FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2103345862> ?p ?o ?g. }

• W2103345862 endingPage "3745" @default.
• W2103345862 startingPage "3738" @default.
• W2103345862 abstract "Trypanosoma cruzi phosphodiesterase (PDE) C (TcrPDEC), a novel and rather unusual PDE in which, unlike all other class I PDEs, the catalytic domain is localized in the middle of the polypeptide chain, is able to hydrolyze cyclic GMP (cGMP), although it prefers cyclic AMP (cAMP), and has a FYVE-type domain in its N-terminal region (S. Kunz et al., FEBS J. 272:6412-6422, 2005). TcrPDEC shows homology to the mammalian PDE4 family members. PDE4 inhibitors are currently under development for the treatment of inflammatory diseases, such as asthma, chronic pulmonary diseases, and psoriasis, and for treating depression and serving as cognitive enhancers. We therefore tested a number of compounds originally synthesized as potential PDE4 inhibitors on T. cruzi amastigote growth, and we obtained several useful hits. We then conducted homology modeling of T. cruzi PDEC and identified other compounds as potential inhibitors through virtual screening. Testing of these compounds against amastigote growth and recombinant TcrPDEC activity resulted in several potent inhibitors. The most-potent inhibitors were found to increase the cellular concentration of cAMP. Preincubation of cells in the presence of one of these compounds stimulated volume recovery after hyposmotic stress, in agreement with their TcrPDEC inhibitory activity in vitro, providing chemical validation of this target. The compounds found could be useful tools in the study of osmoregulation in T. cruzi. In addition, their further optimization could result in the development of new drugs against Chagas' disease and other trypanosomiases." @default.
• W2103345862 created "2016-06-24" @default.
• W2103345862 creator A5000785841 @default.
• W2103345862 creator A5000842323 @default.
• W2103345862 creator A5017591405 @default.
• W2103345862 creator A5031346796 @default.
• W2103345862 creator A5032790556 @default.
• W2103345862 creator A5040885428 @default.
• W2103345862 creator A5044174487 @default.
• W2103345862 creator A5083535398 @default.
• W2103345862 date "2010-09-01" @default.
• W2103345862 modified "2023-10-02" @default.
• W2103345862 title "Chemical Validation of Phosphodiesterase C as a Chemotherapeutic Target in <i>Trypanosoma cruzi</i> , the Etiological Agent of Chagas' Disease" @default.
• W2103345862 cites W1539947917 @default.
• W2103345862 cites W1592950931 @default.
• W2103345862 cites W1596929908 @default.
• W2103345862 cites W1605578858 @default.
• W2103345862 cites W1996165413 @default.
• W2103345862 cites W2010506933 @default.
• W2103345862 cites W2015242911 @default.
• W2103345862 cites W2017491649 @default.
• W2103345862 cites W2021217831 @default.
• W2103345862 cites W2034630021 @default.
• W2103345862 cites W2035292911 @default.
• W2103345862 cites W2037535298 @default.
• W2103345862 cites W2047047546 @default.
• W2103345862 cites W2048528133 @default.
• W2103345862 cites W2049600165 @default.
• W2103345862 cites W2053411402 @default.
• W2103345862 cites W2056179306 @default.
• W2103345862 cites W2056356546 @default.
• W2103345862 cites W2063073602 @default.
• W2103345862 cites W2068672372 @default.
• W2103345862 cites W2072682248 @default.
• W2103345862 cites W2072683434 @default.
• W2103345862 cites W2080062757 @default.
• W2103345862 cites W2082304925 @default.
• W2103345862 cites W2118233996 @default.
• W2103345862 cites W2119774957 @default.
• W2103345862 cites W2121929754 @default.
• W2103345862 cites W2135083301 @default.
• W2103345862 cites W2142919646 @default.
• W2103345862 cites W2156328030 @default.
• W2103345862 cites W2160375308 @default.
• W2103345862 cites W2166615477 @default.
• W2103345862 cites W2170492999 @default.
• W2103345862 cites W22857079 @default.
• W2103345862 cites W4237440937 @default.
• W2103345862 doi "https://doi.org/10.1128/aac.00313-10" @default.
• W2103345862 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/2934955" @default.
• W2103345862 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/20625148" @default.
• W2103345862 hasPublicationYear "2010" @default.
• W2103345862 type Work @default.
• W2103345862 sameAs 2103345862 @default.
• W2103345862 citedByCount "36" @default.
• W2103345862 countsByYear W21033458622012 @default.
• W2103345862 countsByYear W21033458622013 @default.
• W2103345862 countsByYear W21033458622014 @default.
• W2103345862 countsByYear W21033458622015 @default.
• W2103345862 countsByYear W21033458622016 @default.
• W2103345862 countsByYear W21033458622017 @default.
• W2103345862 countsByYear W21033458622018 @default.
• W2103345862 countsByYear W21033458622019 @default.
• W2103345862 countsByYear W21033458622020 @default.
• W2103345862 countsByYear W21033458622021 @default.
• W2103345862 countsByYear W21033458622022 @default.
• W2103345862 countsByYear W21033458622023 @default.
• W2103345862 crossrefType "journal-article" @default.
• W2103345862 hasAuthorship W2103345862A5000785841 @default.
• W2103345862 hasAuthorship W2103345862A5000842323 @default.
• W2103345862 hasAuthorship W2103345862A5017591405 @default.
• W2103345862 hasAuthorship W2103345862A5031346796 @default.
• W2103345862 hasAuthorship W2103345862A5032790556 @default.
• W2103345862 hasAuthorship W2103345862A5040885428 @default.
• W2103345862 hasAuthorship W2103345862A5044174487 @default.
• W2103345862 hasAuthorship W2103345862A5083535398 @default.
• W2103345862 hasBestOaLocation W21033458622 @default.
• W2103345862 hasConcept C112418997 @default.
• W2103345862 hasConcept C136764020 @default.
• W2103345862 hasConcept C150903083 @default.
• W2103345862 hasConcept C181199279 @default.
• W2103345862 hasConcept C203014093 @default.
• W2103345862 hasConcept C207001950 @default.
• W2103345862 hasConcept C2777625466 @default.
• W2103345862 hasConcept C2781092759 @default.
• W2103345862 hasConcept C41008148 @default.
• W2103345862 hasConcept C55493867 @default.
• W2103345862 hasConcept C62826618 @default.
• W2103345862 hasConcept C71928629 @default.
• W2103345862 hasConcept C86803240 @default.
• W2103345862 hasConcept C98274493 @default.
• W2103345862 hasConcept C98319499 @default.
• W2103345862 hasConceptScore W2103345862C112418997 @default.
• W2103345862 hasConceptScore W2103345862C136764020 @default.
• W2103345862 hasConceptScore W2103345862C150903083 @default.
• W2103345862 hasConceptScore W2103345862C181199279 @default.
• W2103345862 hasConceptScore W2103345862C203014093 @default.
• W2103345862 hasConceptScore W2103345862C207001950 @default.

• next