326923-35-7Relevant academic research and scientific papers
STEPWISE ASSEMBLED CAPTURE COMPOUNDS COMPRISING A CLEAVABLE FUNCTION AND METHOD FOR ISOLATING AND/OR CHARACTERIZING BIOMOLECULES OR BIOMOLECULE FRAGMENTS, IN PARTICULAR PROTEINS OR PROTEIN FRAGMENTS, OF COMPLEX MIXTURES
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Paragraph 0437-0438, (2016/12/22)
The invention relates to a process for isolating and/or characterising biomolecules and/or biomolecule fragments, in particular proteins and/or protein fragments, comprising the steps: provision of an immobilized compound IC through the interaction of a c
A trifluoromethylphenyl diazirine-based SecinH3 photoaffinity probe
Albertoni, Barbara,Hannam, Jeffrey S.,Ackermann, Damian,Schmitz, Anton,Famulok, Michael
supporting information; experimental part, p. 1272 - 1274 (2012/02/15)
The synthesis of a trifluoromethylphenyl diazirine photoaffinity probe of the cytohesin inhibitor SecinH3 is described. The probe exhibits improved labelling efficiency over a benzophenone-based probe and thus is more suitable for photoaffinity labelling
A diazirine-based photoaffinity etoposide probe for labeling topoisomerase II
Chee, Gaik-Lean,Yalowich, Jack C.,Bodner, Andrew,Wu, Xing,Hasinoff, Brian B.
experimental part, p. 830 - 838 (2010/05/02)
Etoposide is a widely used anticancer drug that targets topoisomerase II, an essential nuclear enzyme. However, despite the fact that it has been in use and studied for more than 30 years the specific site on the enzyme to which it binds is unknown. In or
Convenient synthesis of a [1-14C]diazirinylbenzoic acid as a photoaffinity label for binding studies of V-ATPase inhibitors
Bender, Tobias,Huss, Markus,Wieczorek, Helmut,Grond, Stephanie,Von Zezschwitz, Paultheo
, p. 3870 - 3878 (2008/02/13)
Diazirine-tagged systems are considered reliable compounds for photoaffinity labeling (PAL) in biochemical studies as they enable investigation and understanding of biological mechanisms through covalent bonding to the target and subsequent detection. 14C-labeled 4-(3-trifluoromethyl-3H- diazirin-3-yl)benzoic acid (11) was prepared by a lithium-bromide exchange on the bis-silylated 4-bromophenyldiaziridine 19 with subsequent transformations with electrophiles as key steps of the synthesis. Using 14CO 2, which was generated from rather inexpensive Ba14CO 3, the desired diaziridinylbenzoic acid 21 was obtained in 78% yield based on the employed radioactive material. Oxidation under mild conditions then yielded diazirine 11 in a 100 mg scale. This versatile photoaffinity label was selectively attached to the tetrahydropyrane ring of bafilomycin A1 (2) and concanamycin A-derived 3, which both specifically inhibit the V-ATPases. Inhibition assays were performed and revealed that the inhibitory capacities of the labeled derivatives are suitable for PAL studies on this important group of enzymes to elucidate the as yet unknown binding sites. Wiley-VCH Verlag GmbH & Co. KGaA, 2007.
Synthesis of a tetronic acid library focused on inhibitors of tyrosine and dual-specificity protein phosphatases and its evaluation regarding VHR and Cdc25B inhibition
Sodeoka,Sampe,Kojima,Baba,Usui,Ueda,Osada
, p. 3216 - 3222 (2007/10/03)
Selective inhibitors of protein tyrosine phosphatases (PTPs) and dual-specificity phosphatases (DSPs) are expected to be useful tools for clarifying the biological functions of the PTPs themselves and also to be candidates for novel therapeutics. We planned a library approach for the identification of PTP/DSP inhibitors in which 3-acyltetronic acid is used as a "core" phosphate mimic. A series of novel tetronic acid derivatives were synthesized and evaluated as inhibitors of the dual-specificity protein phosphatases VHR and cdc25B. Several compounds are found to be potent inhibitors of cdc25B, which is a key enzyme for cell-cycle progression. The promising results described herein strongly indicated that this tetronic acid library is potent as a library focused on the PTP/DSP-selective inhibitor.
