Matches in SemOpenAlex for { <https://semopenalex.org/work/W4220791824> ?p ?o ?g. }
- W4220791824 endingPage "324" @default.
- W4220791824 startingPage "324" @default.
- W4220791824 abstract "The degree of acetylation of lysine residues on histones influences the accessibility of DNA and, furthermore, the gene expression. Histone deacetylases (HDACs) are overexpressed in various tumour diseases, resulting in the interest in HDAC inhibitors for cancer therapy. The aim of this work is the development of a novel 18F-labelled HDAC1/2-specific inhibitor with a benzamide-based zinc-binding group to visualize these enzymes in brain tumours by positron emission tomography (PET). BA3, exhibiting high inhibitory potency for HDAC1 (IC50 = 4.8 nM) and HDAC2 (IC50 = 39.9 nM), and specificity towards HDAC3 and HDAC6 (specificity ratios >230 and >2080, respectively), was selected for radiofluorination. The two-step one-pot radiosynthesis of [18F]BA3 was performed in a TRACERlab FX2 N radiosynthesizer by a nucleophilic aliphatic substitution reaction. The automated radiosynthesis of [18F]BA3 resulted in a radiochemical yield of 1%, a radiochemical purity of >96% and a molar activity between 21 and 51 GBq/µmol (n = 5, EOS). For the characterization of BA3, in vitro and in vivo experiments were carried out. The results of these pharmacological and pharmacokinetic studies indicate a suitable inhibitory potency of BA3, whereas the applicability for non-invasive imaging of HDAC1/2 by PET requires further optimization of the properties of this compound." @default.
- W4220791824 created "2022-04-03" @default.
- W4220791824 creator A5027484175 @default.
- W4220791824 creator A5036623198 @default.
- W4220791824 creator A5042184078 @default.
- W4220791824 creator A5044976489 @default.
- W4220791824 creator A5048484340 @default.
- W4220791824 creator A5053568782 @default.
- W4220791824 creator A5056823141 @default.
- W4220791824 creator A5060834713 @default.
- W4220791824 creator A5063251608 @default.
- W4220791824 creator A5063563499 @default.
- W4220791824 creator A5065455817 @default.
- W4220791824 creator A5073720321 @default.
- W4220791824 creator A5084398220 @default.
- W4220791824 date "2022-03-08" @default.
- W4220791824 modified "2023-10-14" @default.
- W4220791824 title "Development and Biological Evaluation of the First Highly Potent and Specific Benzamide-Based Radiotracer [18F]BA3 for Imaging of Histone Deacetylases 1 and 2 in Brain" @default.
- W4220791824 cites W190758130 @default.
- W4220791824 cites W1964951942 @default.
- W4220791824 cites W1972100007 @default.
- W4220791824 cites W1973522169 @default.
- W4220791824 cites W1974209136 @default.
- W4220791824 cites W1978205433 @default.
- W4220791824 cites W1979743501 @default.
- W4220791824 cites W1982555880 @default.
- W4220791824 cites W1982900240 @default.
- W4220791824 cites W1985515161 @default.
- W4220791824 cites W1986312407 @default.
- W4220791824 cites W1991080755 @default.
- W4220791824 cites W1993915316 @default.
- W4220791824 cites W1997154923 @default.
- W4220791824 cites W1997842655 @default.
- W4220791824 cites W1998106408 @default.
- W4220791824 cites W1998635761 @default.
- W4220791824 cites W2003241187 @default.
- W4220791824 cites W2021098795 @default.
- W4220791824 cites W2028391746 @default.
- W4220791824 cites W2029148944 @default.
- W4220791824 cites W2034580095 @default.
- W4220791824 cites W2035491907 @default.
- W4220791824 cites W2036407435 @default.
- W4220791824 cites W2042828682 @default.
- W4220791824 cites W2046392396 @default.
- W4220791824 cites W2048709650 @default.
- W4220791824 cites W2053611887 @default.
- W4220791824 cites W2086165696 @default.
- W4220791824 cites W2087966689 @default.
- W4220791824 cites W2090601659 @default.
- W4220791824 cites W2102650381 @default.
- W4220791824 cites W2103312948 @default.
- W4220791824 cites W2113056756 @default.
- W4220791824 cites W2115593774 @default.
- W4220791824 cites W2132682917 @default.
- W4220791824 cites W2144135270 @default.
- W4220791824 cites W2179490146 @default.
- W4220791824 cites W2314360077 @default.
- W4220791824 cites W2320936212 @default.
- W4220791824 cites W2326942426 @default.
- W4220791824 cites W2346639870 @default.
- W4220791824 cites W2472055225 @default.
- W4220791824 cites W2499381514 @default.
- W4220791824 cites W2576290078 @default.
- W4220791824 cites W2597244427 @default.
- W4220791824 cites W2603495945 @default.
- W4220791824 cites W2617506851 @default.
- W4220791824 cites W2791835482 @default.
- W4220791824 cites W2793811432 @default.
- W4220791824 cites W2795615449 @default.
- W4220791824 cites W2883108221 @default.
- W4220791824 cites W2888266882 @default.
- W4220791824 cites W3017483406 @default.
- W4220791824 cites W3022192612 @default.
- W4220791824 cites W3037025246 @default.
- W4220791824 cites W3039236515 @default.
- W4220791824 cites W3090676142 @default.
- W4220791824 cites W3097736767 @default.
- W4220791824 cites W3126559718 @default.
- W4220791824 cites W3131621610 @default.
- W4220791824 cites W3133864028 @default.
- W4220791824 cites W3138950546 @default.
- W4220791824 cites W3151024962 @default.
- W4220791824 cites W3202946278 @default.
- W4220791824 cites W4206962742 @default.
- W4220791824 cites W1861608330 @default.
- W4220791824 cites W2286694297 @default.
- W4220791824 doi "https://doi.org/10.3390/ph15030324" @default.
- W4220791824 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/35337122" @default.
- W4220791824 hasPublicationYear "2022" @default.
- W4220791824 type Work @default.
- W4220791824 citedByCount "0" @default.
- W4220791824 crossrefType "journal-article" @default.
- W4220791824 hasAuthorship W4220791824A5027484175 @default.
- W4220791824 hasAuthorship W4220791824A5036623198 @default.
- W4220791824 hasAuthorship W4220791824A5042184078 @default.
- W4220791824 hasAuthorship W4220791824A5044976489 @default.
- W4220791824 hasAuthorship W4220791824A5048484340 @default.
- W4220791824 hasAuthorship W4220791824A5053568782 @default.