183271-28-5Relevant academic research and scientific papers
Establishment of Molecular Design Strategy to Obtain Activatable Fluorescent Probes for Carboxypeptidases
Kuriki, Yugo,Kamiya, Mako,Kubo, Hidemasa,Komatsu, Toru,Ueno, Tasuku,Tachibana, Ryo,Hayashi, Kento,Hanaoka, Kenjiro,Yamashita, Suguru,Ishizawa, Takeaki,Kokudo, Norihiro,Urano, Yasuteru
, p. 1767 - 1773 (2018)
Carboxypeptidases (CPs) are a family of hydrolases that cleave one or more amino acids from the C-terminal of peptides or proteins. However, methodology to monitor the activities of CPs is poorly developed. Here, we present the first versatile design strategy to obtain activatable fluorescent probes for CPs by utilizing intramolecular spirocyclization of rhodamine to translate the aliphatic carboxamide to aliphatic carboxylate structural conversion catalyzed by CPs into dynamic fluorescence activation. Based on this novel strategy, we developed probes for carboxypeptidases A and B. One of these probes was able to detect pancreatic juice leakage in mice ex vivo, suggesting that its suitability for intraoperative diagnosis of pancreatic fistula. This design strategy should be broadly applicable to CPs, as well as other previously untargetable enzymes, enabling development of fluorescent probes to study various pathological and biological processes.
A green-light-emitting, spontaneously blinking fluorophore based on intramolecular spirocyclization for dual-colour super-resolution imaging
Uno, Shin-Nosuke,Kamiya, Mako,Morozumi, Akihiko,Urano, Yasuteru
supporting information, p. 102 - 105 (2017/12/27)
We have developed the first green-light-emitting, spontaneously blinking fluorophore (SBF), HEtetTFER. In combination with our near-infrared-light-emitting SBF (HMSiR), HEtetTFER allows dual-colour single-molecule localization microscopy (SMLM) in buffer solution without any additive and without photoactivation.
FLUORESCENT PROBE FOR DETECTING DIPEPTIDYL PEPTIDASE IV
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Paragraph 0070; 0071, (2017/09/02)
[Problem] To provide a novel fluorescent probe for dipeptidyl peptidase IV, and a detection method and a detection kit using the fluorescent probe. [Solution] A fluorescent probe for detecting dipeptidyl peptidase IV (DPP-IV), said probe comprising a compound represented by formula (I) or a salt, thereof. In formula (I): A and B are either the same or different and independently represent an amino acid residue, provided that A is bonded via an amide bond to NH in an adjacent formula and B is bonded via an amide bond to A; R1 represents hydrogen atom(s) or 1 to 4 substituents bonded to the benzene ring, said substituents being either the same or different; R2, R3, R4, R5, R6 and R7 independently represent a hydrogen atom, a hydroxyl group, an alkyl group or a halogen atom; R8 and R9 independently represent a hydrogen atom or an alkyl group; and X represents a C1-C5 alkylene group.
Rhodanol Synthons for Fluorescent Labeling and Drug Conjugates
Spassova, Maria,Kois, Pavol,Watanabe, Kyoichi
, p. S290 - S293 (2007/10/03)
The synthesis of Rhodanol derivatives 1b-1j is described.Rhodamine 123 was reduced to the corresponding alcohol and after acetylation of the amino functionalities, the protected Rhodanol was further derivatized by alkylation with oxirane, chloromethyloxirane and 2-acetoxyethoxymethylchloride.The coupling of some synthons to FU and FUrd at different conditions was studied.Synthons 1a, 1b and 1f were converted to phosphoramidites and used for 5'-labeling of oligonucleotides as a final step in solid-phase synthesis on automated DNA synthesizer.
