Drug Metabolism Databases and High-Throughput Testing During Drug Design and Development Edited by Paul W. Ehrhardt. International Union of Pure and Applied Chemistry, Blackwell Science, Ltd., Malden, MA. 1999. 340 pp. 19 x 25 cm. ISBN 0-632-05342-9. $60.00.

2000 ◽  
Vol 43 (16) ◽  
pp. 3197-3198
Author(s):  
Rory P. Remmel
Keyword(s):  
Drug Design ◽  
Drug Metabolism ◽  
High Throughput ◽  
Design And Development ◽  
International Union ◽  
Applied Chemistry

scholarly journals A Taxon-Specific and High-Throughput Method for Measuring Ligand Binding to Nicotinic Acetylcholine Receptors

Toxins ◽  
2019 ◽  
Vol 11 (10) ◽  
pp. 600 ◽  
Author(s):  
Christina N. Zdenek ◽  
Richard J. Harris ◽  
Sanjaya Kuruppu ◽  
Nicholas J. Youngman ◽  
James S. Dobson ◽  
...  
Keyword(s):  
Drug Design ◽  
Ligand Binding ◽  
High Throughput ◽  
Nicotinic Acetylcholine Receptors ◽  
Acetylcholine Receptors ◽  
Design And Development ◽  
Evolutionary Patterns ◽  
Nicotinic Acetylcholine ◽  
Specialist Species ◽  
Ophiophagus Hannah

The binding of compounds to nicotinic acetylcholine receptors is of great interest in biomedical research. However, progress in this area is hampered by the lack of a high-throughput, cost-effective, and taxonomically flexible platform. Current methods are low-throughput, consume large quantities of sample, or are taxonomically limited in which targets can be tested. We describe a novel assay which utilizes a label-free bio-layer interferometry technology, in combination with adapted mimotope peptides, in order to measure ligand binding to the orthosteric site of nicotinic acetylcholine receptor alpha-subunits of diverse organisms. We validated the method by testing the evolutionary patterns of a generalist feeding species (Acanthophis antarcticus), a fish specialist species (Aipysurus laevis), and a snake specialist species (Ophiophagus hannah) for comparative binding to the orthosteric site of fish, amphibian, lizard, snake, bird, marsupial, and rodent alpha-1 nicotinic acetylcholine receptors. Binding patterns corresponded with diet, with the Acanthophis antarcticus not showing bias towards any particular lineage, while Aipysurus laevis showed selectivity for fish, and Ophiophagus hannah a selectivity for snake. To validate the biodiscovery potential of this method, we screened Acanthophis antarcticus and Tropidolaemus wagleri venom for binding to human alpha-1, alpha-2, alpha-3, alpha-4, alpha-5, alpha-6, alpha-7, alpha-9, and alpha-10. While A. antarcticus was broadly potent, T. wagleri showed very strong but selective binding, specifically to the alpha-1 target which would be evolutionarily selected for, as well as the alpha-5 target which is of major interest for drug design and development. Thus, we have shown that our novel method is broadly applicable for studies including evolutionary patterns of venom diversification, predicting potential neurotoxic effects in human envenomed patients, and searches for novel ligands of interest for laboratory tools and in drug design and development.

What Is A Chemical Element?

2020 ◽  
Keyword(s):  
Periodic Table ◽  
Chemical Element ◽  
Abstract Concept ◽  
International Union ◽  
Applied Chemistry ◽  
Educational Levels ◽  
Unique Position ◽  
Current State ◽  
Element Carbon ◽  
Definition Of

The term “element” is typically used in two distinct senses. First it is taken to mean isolated simple substances such as the green gas chlorine or the yellow solid sulphur. In some languages, including English, it is also used to denote an underlying abstract concept that subsumes simple substances but possesses no properties as such. The allotropes and isotopes of carbon, for example, all represent elements in the sense of simple substances. However, the unique position for the element carbon in the periodic table refers to the abstract sense of “element.” The dual definition of elements proposed by the International Union for Pure and Applied Chemistry contrasts an abstract meaning and an operational one. Nevertheless, the philosophical aspects of this notion are not fully captured by the IUPAC definition, despite the fact that they were crucial for the construction of the periodic table. This pivotal chemical notion remains ambiguous and such ambiguity raises problems at the epistemic, logical, and educational levels. These aspects are discussed throughout the book, from different perspectives. This collective book provides an overview of the current state of the debate on the notion of chemical element. Its authors are historians of chemistry, philosophers of chemistry, and chemists with epistemological and educational concerns.

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