|
Polypharmacology
Polypharmacology is the design or use of pharmaceutical agents that act on multiple targets or disease pathways. Despite scientific advancements and an increase of global R&D spending, drugs are frequently withdrawn from markets. This is primarily due to their side effects or toxicities. Drug molecules often interact with multiple targets and the unintended drug-target interactions can cause side effects. Polypharmacology remains to be one of the major challenges in drug development, and it opens novel avenues to rationally design the next generation of more effective but less toxic therapeutic agents. Polypharmacology suggests that more effective drugs can be developed by specifically modulating multiple targets. It is generally thought that complex diseases such as cancer and central nervous system diseases may require complex therapeutic approaches. In this respect, a drug that "hits" multiple sensitive nodes belonging to a network of interacting targets offers the potential for ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chemoproteomics
Chemoproteomics entails a broad array of techniques used to identify and interrogate protein- small molecule interactions. Chemoproteomics complements phenotypic drug discovery, a paradigm that aims to discover lead compounds on the basis of alleviating a disease phenotype, as opposed to target-based drug discovery (reverse pharmacology), in which lead compounds are designed to interact with predetermined disease-driving biological targets. As phenotypic drug discovery assays do not provide confirmation of a compound's mechanism of action, chemoproteomics provides valuable follow-up strategies to narrow down potential targets and eventually validate a molecule's mechanism of action. Chemoproteomics also attempts to address the inherent challenge of drug promiscuity in small molecule drug discovery by analyzing protein-small molecule interactions on a proteome-wide scale. A major goal of chemoproteomics is to characterize the interactome of drug candidates to gain insight into m ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chemoproteomics
Chemoproteomics entails a broad array of techniques used to identify and interrogate protein- small molecule interactions. Chemoproteomics complements phenotypic drug discovery, a paradigm that aims to discover lead compounds on the basis of alleviating a disease phenotype, as opposed to target-based drug discovery (reverse pharmacology), in which lead compounds are designed to interact with predetermined disease-driving biological targets. As phenotypic drug discovery assays do not provide confirmation of a compound's mechanism of action, chemoproteomics provides valuable follow-up strategies to narrow down potential targets and eventually validate a molecule's mechanism of action. Chemoproteomics also attempts to address the inherent challenge of drug promiscuity in small molecule drug discovery by analyzing protein-small molecule interactions on a proteome-wide scale. A major goal of chemoproteomics is to characterize the interactome of drug candidates to gain insight into m ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Side Effect
In medicine, a side effect is an effect, whether therapeutic or adverse, that is secondary to the one intended; although the term is predominantly employed to describe adverse effects, it can also apply to beneficial, but unintended, consequences of the use of a drug. Developing drugs is a complicated process, because no two people are exactly the same, so even drugs that have virtually no side effects, might be difficult for some people. Also, it is difficult to make a drug that targets one part of the body but that does not affect other parts, the fact that increases the risk of side effects in the untargeted parts. Occasionally, drugs are prescribed or procedures performed specifically for their side effects; in that case, said side effect ceases to be a side effect and is now an intended effect. For instance, X-rays were historically (and are currently) used as an imaging technique; the discovery of their oncolytic capability led to their employ in radiotherapy (ablation o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Drug Target
A biological target is anything within a living organism to which some other entity (like an endogenous ligand (biochemistry), ligand or a drug) is directed and/or binds, resulting in a change in its behavior or function. Examples of common classes of biological targets are proteins and nucleic acids. The definition is context-dependent, and can refer to the biological target of a pharmacological activity, pharmacologically active drug Chemical compound, compound, the receptor target of a hormone (like insulin), or some other target of an external stimulus. Biological targets are most commonly proteins such as enzymes, ion channels, and receptor (biochemistry), receptors. Mechanism The external stimulus (''i.e.'', the drug or ligand) physically binds to ("hits") the biological target. The interaction between the substance and the target may be: * noncovalent bonding, noncovalent – A relatively weak interaction between the stimulus and the target where no chemical bond is forme ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chemical Biology
Chemical biology is a scientific discipline spanning the fields of chemistry and biology. The discipline involves the application of chemical techniques, analysis, and often small molecules produced through synthetic chemistry, to the study and manipulation of biological systems. In contrast to biochemistry, which involves the study of the chemistry of biomolecules and regulation of biochemical pathways within and between cells, chemical biology deals with chemistry ''applied to'' biology (synthesis of biomolecules, the simulation of biological systems, etc.). Introduction Some forms of chemical biology attempt to answer biological questions by studying biological systems at the chemical level. In contrast to research using biochemistry, genetics, or molecular biology, where mutagenesis can provide a new version of the organism, cell, or biomolecule of interest, chemical biology probes systems ''in vitro'' and ''in vivo'' with small molecules that have been designed for a specific ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bryan Roth
Bryan L. Roth is the Michael Hooker Distinguished Professor of Protein Therapeutics and Translational Proteomics, University of North Carolina School of Medicine. He is recognized for his discoveries and inventions in the general areas of molecular pharmacology, GPCR structure, and function and synthetic neurobiology. He is a member of the American Academy of Arts and Sciences (AAAS) and the National Academy of Medicine of the National Academy of Sciences (NAM) Education Roth earned his B.A. in biology from Carroll College in 1977 and his M.D. and Ph.D. in biochemistry from Saint Louis University in 1983. After postdoctoral training at the National Institute of Mental Health (NIMH), he completed a psychiatry residency and fellowship at Stanford University in 1991. In 2007 he was appointed as the Michael Hooker Distinguished Professor of Protein Therapeutics and Translational Proteomics, UNC School of Medicine. Research Roth has made contributions to the fields of G p ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
