scholarly journals Development of a Method for Quantification of Drugs in Biological Tissue Sections by Imaging Mass Spectrometry and Application of Imaging Mass Spectrometry to Drug Discovery Research

2015 ◽  
Vol 63 (6) ◽  
pp. 139-144
Author(s):  
Yukari TANAKA
Keyword(s):  
Mass Spectrometry ◽  
Drug Discovery ◽  
Biological Tissue ◽  
Imaging Mass Spectrometry ◽  
Tissue Sections ◽  
Discovery Research ◽  
Drug Discovery Research

Mass Spectrometry (MS/MS) and Proteomics: A High-Performance Bioanalytical Technique for The Peptide Drug Discovery

2020 ◽  
Vol 17 ◽  
Author(s):  
T. Durai Ananda Kumar ◽  
Sandhya Desai ◽  
Soumya Venkaraddiyavar ◽  
Naraparaju Swathi ◽  
Gurubasavaraj V. Pujar
Keyword(s):  
Mass Spectrometry ◽  
Drug Discovery ◽  
Mass Spectroscopy ◽  
Data Science ◽  
Protein Sequencing ◽  
Peptide Drug ◽  
Peptide Therapeutics ◽  
Computational Proteomics ◽  
Discovery Research ◽  
Drug Discovery Research

Abstract:: Drug discovery research focuses on Rational Drug Design (RDD) concepts and the major obstacles in the drug discovery process are lack of target specificity and selectivity. The realization of higher target selectivity of peptide drugs promoted the peptide research. Rapid growth in the genomics along with recombinant DNA (rDNA) technology and gene expression studies stimulated the peptide research. The promising use of peptide therapeutics demands sensitive and selective quantification methods. Protein sequencing and proteomic investigations can be successfully accomplished through Mass Spectroscopy (MS) based methods. Mass spectroscopy-based soft ionization methods namely, electrospray ionization (ESI) and Matrix-Assisted Laser Desorption/Ionization (MALDI) offers high-throughput sequencing provide the characterization (sequence and structure) of intact proteins/peptides. The advent of tandem Mass Spectrometry (MS/MS) along with data acquisition methods are the basis for the evolution in peptide therapeutics research. The evolution of data science, helped in developing computational proteomics, which assists in the quantitative determination of protein samples. This review narrates the role of mass spectrometry in the peptide drug discovery in particular the sequence characterization along with latest developments, such as computational proteomics.

MALDI-TOF Mass Spectrometry-Based High-Throughput Screening for Inhibitors of the Cytosolic DNA Sensor cGAS

2019 ◽  
Vol 25 (4) ◽  
pp. 372-383 ◽  
Author(s):  
Roman P. Simon ◽  
Martin Winter ◽  
Carola Kleiner ◽  
Robert Ries ◽  
Gisela Schnapp ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Drug Discovery ◽  
High Throughput ◽  
Cyclic Gmp ◽  
High Throughput Screening ◽  
Detection Methods ◽  
Maldi Tof Mass Spectrometry ◽  
Maldi Tof ◽  
Discovery Research ◽  
Drug Discovery Research

Comprehensive and unbiased detection methods are a prerequisite for high-throughput screening (HTS) campaigns within drug discovery research. Label-free matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) mass spectrometry (MS) has been introduced as an HTS-compatible readout for biochemical test systems to support the drug discovery process. So far, reported HTS applications were based on surface-modified systems or proof-of-concept studies. We present the utilization of a MALDI-TOF-based screening platform to identify inhibitors of human cyclic GMP-AMP synthase (cGAS), a mediator of innate immune response whose aberration has been causally correlated to a number of inflammatory disorders. In this context, the development and validation of a MALDI-TOF-based activity assay is reported to demonstrate fast, robust, and accurate detection of chemical cGAS inhibition by direct quantification of the physiological reaction product cyclic GMP-ATP (cGAMP). Results from a screen of a diverse library of more than 1 million small molecules in 1536-well format against the catalytic cGAS activity are presented with excellent assay performance and data quality. Identified hits were qualified in dose–response experiments and confirmed by RapidFire-MS measurements. Conclusively, the presented data provide the first proof of applicability of direct automated MALDI-TOF MS as a readout strategy for large-scale drug discovery HTS campaigns.

scholarly journals Modern Approaches in the Discovery and Development of Plant-Based Natural Products and Their Analogues as Potential Therapeutic Agents

Molecules ◽  
2022 ◽  
Vol 27 (2) ◽  
pp. 349
Author(s):  
Asim Najmi ◽  
Sadique A. Javed ◽  
Mohammed Al Bratty ◽  
Hassan A. Alhazmi
Keyword(s):  
Natural Products ◽  
Drug Discovery ◽  
Natural Product ◽  
Therapeutic Agents ◽  
Throughput Capacity ◽  
Scientific Interest ◽  
Comprehensive Overview ◽  
Natural Sources ◽  
Discovery Research ◽  
Drug Discovery Research

Natural products represents an important source of new lead compounds in drug discovery research. Several drugs currently used as therapeutic agents have been developed from natural sources; plant sources are specifically important. In the past few decades, pharmaceutical companies demonstrated insignificant attention towards natural product drug discovery, mainly due to its intrinsic complexity. Recently, technological advancements greatly helped to address the challenges and resulted in the revived scientific interest in drug discovery from natural sources. This review provides a comprehensive overview of various approaches used in the selection, authentication, extraction/isolation, biological screening, and analogue development through the application of modern drug-development principles of plant-based natural products. Main focus is given to the bioactivity-guided fractionation approach along with associated challenges and major advancements. A brief outline of historical development in natural product drug discovery and a snapshot of the prominent natural drugs developed in the last few decades are also presented. The researcher’s opinions indicated that an integrated interdisciplinary approach utilizing technological advances is necessary for the successful development of natural products. These involve the application of efficient selection method, well-designed extraction/isolation procedure, advanced structure elucidation techniques, and bioassays with a high-throughput capacity to establish druggability and patentability of phyto-compounds. A number of modern approaches including molecular modeling, virtual screening, natural product library, and database mining are being used for improving natural product drug discovery research. Renewed scientific interest and recent research trends in natural product drug discovery clearly indicated that natural products will play important role in the future development of new therapeutic drugs and it is also anticipated that efficient application of new approaches will further improve the drug discovery campaign.

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