Elsevier Chemistry Connect China
Chemistry Advancing Health
Shanghai University | March 25, 2019 — Tsinghua University | March 28, 2019
Modern scientific research has become very interdisciplinary, and experts with different backgrounds work together to face universal challenges. One such topic is human health and a great variety of chemists are working together towards a better understanding of the underlying biological processes as well as developing better diagnostics and treatments. The Elsevier Chemistry Connect China Tour – Chemistry Advancing Health in collaboration with Shanghai University [***or Tsinghua University***] is designed to provide you with an overview and inspiration from the various contributions chemists have made to human health. The talks will cover the investigation of diseases, generation of drugs and the monitoring of human health. The program invites you to discuss and network with colleagues interested in related areas of your research to further China’s leading role in this interdisciplinary research topic.
Prof. Liang Li
University of Alberta, Canada
Prof. Li will talk about the use of Proteomics and Metabolomics to study human diseases.
Prof. Hervé Galons
Editor-in-Chief of the European Journal of Medicinal Chemistry
Prof. Galons will discuss New therapeutics to treat diseases.
Prof. Zheng Ouyang
Co-Editor-in-Chief of the International Journal of Mass Spectrometry
To talk about Miniaturization of detection systems for pre-clinical studies.
Prof Xian-En Zhang
To discuss Biosensors for clinical diagnostics. Prof. Xian-En Zhang is also a conference committee member of the Biosensors World Congress.
Prof. David Gadian
Editor of Progress in Nuclear Magnetic Resonance Spectroscopy
Prof. Gadian will talk about Magnetic resonance techniques and their applications in diseases
Prof. Lei Fu
Editor of Bioorganic Chemistry
Professor Fu will explore the possibility of human dormancy by regulating the activity of cytochrome oxidase in mitochondria through chemical means.
|9:00||Introduction & Welcome Dean|
|9:15||Introduction & Welcome Elsevier|
Prof. Liang Li - Proteomics and Metabolomics to study human diseases
Towards Near-Complete Metabolome Profiling of Biological and Clinical Systems: Analytical Method Development and Health Research Applications
Liang Li, Department of Chemistry, University of Alberta, Edmonton, Alberta, Canada
New advances in analytical technologies such as genome sequencing have made a huge impact on health science research. The arrival of rapid DNA sequencing technology has significantly raised the bar on the requirement of performing proteome and metabolome analysis, ideally reaching the complete proteome and metabolome coverage. This presentation will focus on advances in metabolomics technology and its applications in health research. Metabolomics is a relatively newcomer of the omics family for large scale characterization of molecular features of a biological system. A key step in metabolomics is to perform relative quantification of metabolomic changes among different samples. High-coverage metabolome profiling will benefit research in systems biology and disease biomarker discovery, but is currently a challenging task. To increase coverage, traditionally, multiple analytical tools and methods are used to generate a combined metabolome data set. However, this approach requires heavy investment on equipment and high analytical skills and expertise. Even with the combined results, the overall metabolome coverage is still low, particularly for quantitative metabolite analysis. In this presentation, I will discuss a simple and robust platform for in-depth metabolome analysis based on chemical isotope labeling (CIL) liquid chromatography (LC) mass spectrometry (MS). I will discuss the research strategies behind the development of the instrumental platform and standardized workflows for sample preparation, sample analysis, data processing and results analysis. I will then use several examples of applications to showcase the CIL LC-MS platform for disease biomarker discovery research as well as biological studies.
Prof. Hervé Galons - New therapeutics to treat diseases
Towards selective kinase inhibitors. Elucidation of their molecular mechanism of action
Hervé Galons, INSERM U1022, Université Paris Descartes, Paris, France and Tianjin University of Science and Technology, Tianjin, China
The development of precision medicine is giving a boost to the kinase drug discovery field. Not less than 7 kinase inhibitors were approved by the FDA in 2018, adding to the 4 which reached the market in 2017. Several of these drugs benefited from orphan drug designation.
Cyclin dependent kinase (CDKs) have recently attracted interest as 3 CDK4/CDK6 inhibitors have been approved against estrogen positive breast cancer . Most of the recently marketed drugs are selective inhibitors. We wish to present our recent results in the discovery of potent inhibitors.
Crystal structures and molecular modeling are guiding the design of new series of compounds . Their molecular targets were studied through affinity chromatography assays. The probes prepared for the identification of these molecular targets were also useful for a better understanding of the mechanism of diseases. These experiments guided us in the search of new inhibitors with distinct inhibition profiles.
Among our most recently prepared families of inhibitors, selective inhibitors of CDK7 were identified following a kinome scan against 250 kinases. CDK7 control the activity of CDK2, CDK4, CDK6 and transcription. This kinase has been identified as a biomarker in several cancers. It can therefore be considered as a promising target for precision medicine .
Unexpectedly, this series of compounds exhibited anti-angiogenic activity. Several of these compounds were even found more antiangiogenic than Sunitinib. The mechanism of the antiangiogenic activity is under investigation.
1. Sherr CJ, Beach D, Shapiro GI. Targeting CDK4 and CDK6: From Discovery to Therapy. Cancer Discovery 2016 : 6 :353-67.
2. El Hage K, Piquemal J-P, Oumata N, Meijer L, Galons H, Gresh N. A Simple Isomerization of the Purine Scaffold of a Kinase Inhibitor, Roscovitine, Affords a Four- to Seven-Fold Enhancement of Its Affinity for Four CDKs. Could This Be Traced Back to Conjugation-Induced Stiffenings/Loosenings of Rotational Barriers? ACS-Omega 2017,2: 3467-3474.
3. Li B, Ni Chonghaile T, Fan Y, Madden SF, Klinger R, O'Connor AE, Walsh L, O'Hurley G, Malaya, Joseph J, Tarrant F, Conroy E, Gaber A, Chin SF, Bardwell HA, Provenzano E, Crown J, Dubois T, Linn S, Jirstrom K, Caldas C, O'Connor DP, Gallagher. Therapeutic Rationale to Target Highly Expressed CDK7 Conferring Poor Outcomes in Triple-Negative Breast Cancer. Cancer Res. 2017; 77: 3834-3845.
Prof. Zheng Ouyang - Miniaturization of detection systems for pre-clinical
Mass Spectrometry Technologies for Point-of-Care Analysis
This presentation intends to explore the potential of mass spectrometry (MS) for clinical and point-of-care (POC) analysis. Recent development in direct sampling, ionization and the miniaturization of the MS analytical systems will be introduced. The strategy and the technical implementation for performing high-performance qualitative and quantitation analysis for point-of-care testing will be discussed. Chemical reactions have also been used online for improving the sensitivity and selectivity of the analysis. The advances in method and instrumentation for analyzing organic and biological molecules as biomarkers in biofluid and tissue samples using miniature mass spectrometry systems will be presented with a discussion on future vision of the POC MS system.
Prof Xian-En Zhang - Biosensors for clinical diagnostics
Biosensors for health diagnostics
Xian-En Zhang 张先恩, National Laboratory of Biomacromolecules, CAS Center for Excellence in Biomacromolecules, Institute of Biophysics, Chinese Academy of Sciences
Biosensors are the devices consist of biological elements and physical or chemical transducers. Since the invention of the first biosensor, i.e. the Clark enzyme electrode, biosensor technology has experienced three historical periods: introduction of various physical and chemical transducer principles, industrialization and commercialization, integration of nanotechnology, and now is entering a new stage of vigorous development. The main driving force is the implementation of the concept of One-Health. Hot topics include wearable and portable biosensing for point-of-care testing (POCT), home care, noninvasive analysis, in vivo analysis, online analysis, field test, ultra-high temporal-spatial resolution for single-cell biology. The author of this presentation will highlight the latest progress and discuss the challenges remained, as well as the growing contribution of the Chinese researches in the field.
|14:30||How digital tools can help you with your research – introduction to Reaxys|
Prof. David Gadian - Magnetic resonance techniques and their applications in diseases
Magnetic resonance techniques and their applications in disease
David Gadian, University College London
Magnetic resonance imaging (MRI) and spectroscopy (MRS) techniques have extensive applications in biomedical research and in diagnostic radiology. MRI provides anatomical images with excellent tissue contrast. It can also yield remarkable physiological and functional information, as exemplified by investigations of brain activation. MRS gives additional information about tissue biochemistry. As described in this lecture, continuing technological developments over several decades have led to an ever-increasing role for magnetic resonance techniques in the diagnosis and understanding of disease, and in the guiding and evaluation of treatment.
Prof. Lei Fu - Mitochondrial Tune-Up — Can Humans hibernate?
Mitochondrial Tune-Up — Can Humans hibernate?
We have discovered a family of compounds that reversibly change the activities of cytochrome c oxidase in mitochondria, causing periods of hypothermia. These are small molecules that have low levels of toxicity. We have also developed a simple strategy to increase the activity and bioavailability of this new class of drugs. Our protocol begins with the synthesis of drug candidates followed by “in vitro” studies of living cells and progresses to “in vivo” animal studies. Understanding the mechanism of this effect should allow us to develop a number of even more active chemicals directed specifically on particular disease states.
Reception & Networking