Gujral, TS; Peshkin, L; Kirschner, MW (April 1, 2014). "Exploiting polypharmacology for drug target deconvolution". Proc. Natl ...
Langer, Thierry; Bryant, Sharon D (2013-10-01). "Computational methods for drug target profiling and polypharmacology". In ...
"Dual kinase-bromodomain inhibitors for rationally designed polypharmacology". Nature Chemical Biology. 10 (4): 305-12. doi: ...
"5-HT2C Receptor Structures Reveal the Structural Basis of GPCR Polypharmacology". Cell. 172 (4): 719-730.e14. doi:10.1016/j. ...
The group was unable to rule out partial polypharmacology against other targets. DS54360155, a novel compound with a unique and ...
During this time he developed an interest in the polypharmacology of ADME/Tox proteins. In 2004 he joined GeneGo (now owned by ...
A perspective from polypharmacology". Current Medicinal Chemistry. 26. doi:10.2174/0929867326666191212103330. ISSN 1875-533X. ...
Toward a Targeted Polypharmacology To Control Nitric Oxide". Biochemistry. 48 (36): 8624-8635. doi:10.1021/bi9007098. PMC ...
Combination therapy for a complex disease (polypharmacology) is suggested in this field since one active pharmaceutical ...
"5-HT2C receptor structures reveal the structural basis of GPCR polypharmacology" Cell 172, 719-730 (2018). Online 01Feb2018. ...
Epigenetic Polypharmacology' or 'Targeted Polypharmacology', a branch of Polypharmacology.[13] In 2008, Professor Keven Shokat ... Polypharmacology'.[14] Since then, Polypharmacology has become a new branch of Pharmacology discipline and research field as ... Polypharmacology remains to be one of the major challenges in drug development, and it opens novel avenues to rationally design ... Polypharmacology is the design or use of pharmaceutical agents that act on multiple targets or disease pathways. Despite ...
... is a pharmacological concept describing subjects' reduced reaction to a drug following its repeated use. Increasing its dosage may re-amplify the drug's effects; however, this may accelerate tolerance, further reducing the drug's effects. Drug tolerance is indicative of drug use but is not necessarily associated with drug dependence or addiction.[5] The process of tolerance development is reversible (e.g., through a drug holiday[6]) and can involve both physiological factors and psychological factors.[7] One may also develop drug tolerance to side effects,[8] in which case tolerance is a desirable characteristic. A medical intervention that has an objective to increase tolerance (e.g., allergen immunotherapy, in which one is exposed to larger and larger amounts of allergen to decrease one's allergic reactions) is called drug desensitization.[9] The opposite concept to drug tolerance is drug reverse tolerance (or drug sensitization), in which case the subject's reaction or effect ...
A drug's pharmacological effects can only occur once it has been fully solubilized and has entered the blood stream. For most drugs administered orally, the drug must be ingested, pass through the stomach, and into the small intestine, where the drug molecules enter the blood stream through the villi and microvilli.[1] Gastric emptying time can vary from 0 to 3 hours,[2] and therefore plays a major role in onset of action for orally administered drugs. For intravenous administration, the pathway is much shorter because the drug is administered (usually already in solution) directly to the bloodstream. ...
In pharmacology, efficacy (Emax) is the maximum response achievable from an applied or dosed agent, for instance, a small molecule drug.[2] Intrinsic activity is a relative term for a drug's efficacy relative to a drug with the highest observed efficacy.[3] It is a purely descriptive term that has little or no mechanistic interpretation. In order for a drug to have an effect, it needs to bind to its target, and then to affect the function of this target. The target of a drug is commonly referred to as a receptor, but can in general be any chemically sensitive site on any molecule found in the body. The nature of such binding can be quantified by characterising how tightly these molecules, the drug and its receptor, interact: this is known as the affinity. Efficacy, on the other hand, is a measure of the action of a drug once binding has occurred. The maximum response, Emax, will be reduced if efficacy is sufficiently low. The definition of efficacy has been object for discussion.[4] The only way ...
The origins of clinical pharmacology date back to the Middle Ages, with pharmacognosy and Avicenna's The Canon of Medicine, Peter of Spain's Commentary on Isaac, and John of St Amand's Commentary on the Antedotary of Nicholas.[7] Early pharmacology focused on herbalism and natural substances, mainly plant extracts. Medicines were compiled in books called pharmacopoeias. Crude drugs have been used since prehistory as a preparation of substances from natural sources. However, the active ingredient of crude drugs are not purified and the substance is adulterated with other substances. Traditional medicine varies between cultures and may be specific to a particular culture, such as in traditional Chinese, Mongolian, Tibetan and Korean medicine. However much of this has since been regarded as pseudoscience. Pharmacological substances known as entheogens may have spiritual and religious use and historical context. In the 17th century, the English Physician Nicholas Culpeper translated and used ...
Polypharmacology. *Chemotherapy. *List of drugs. *WHO list of essential medicines. *Methods (Gut bath, Radioligand binding ...