Boramino acid as a marker for amino acid transporters.
Zhibo Liu,Haojun Chen,Haojun Chen,Kai Chen,Yihan Shao,Dale O. Kiesewetter,Gang Niu,Xiaoyuan Chen +7 more
TLDR
A new class of boramino acids (BAAs) has been developed as the general marker for imaging the expression of amino acid transporters, suggesting that BAAs hold great promise for the development of new imaging probes and smart AAT-targeting drugs.Abstract:
Amino acid transporters (AATs) are a series of integral channels for uphill cellular uptake of nutrients and neurotransmitters. Abnormal expression of AATs is often associated with cancer, addiction, and multiple mental diseases. Although methods to evaluate in vivo expression of AATs would be highly useful, efforts to develop them have been hampered by a lack of appropriate tracers. We describe a new class of AA mimics-boramino acids (BAAs)-that can serve as general imaging probes for AATs. The structure of a BAA is identical to that of the corresponding natural AA, except for an exotic replacement of the carboxylate with -BF3 (-). Cellular studies demonstrate strong AAT-mediated cell uptake, and animal studies show high tumor-specific accumulation, suggesting that BAAs hold great promise for the development of new imaging probes and smart AAT-targeting drugs.read more
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A Bioorthogonal System Reveals Antitumour Immune Function of Pyroptosis
Qinyang Wang,Yupeng Wang,Jingjin Ding,Chunhong Wang,Xuehan Zhou,Wenqing Gao,Huanwei Huang,Feng Shao,Feng Shao,Zhibo Liu +9 more
TL;DR: In mouse models of cancer, a biorthogonal chemical system based on desilylation catalysed by phenylalanine trifluoroborate enables the controlled release of gasdermin to induce pyroptosis selectively in tumour cells, suggesting that pyroPTosis-induced inflammation triggers robust antitumour immunity and can synergize with checkpoint blockade.
Journal ArticleDOI
Simple bioconjugate chemistry serves great clinical advances: albumin as a versatile platform for diagnosis and precision therapy
Zhibo Liu,Xiaoyuan Chen +1 more
TL;DR: This review article summarizes the mainstream chemical strategies of developing HSA binding molecules for coupling with drug molecules, and concisely condense the recent progress of the most important clinical applications of HSA-binding platforms.
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Chemistry for Positron Emission Tomography: Recent Advances in 11 C-, 18 F-, 13 N-, and 15 O-Labeling Reactions.
TL;DR: An overview of commonly used labeling reactions through examples of clinically relevant PET tracers is provided and the most recent developments and breakthroughs over the past decade are highlighted, with a focus on 11 C, 18 F, 13 N, and 15 O.
Journal ArticleDOI
18F-Fluorination of Unactivated C-H Bonds in Branched Aliphatic Amino Acids: Direct Synthesis of Oncological Positron Emission Tomography Imaging Agents.
Matthew B. Nodwell,Hua Yang,Milena Čolović,Zheliang Yuan,Zheliang Yuan,Helen Merkens,Rainer E. Martin,Francois Benard,Paul Schaffer,Paul Schaffer,Robert Britton +10 more
TL;DR: Positron emission tomography imaging of mice bearing PC3 (prostate) or U87 (glioma) xenografts using 5-[18F]-fluorohomoleucine showed high tumor uptake and excellent tumor visualization, highlighting the utility of this strategy for rapid tracer discovery for oncology.
Journal ArticleDOI
Activating TiO2 Nanoparticles: Gallium-68 Serves as a High-Yield Photon Emitter for Cerenkov-Induced Photodynamic Therapy.
TL;DR: This study proved that Ga-68 is a more potent radionuclide for PDT than F-18 both in vitro and in vivo, and offered a promising strategy of using a diagnostic dose of radioactivity to achieve depth-independent cancer therapy without using any external light source.
References
More filters
Journal ArticleDOI
Hallmarks of cancer: the next generation.
TL;DR: Recognition of the widespread applicability of these concepts will increasingly affect the development of new means to treat human cancer.
Journal ArticleDOI
PROCHECK: a program to check the stereochemical quality of protein structures
TL;DR: The PROCHECK suite of programs as mentioned in this paper provides a detailed check on the stereochemistry of a protein structure and provides an assessment of the overall quality of the structure as compared with well refined structures of the same resolution.
Journal ArticleDOI
AutoDock4 and AutoDockTools4: Automated docking with selective receptor flexibility
Garrett M. Morris,Ruth Huey,William Lindstrom,Michel F. Sanner,Richard K. Belew,David S. Goodsell,Arthur J. Olson +6 more
TL;DR: AutoDock4 incorporates limited flexibility in the receptor and its utility in analysis of covalently bound ligands is reported, using both a grid‐based docking method and a modification of the flexible sidechain technique.
Journal ArticleDOI
CHARMM general force field: A force field for drug-like molecules compatible with the CHARMM all-atom additive biological force fields.
Kenno Vanommeslaeghe,Elizabeth Hatcher,Chayan Acharya,Sibsankar Kundu,Shijun Zhong,Jihyun Shim,Eva Darian,Olgun Guvench,Pedro E. M. Lopes,Igor Vorobyov,Alexander D. MacKerell +10 more
TL;DR: An extension of the CHARMM force field to drug‐like molecules is presented, making it possible to perform “all‐CHARMM” simulations on drug‐target interactions thereby extending the utility ofCHARMM force fields to medicinally relevant systems.
Journal ArticleDOI
SWISS-MODEL: modelling protein tertiary and quaternary structure using evolutionary information
Marco Biasini,Stefan Bienert,Andrew Waterhouse,Konstantin Arnold,Gabriel Studer,Tobias Schmidt,Florian Kiefer,Tiziano Gallo Cassarino,Martino Bertoni,Lorenza Bordoli,Torsten Schwede,Torsten Schwede +11 more
TL;DR: The latest version of the SWISS-MODEL expert system for protein structure modelling is described, which makes extensive use of model quality estimation for selection of the most suitable templates and provides estimates of the expected accuracy of the resulting models.