Classical Pharmacology
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Classical Pharmacology
In the field of drug discovery, classical pharmacology, also known as forward pharmacology, or phenotypic drug discovery (PDD), relies on phenotypic screening (screening in intact cells or whole organisms) of chemical libraries of synthetic small molecules, natural products or extracts to identify substances that have a desirable therapeutic effect. Using the techniques of medicinal chemistry, the potency, selectivity, and other properties of these screening hits are optimized to produce candidate drugs. Historical background Classical pharmacology traditionally has been the basis for the discovery of new drugs. Compounds are screened in cellular or animal models of disease to identify compounds that cause a desirable change in phenotype. Only after the compounds have been discovered, an effort is made to determine the biological target of the compounds through target validation experiments often involving chemoproteomics. More recently it has become popular to develop a h ...
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Forward And Reverse Pharmacology
Forward is a relative direction, the opposite of backward. Forward may also refer to: People * Forward (surname) Sports * Forward (association football) * Forward (basketball), including: ** Point forward ** Power forward (basketball) ** Small forward * Forward (ice hockey) ** Power forward (ice hockey) * In rugby football: ** Forwards (rugby league), in rugby league football ** Forwards (rugby union), in rugby union football * Forward Sports, a Pakistan sportswear brand * BK Forward, a Swedish club for association football and bandy Politics * Avante (political party) (Portuguese for ''forward''), a political party in Brazil * Forward (Belgium), a political party in Belgium * Forward (Denmark), a political party in Denmark * Forward (Greenland), a political party in Greenland * Forward Party (United States), a centrist American political party * Kadima (Hebrew for ''forward''), a political party in Israel * La République En Marche! (sometimes translated as ''Forward! ...
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High-throughput Screening
High-throughput screening (HTS) is a method for scientific experimentation especially used in drug discovery and relevant to the fields of biology, materials science and chemistry. Using robotics, data processing/control software, liquid handling devices, and sensitive detectors, high-throughput screening allows a researcher to quickly conduct millions of chemical, genetic, or pharmacological tests. Through this process one can quickly recognize active compounds, antibodies, or genes that modulate a particular biomolecular pathway. The results of these experiments provide starting points for drug design and for understanding the noninteraction or role of a particular location. Assay plate preparation The key labware or testing vessel of HTS is the microtiter plate, which is a small container, usually disposable and made of plastic, that features a grid of small, open divots called ''wells''. In general, microplates for HTS have either 96, 192, 384, 1536, 3456 or 6144 wells. The ...
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Ayurvedic Medicaments
Ayurveda () is an alternative medicine system with historical roots in the Indian subcontinent. The theory and practice of Ayurveda is pseudoscientific. Ayurveda is heavily practiced in India and Nepal, where around 80% of the population report using it. Ayurveda therapies have varied and evolved over more than two millennia. Therapies include herbal medicines, special diets, meditation, yoga, massage, laxatives, enemas, and medical oils. Ayurvedic preparations are typically based on complex herbal compounds, minerals, and metal substances (perhaps under the influence of early Indian alchemy or ''rasashastra''). Ancient Ayurveda texts also taught surgical techniques, including rhinoplasty, kidney stone extractions, sutures, and the extraction of foreign objects. The main classical Ayurveda texts begin with accounts of the transmission of medical knowledge from the gods to sages, and then to human physicians. Printed editions of the ''Sushruta Samhita'' (''Sushruta's Compendi ...
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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 ...
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Phenotypic Screening
In genetics, the phenotype () is the set of observable characteristics or traits of an organism. The term covers the organism's morphology or physical form and structure, its developmental processes, its biochemical and physiological properties, its behavior, and the products of behavior. An organism's phenotype results from two basic factors: the expression of an organism's genetic code, or its genotype, and the influence of environmental factors. Both factors may interact, further affecting phenotype. When two or more clearly different phenotypes exist in the same population of a species, the species is called polymorphic. A well-documented example of polymorphism is Labrador Retriever coloring; while the coat color depends on many genes, it is clearly seen in the environment as yellow, black, and brown. Richard Dawkins in 1978 and then again in his 1982 book ''The Extended Phenotype'' suggested that one can regard bird nests and other built structures such as cad ...
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Reverse Pharmacology
In the field of drug discovery, reverse pharmacology also known as target-based drug discovery (TDD), a hypothesis is first made that modulation of the activity of a specific protein target thought to be disease modifying will have beneficial therapeutic effects. Screening of chemical libraries of small molecules is then used to identify compounds that bind with high affinity to the target. The hits from these screens are then used as starting points for drug discovery. This method became popular after the sequencing of the human genome which allowed rapid cloning and synthesis of large quantities of purified proteins. This method is the most widely used in drug discovery today. Differently than the classical (forward) pharmacology, with the reverse pharmacology approach ''in vivo'' efficacy of identified active (lead) compounds is usually performed in the final drug discovery stages. See also * Classical pharmacology * Reverse vaccinology Reverse vaccinology is an imp ...
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Folk Medicine
Traditional medicine (also known as indigenous medicine or folk medicine) comprises medical aspects of traditional knowledge that developed over generations within the folk beliefs of various societies, including indigenous peoples, before the era of modern medicine. The World Health Organization (WHO) defines traditional medicine as "the sum total of the knowledge, skills, and practices based on the theories, beliefs, and experiences indigenous to different cultures, whether explicable or not, used in the maintenance of health as well as in the prevention, diagnosis, improvement or treatment of physical and mental illness". Traditional medicine is often contrasted with scientific medicine. In some Asian and African countries, up to 80% of the population relies on traditional medicine for their primary health care needs. When adopted outside its traditional culture, traditional medicine is often considered a form of alternative medicine. Practices known as traditional medicines ...
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Pharmacognosy
Pharmacognosy is the study of medicinal plants and other natural substances as sources of drugs. The American Society of Pharmacognosy defines pharmacognosy as "the study of the physical, chemical, biochemical, and biological properties of drugs, drug substances, or potential drugs or drug substances of natural origin as well as the search for new drugs from natural sources". Description The word "pharmacognosy" is derived from two Greek words: ', (drug), and ''gnosis'' (knowledge) or the Latin verb '' cognosco'' (', 'with', and , 'know'; itself a cognate of the Greek verb , , meaning 'I know, perceive'), meaning 'to conceptualize' or 'to recognize'. The term "pharmacognosy" was used for the first time by the Austrian physician Schmidt in 1811 and by Anotheus Seydler in 1815 in a work titled ''Analecta Pharmacognostica''. Originally—during the 19th century and the beginning of the 20th century—"pharmacognosy" was used to define the branch of medicine or commodity scie ...
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Reverse Pharmacology
In the field of drug discovery, reverse pharmacology also known as target-based drug discovery (TDD), a hypothesis is first made that modulation of the activity of a specific protein target thought to be disease modifying will have beneficial therapeutic effects. Screening of chemical libraries of small molecules is then used to identify compounds that bind with high affinity to the target. The hits from these screens are then used as starting points for drug discovery. This method became popular after the sequencing of the human genome which allowed rapid cloning and synthesis of large quantities of purified proteins. This method is the most widely used in drug discovery today. Differently than the classical (forward) pharmacology, with the reverse pharmacology approach ''in vivo'' efficacy of identified active (lead) compounds is usually performed in the final drug discovery stages. See also * Classical pharmacology * Reverse vaccinology Reverse vaccinology is an imp ...
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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 ...
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Drug Discovery
In the fields of medicine, biotechnology and pharmacology, drug discovery is the process by which new candidate medications are discovered. Historically, drugs were discovered by identifying the active ingredient from traditional remedies or by serendipitous discovery, as with penicillin. More recently, chemical libraries of synthetic small molecules, natural products or extracts were screened in intact cells or whole organisms to identify substances that had a desirable therapeutic effect in a process known as classical pharmacology. After sequencing of the human genome allowed rapid cloning and synthesis of large quantities of purified proteins, it has become common practice to use high throughput screening of large compounds libraries against isolated biological targets which are hypothesized to be disease-modifying in a process known as reverse pharmacology. Hits from these screens are then tested in cells and then in animals for efficacy. Modern drug discovery involves the ...
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Biological Target
A biological target is anything within a living organism to which some other entity (like an endogenous 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 pharmacologically active drug 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 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 – A relatively weak interaction between the stimulus and the target where no chemical bond is formed between the two interacting partners and hence the interaction is completely reversible. * reversible covalent â ...
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