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Lead-Seeking Approaches
High quality leads provide the foundation for the discovery of successful clinical development candidates, and therefore the identi?cation of leads is an essential part of drug discovery. The process for the identi?cation of leads generally starts with the screening of a compound collection, either an HTS of a relatively large compound collection (hundreds of thousands to one million plus compounds) or a more focused screen of a smaller set of compounds that have been preselected for the target of interest. Virtual screening methods such as structure-based or pharmacophore-based searches can complement or replace one of the above approaches. Once hits are identi?ed from one or more of these ...
The Dorsey Family
The work at hand is the only comprehensive history of Anson County, spanning over 225 years of the county's growth from a vast wilderness to a thriving industrial and agricultural community. The first third of the volume traces politics in the county. The middle portion covers Anson's social history, including education, religion, agriculture and industry, social and cultural life, etc. The final third of the book provides biographical sketches of scores of Anson "Men and Women of Note" and a number of source record collections of great import to genealogists.
Young England
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Fencing for Conservation
The conflict between increasing human population and biodiversity conservation is one of the IUCN’s key threatening processes. Conservation planning has received a great deal of coverage and research as a way of conserving biodiversity yet, while theoretically successful, it has never been tested. Simple lines on maps to illustrate conservation areas are unlikely to be successful in the light of human encroachment. It may be that some form of overt display is necessary to ensure the protection of reserves. This may be signage, presence of guards/rangers or physical fencing structures. The need for some form of barrier goes beyond restricting human access. The megafauna of Africa pose a gen...
Kinase Drug Discovery
Kinase inhibition remains an area of significant interest, and growing importance, across academia and the pharmaceutical industry. There are now many marketed drugs that target kinases and a significant number of compounds are currently in various stages of clinical development. This book is a forward-looking analysis of a number of key areas for kinase inhibition in the coming years and builds on the first volume. This includes topics such as screening approaches to target kinases along with different modes of inhibition such as allosteric and covalent. Novel approaches such as macrocyclisation are considered along with how the properties of kinase inhibitors have evolved, including the potential for brain penetration. Recent areas of great importance also covered include cutting edge molecular modelling approaches and the importance of kinase mutations. The evolving biology of kinases has also resulted in increased interest in the immuno-oncology area and also pseudokinases as a target family. As with the first volume the book finishes with a forward looking view of how research against this fascinating target class may evolve.
Journal
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Kinase Drug Discovery
Kinase inhibition remains an area of significant interest, and growing importance, across academia and the pharmaceutical industry. There are now many marketed drugs that target kinases and a significant number of compounds are currently in various stages of clinical development. This book is a forward-looking analysis of a number of key areas for kinase inhibition in the coming years and builds on the first volume. This includes topics such as screening approaches to target kinases along with different modes of inhibition such as allosteric and covalent. Novel approaches such as macrocyclisation are considered along with how the properties of kinase inhibitors have evolved, including the potential for brain penetration. Recent areas of great importance also covered include cutting edge molecular modelling approaches and the importance of kinase mutations. The evolving biology of kinases has also resulted in increased interest in the immuno-oncology area and also pseudokinases as a target family. As with the first volume the book finishes with a forward looking view of how research against this fascinating target class may evolve.
