126385-72-6Relevant academic research and scientific papers
Tracking a new cell-penetrating (W/R) nonapeptide, through an enzyme-stable mass spectrometry reporter tag
Delaroche, Diane,Aussedat, Baptiste,Aubry, Soline,Chassaing, Gerard,Burlina, Fabienne,Clodic, Gilles,Bolbach, Gerard,Lavielle, Solange,Sagan, Sandrine
, p. 1932 - 1938 (2007)
We have designed a mass stable reporter (msr) tag with m/z over 500, trifluoroacetyl(α,α-diemyl)Gly-Lys(Nebiotin)-(D)Lys-Cys, for the quantification of the uptake and study of the degradation processes of cell-penetrating peptides (CPP), by matrix assisted laser desorption/ionization time-of-flight (MALDI-TOF) mass spectrometry. This tag was found stable in cell lysis conditions. Using a quantitative MALDI-TOF mass spectrometry analysis based method, an accurate tracking of a new CPP and of its degradation products could be done. (1) The new msr(W/ R) nonapeptide (H-RRWWRRWRR-NH 2) enters chinese hamster ovary (CHO) K1 cells with a kinetic reaching a steady state after 30-60 min of incubation. This plateau was stable for 4 h and decreased slowly afterward. (2) The peptide msr(W/R) nonapeptide was not cytotoxic over 48 h incubation with CHO cells. (3) After 1 h incubation, the msr(W/R) nonapeptide accumulated with a 3-fold higher concentration than the extracellularly added concentration (7.5 μM). (4) The intracellular quantification was accurate with less than 3% of the quantified peptide being potentially membrane-bound. (5) There was no leakage of the full-length CPP outside the cells. And, finally, (6) analysis of the degradation process of this new CPP suggests that the peptide did not traffick to lysosomes.
Site-Selective γ-C(sp3)?H and γ-C(sp2)?H Arylation of Free Amino Esters Promoted by a Catalytic Transient Directing Group
Lin, Hua,Wang, Chao,Bannister, Thomas D.,Kamenecka, Theodore M.
supporting information, p. 9535 - 9541 (2018/07/14)
The first selective PdII-catalysed γ-C(sp3)?H and γ-C(sp2)?H arylation of free amino esters using a commercially available catalytic transient directing group. A variety of free amino esters, including α-amino esters and β-amino esters, amino monoesters and amino bis-esters, are shown to react with a diverse range of simple aryl and heteroaryl iodide reagents.
Selective and brain-permeable polo-like kinase-2 (Plk-2) inhibitors that reduce α-synuclein phosphorylation in rat brain
Aubele, Danielle L.,Hom, Roy K.,Adler, Marc,Galemmo, Robert A.,Bowers, Simeon,Truong, Anh P.,Pan, Hu,Beroza, Paul,Neitz, R. Jeffrey,Yao, Nanhua,Lin, May,Tonn, George,Zhang, Heather,Bova, Michael P.,Ren, Zhao,Tam, Danny,Ruslim, Lany,Baker, Jeanne,Diep, Linnea,Fitzgerald, Kent,Hoffman, Jennifer,Motter, Ruth,Fauss, Donald,Tanaka, Pearl,Dappen, Michael,Jagodzinski, Jacek,Chan, Wayman,Konradi, Andrei W.,Latimer, Lee,Zhu, Yong L.,Sham, Hing L.,Anderson, John P.,Bergeron, Marcelle,Artis, Dean R.
supporting information, p. 1295 - 1313 (2013/08/23)
Polo-like kinase-2 (Plk-2) has been implicated as the dominant kinase involved in the phosphorylation of α-synuclein in Lewy bodies, which are one of the hallmarks of Parkinson's disease neuropathology. Potent, selective, brain-penetrant inhibitors of Plk
A facile synthesis of multigram quantity of ethyl 3-ethylmorpholine-3- carboxylate
Jagodzinski, Jacek J.,Aubele, Danielle L.,Quincy, David A.,Dappen, Michael S.,Latimer, Lee H.,Hom, Roy K.,Galemmo Jr., Robert A.,Konradi, Andrei W.,Sham, Hing L.
supporting information; experimental part, p. 2471 - 2472 (2011/05/16)
A five-step synthesis of ethyl 3-ethylmorpholine-3-carboxylate proceeding from readily available 2-aminobutyric acid is detailed herein.
