1450752-97-2Relevant academic research and scientific papers
Quantitative and Comparative Profiling of Protease Substrates through a Genetically Encoded Multifunctional Photocrosslinker
He, Dan,Xie, Xiao,Yang, Fan,Zhang, Heng,Su, Haomiao,Ge, Yun,Song, Haiping,Chen, Peng R.
, p. 14521 - 14525 (2017)
A genetically encoded, multifunctional photocrosslinker was developed for quantitative and comparative proteomics. By bearing a bioorthogonal handle and a releasable linker in addition to its photoaffinity warhead, this probe enables the enrichment of transient and low-abundance prey proteins after intracellular photocrosslinking and prey–bait separation, which can be subject to stable isotope dimethyl labeling and mass spectrometry analysis. This quantitative strategy (termed isoCAPP) allowed a comparative proteomic approach to be adopted to identify the proteolytic substrates of an E. coli protease–chaperone dual machinery DegP. Two newly identified substrates were subsequently confirmed by proteolysis experiments.
Exploring the potential intracellular targets of vascular normalization based on active candidates
Shan, Yuanyuan,Wang, Jin,Si, Ru,Ma, Yuexiang,Li, Jing,Zhang, Qingqing,Lu, Wen,Zhang, Jie
, (2020/12/29)
We previously developed two candidates with potency of inducing vascular normalization, BD7 and B14. However, the definite intracellular molecular target(s) responsible for their activity remains unknown. Herein, we report the discovery and functional assessment of several multifunctional photoaffinity probes for determining the potential biological targets of active compounds. The probes bear a photoaffinity moiety and a bioorthogonal unit attached to B7 or B14 and maintained the bioactivity of the parent active molecules. Using in vitro biological assays, we preliminarily identified VEGFR-2 as a potential intracellular target for the active candidates. Our results demonstrate the utility of these multifunctional photoaffinity probes for analyzing the biological activity and subcellular localization of the intracellular target proteins of active candidates.
Preparation method and application of sorafenib photoaffinity probe molecule based on halogen intermediate
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Paragraph 0025; 0027, (2021/07/09)
The invention discloses a preparation method and application of a sorafenib photoaffinity probe molecule based on a halogen intermediate, and relates to the technical field of biological medicines. The preparation method of the sorafenib photoaffinity pro
Cortex pseudolaricis acetic acid photoaffinity probe halogen midbody and preparation method thereof
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, (2019/03/08)
The invention relates to a cortex pseudolaricis acetic acid photoaffinity probe halogen midbody and a preparation method thereof. The general formula of the chemical structure of the cortex pseudolaricis acetic acid photoaffinity probe halogen midbody is as shown in specifications. By designing a new synthetic route, the compound 6 with high yield and high purity can be obtained; and the compoundcan be used to continue reacting with other materials for the preparation of a cortex pseudolaricis acetic acid photoaffinity probe.
Pseudolaric acid photoaffinity probe carbonyl intermediate and preparation method thereof
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, (2019/04/02)
The invention relates to a pseudolaric acid photoaffinity probe carbonyl intermediate and a preparation method thereof. The chemical structural formula of the pseudolaric acid photoaffinity probe carbonyl intermediate is shown as follows. The compound 4, namely the pseudolaric acid photoaffinity probe carbonyl intermediate, can be prepared at a high yield and high purity by designing new syntheticroutes, and further, can be applied to continuing to react with other raw materials for preparing a pseudolaric acid photoaffinity probe.
Cortex pseudolaricis acetic acid photoaffinity probe and preparation method thereof
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, (2019/04/04)
The invention relates to a cortex pseudolaricis acetic acid photoaffinity probe and a preparation method thereof. A chemical structure general formula of the cortex pseudolaricis acetic acid photoaffinity probe is as follows: the formula is shown in the description, wherein a group Ac is an acetyl group. By adopting the design, a cortex pseudolaricis acetic acid group is connected to an acylaminocompound containing an alkynyl group to form a special chemical structure; the cortex pseudolaricis acetic acid photoaffinity probe can be used for capturing and identifying corresponding binding protein and specifically binding the binding protein to determine a PAB bacteriostasis target spot.
Design and synthesis of minimalist terminal alkyne-containing diazirine photo-crosslinkers and their incorporation into kinase inhibitors for cell- and tissue-based proteome profiling
Li, Zhengqiu,Hao, Piliang,Li, Lin,Tan, Chelsea Y. J.,Cheng, Xiamin,Chen, Grace Y. J.,Sze, Siu Kwan,Shen, Han-Ming,Yao, Shao Q.
, p. 8551 - 8556 (2013/09/12)
Less is more: A minimalist "clickable" photo-crosslinker (see scheme) was incorporated with numerous small-molecule kinase inhibitors. The resulting probes were used for both in vitro (cell lysates) and in situ (live cells) proteome profiling, for large-scale identification of their potential cellular kinase targets and shows improved outcomes over previous probes. Copyright
