1569067568 cites W1963723754 @default.
- W1569067568 cites W1966622156 @default.
- W1569067568 cites W1967206933 @default.
- W1569067568 cites W1969794825 @default.
- W1569067568 cites W1970346631 @default.
- W1569067568 cites W1970541564 @default.
- W1569067568 cites W1972433289 @default.
- W1569067568 cites W1976810992 @default.
- W1569067568 cites W1978089234 @default.
- W1569067568 cites W1978362943 @default.
- W1569067568 cites W1979885599 @default.
- W1569067568 cites W1984553131 @default.
- W1569067568 cites W1985049947 @default.
- W1569067568 cites W1986371873 @default.
- W1569067568 cites W1988724861 @default.
- W1569067568 cites W1993841012 @default.
- W1569067568 cites W1997986150 @default.
- W1569067568 cites W2000625166 @default.
- W1569067568 cites W2003750493 @default.
- W1569067568 cites W2004390050 @default.
- W1569067568 cites W2009324529 @default.
- W1569067568 cites W2010786471 @default.
- W1569067568 cites W2011109931 @default.
- W1569067568 cites W2012123004 @default.
- W1569067568 cites W2012195873 @default.
- W1569067568 cites W2013276329 @default.
- W1569067568 cites W2013640088 @default.
- W1569067568 cites W2013750269 @default.
- W1569067568 cites W2013771584 @default.
- W1569067568 cites W2013930187 @default.
- W1569067568 cites W2013948036 @default.
- W1569067568 cites W2018514331 @default.
- W1569067568 cites W2018917176 @default.
- W1569067568 cites W2021217831 @default.
- W1569067568 cites W2022486379 @default.
- W1569067568 cites W2024618994 @default.
- W1569067568 cites W2026223526 @default.
- W1569067568 cites W2027786060 @default.
- W1569067568 cites W2030030689 @default.
- W1569067568 cites W2030381856 @default.
- W1569067568 cites W2031047447 @default.
- W1569067568 cites W2032388023 @default.
- W1569067568 cites W2035343560 @default.
- W1569067568 cites W2035609779 @default.
- W1569067568 cites W2036956210 @default.
- W1569067568 cites W2041375888 @default.
- W1569067568 cites W2042800847 @default.
- W1569067568 cites W2043306228 @default.
- W1569067568 cites W2045904802 @default.
- W1569067568 cites W2047713231 @default.
- W1569067568 cites W2049991241 @default.
- W1569067568 cites W2051944241 @default.
- W1569067568 cites W2054577474 @default.
- W1569067568 cites W2055309480 @default.
- W1569067568 cites W2055409139 @default.
- W1569067568 cites W2056591660 @default.
- W1569067568 cites W2059145648 @default.
- W1569067568 cites W2059554069 @default.
- W1569067568 cites W2062033942 @default.
- W1569067568 cites W2062895519 @default.
- W1569067568 cites W2063503143 @default.
- W1569067568 cites W2063692687 @default.
- W1569067568 cites W2063741522 @default.
- W1569067568 cites W2063900475 @default.
- W1569067568 cites W2064722724 @default.
- W1569067568 cites W2070464703 @default.
- W1569067568 cites W2073112650 @default.
- W1569067568 cites W2074562571 @default.
- W1569067568 cites W2078173288 @default.
- W1569067568 cites W2079841403 @default.
- W1569067568 cites W2080111338 @default.
- W1569067568 cites W2080412910 @default.
- W1569067568 cites W2081132754 @default.
- W1569067568 cites W2082722598 @default.
- W1569067568 cites W2082891862 @default.
- W1569067568 cites W2084889403 @default.
- W1569067568 cites W2086808617 @default.
- W1569067568 cites W2090025142 @default.
- W1569067568 cites W2091651330 @default.
- W1569067568 cites W2092094276 @default.
- W1569067568 cites W2092612050 @default.
- W1569067568 cites W2094489008 @default.
- W1569067568 cites W2097558240 @default.
- W1569067568 cites W2098262910 @default.
- W1569067568 cites W2099210149 @default.
- W1569067568 cites W2099871562 @default.
- W1569067568 cites W2102096286 @default.
- W1569067568 cites W2102678982 @default.