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Progress in Medicinal Chemistry Journal
Papers
Our understanding of the structural biology of G protein-coupled receptors has undergone a transformation over the past 5 years. New protein-ligand complexes are described almost monthly in high profile journals. Appreciation of how small molecules and natural ligands bind to the...
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An intensive research effort to identify potent, viable drugs for the management of acquired immunodeficiency syndrome (AIDS) resulted in the development of SUSTIVA (efavirenz), the first non-nucleoside reverse transcriptase inhibitor (NNRTI) approved by the FDA as a preferred fi...
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This chapter focuses on the transfer process for ions across the membrane. Passive ion transfer across cell membranes refers to ion movement without the expenditure of metabolic energy by the cell. The driving force for such movements are the existing electrochemical gradients ac...
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This chapter provides a laboratory guide to enzymology for workers in biochemical pharmacology and related fields. It includes a list of just over 100 enzymes of special significance to pharmacological studies together with a minimum bibliography for each one. Enzyme investigatio...
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TRPA1 is a well-validated therapeutic target in areas of high unmet medical need that include pain and respiratory disorders. The human genetic rationale for TRPA1 as a pain target is provided by a study describing a rare gain-of-function mutation in TRPA1, causing familial episo...
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Publisher Summary This chapter describes the classification and structure of protein tyrosine kinases (PTKs), their mode of action, their cellular targets, and the processes in which they are involved. A vast amount of research has been carried out to try to identify the role of ...
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Cystic fibrosis (CF) is a genetic disorder driven by mutations in the cystic fibrosis transmembrane conductance regulator (CFTR) gene. While different mutations lead to varying levels of disease severity, the most common CFTR F508del mutation leads to defects in protein stability...
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This chapter explores that heparin and heparinoids constitute a group of compounds that have many remarkable pharmacological properties. The chapter demonstrates that heparin binds or complexes with proteins and other bases and so modifies their biological activity. As a result, ...
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This chapter explores that the antispasmodic activity of (1) khellin and (2) methylchromone has been known for some time and until recently, these two were the only clinically useful compounds containing the chromone ring system. The discovery that cromoglycic acid (3,R= H) and i...
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Imaging has played an important part in the diagnosis of disease and development of the understanding of the underlying disease mechanisms and is now poised to make an impact in the development of new pharmaceuticals. This chapter discusses the underlying technologies that make t...
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