Abstract
How to construct protein chips and chemically labeling drug molecules without disrupting structures for HTS is still a challenging area. There are two main obstacles, one is that human multitrans membrane receptors, which are major drug targets, exhibit distinct motifs, and fold structures, and they will collapse unfold without membrane support in vitro; another one is that there still lack effective chemical labeling method for small drugs for detection. Therefore, how to acquire high detecting sensitivity for small molecules and to immobilize membrane protein receptors in native conformation with uniform direction on the chip, need to be solved for drug HTS. This paper reviews drug HTS trends in recent years, proposed a new virion-chip model and a feasible C-H activation method for CY-5 labeling drugs. It is expected to provide a good platform for future drug HTS.
Keywords: C-H activation, detecting sensitivity, human multi-trans membrane protein, native conformation, small drugs, Virion-chip.
Mini-Reviews in Medicinal Chemistry
Title:The Development of Protein Chips for High Throughput Screening (HTS) of Chemically Labeling Small Molecular Drugs
Volume: 16 Issue: 10
Author(s): Yingzhu Feng, Bochu Wang, Xinxin Chu, Yazhou Wang and Liancai Zhu
Affiliation:
Keywords: C-H activation, detecting sensitivity, human multi-trans membrane protein, native conformation, small drugs, Virion-chip.
Abstract: How to construct protein chips and chemically labeling drug molecules without disrupting structures for HTS is still a challenging area. There are two main obstacles, one is that human multitrans membrane receptors, which are major drug targets, exhibit distinct motifs, and fold structures, and they will collapse unfold without membrane support in vitro; another one is that there still lack effective chemical labeling method for small drugs for detection. Therefore, how to acquire high detecting sensitivity for small molecules and to immobilize membrane protein receptors in native conformation with uniform direction on the chip, need to be solved for drug HTS. This paper reviews drug HTS trends in recent years, proposed a new virion-chip model and a feasible C-H activation method for CY-5 labeling drugs. It is expected to provide a good platform for future drug HTS.
Export Options
About this article
Cite this article as:
Feng Yingzhu, Wang Bochu, Chu Xinxin, Wang Yazhou and Zhu Liancai, The Development of Protein Chips for High Throughput Screening (HTS) of Chemically Labeling Small Molecular Drugs, Mini-Reviews in Medicinal Chemistry 2016; 16 (10) . https://dx.doi.org/10.2174/1389557515666150511152922
DOI https://dx.doi.org/10.2174/1389557515666150511152922 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...read more
Natural Products in Drug Discovery
Natural products have always been one of the important ways of drug discovery due to their novel skeleton and diverse functional group characteristics. According to statistics, between 1981 and 2019, the FDA approved a total of 1,394 small molecule drugs for marketing, of which 930 marketed drugs originated from the ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Aryl/heteroaryl Substituted Celecoxib Derivatives as COX-2 Inhibitors: Synthesis, Anti-inflammatory Activity and Molecular Docking Studies
Medicinal Chemistry Efficacious One-pot Synthesis of 2-thiazolines and 2-oxazolines Under Solvent and Metal-Free Conditions
Current Organocatalysis Synthesis and Biological Evaluation of Some New Indolizine Derivatives as Antitumoral Agents
Letters in Drug Design & Discovery Synthesis and Biological Evaluation of New imidazo[1,2-a]pyridine Derivatives as Selective COX-2 Inhibitors
Letters in Drug Design & Discovery An Integrated Platform for Bio-Analysis and Drug Delivery
Current Pharmaceutical Biotechnology The Antitumor Effects of Britanin on Hepatocellular Carcinoma Cells and its Real-Time Evaluation by In Vivo Bioluminescence Imaging
Anti-Cancer Agents in Medicinal Chemistry Population Pharmacokinetic Evaluation of a Fully Human IgG2 Monoclonal Antibody in Patients with Inflammatory Diseases
Inflammation & Allergy - Drug Targets (Discontinued) Single Cell Proteomics: Challenge for Current Analytical Science
Current Analytical Chemistry Targeting DNA Associated Processes for Cancer Therapy by the Use of SELEX and Anti-gene Approaches - When Selection Meets Rational Design
Medicinal Chemistry Reviews - Online (Discontinued) Synthetic Lethal Interactions in Cancer Therapy
Current Cancer Drug Targets Novel 5-Methyl-2,4-Disubstitued-Oxazole Derivatives: Synthesis and Anticancer Activity
Letters in Drug Design & Discovery Potential Applications of <i>Sarcopoterium Spinosum</i> as Medicinal Plants: Overview and Future Trends
Current Traditional Medicine The Effects of Caffeine on the Cholinergic System
Mini-Reviews in Medicinal Chemistry Machine Learning Techniques and Drug Design
Current Medicinal Chemistry Emerging Role of GPR30/GPER1 in Skeletal Metabolism
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Organocatalyzed Green Synthesis of 2,3-dihydropyrazines en Route to Medicinally Privileged Novel Polyheterocyclic Systems
Current Organocatalysis Heterologous Expression and Characterization of Flavinadenine Dinucleotide Synthetase from <i>Candida famata</i> for Flavin Adenine Dinucleotide Production
Protein & Peptide Letters The Crosstalk between Tissue Engineering and Pharmaceutical Biotechnology: Recent Advances and Future Directions
Current Pharmaceutical Biotechnology Hydroxyproline Substitutions Stabilize Non-Glycosylated Drosocin Against Serum Proteases Without Challenging its Antibacterial Activity
Protein & Peptide Letters The Pros and the Cons for the Use of Silybin-Rich Oral Formulations in Treatment of Liver Damage (NAFLD in Particular)
Current Medicinal Chemistry