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ACE Inhibitors Drug Design
The discovery of an orally inactive peptide from snake venom established the unimportant role of angiotensin converting enzyme (ACE) Enzyme inhibitor, inhibitors in regulating blood pressure. This led to the drug development, development of Captopril, the first ACE inhibitor. When the adverse effects of Captopril became apparent new derivates were designed. Then after the discovery of two active sites of ACE: N-domain and C-domain, the development of domain-specific ACE inhibitors began. Development of first generation ACE inhibitors The development of the nonapeptide teprotide (glutamic acid, Glu-tryptophan, Trp-proline, Pro-arginine, Arg-Pro-glutamine, Gln-isoleucine, Ile-Pro-Pro), which was originally isolated from the venom of the Brazilian pit viper ''Bothrops jararaca'', greatly clarified the importance of ACE in hypertension. However, its lack of oral activity limited its therapeutic utility. L-benzylsuccinic acid (2(R)-benzyl-3-carboxypropionic acid) was described to be ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ACE And Inhibitor
An ace is a playing card, Dice, die or domino with a single Pip (counting), pip. In the standard French deck, an ace has a single suit (cards), suit symbol (a heart, diamond, spade, or club) located in the middle of the card, sometimes large and decorated, especially in the case of the ace of spades. This embellishment on the ace of spades started when James VI and I, King James VI of Scotland and I of England required an insignia of the printing house to be printed on the ace of spades. This insignia was necessary for identifying the printing house and stamping it as having paid the new stamp tax. Although this requirement was abolished in 1960, the tradition has been kept by many card makers. In other countries the stamp and embellishments are usually found on ace cards; clubs in France, diamonds in Russia, and hearts in Genoa because they have the most blank space. Etymology The word "ace" comes from the Old French word ''as'' (from Latin 'as') meaning 'a unit', from the n ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Isoleucine
Isoleucine (symbol Ile or I) is an α-amino acid that is used in the biosynthesis of proteins. It contains an α-amino group (which is in the protonated −NH form under biological conditions), an α-carboxylic acid group (which is in the deprotonated −COO form under biological conditions), and a hydrocarbon side chain with a branch (a central carbon atom bound to three other carbon atoms). It is classified as a non-polar, uncharged (at physiological pH), branched-chain, aliphatic amino acid. It is essential in humans, meaning the body cannot synthesize it, and must be ingested in our diet. Isoleucine is synthesized from pyruvate employing leucine biosynthesis enzymes in other organisms such as bacteria. It is encoded by the codons AUU, AUC, and AUA. Metabolism Biosynthesis As an essential nutrient, it is not synthesized in the body, hence it must be ingested, usually as a component of proteins. In plants and microorganisms, it is synthesized via several steps, sta ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Carboxylate
In organic chemistry, a carboxylate is the conjugate base of a carboxylic acid, (or ). It is an ion with negative charge. Carboxylate salts are salts that have the general formula , where M is a metal and ''n'' is 1, 2,...; ''carboxylate esters'' have the general formula (or ). R and R′ are organic groups; R′ ≠ H. Synthesis Carboxylate ions can be formed by deprotonation of carboxylic acids. Such acids typically have p''K''a of less than 5, meaning that they can be deprotonated by many bases, such as sodium hydroxide or sodium bicarbonate. :RCOOH + NaOH -> RCOONa + H2O Resonance stabilization of the carboxylate ion Carboxylic acids easily dissociate into a carboxylate anion and a positively charged hydrogen ion (proton), much more readily than alcohols do (into an alkoxide ion and a proton), because the carboxylate ion is stabilized by resonance. The negative charge that is left after deprotonation of the carboxyl group is delocalized betw ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Suggestion
Suggestion is the psychological process by which a person guides their own or another person's desired thoughts, feelings, and behaviors by presenting stimuli that may elicit them as reflexes instead of relying on conscious effort. Nineteenth-century writers on psychology such as William James used the words "suggest" and "suggestion" in the context of a particular idea which was said to ''suggest'' another when it brought that other idea to mind. Early scientific studies of hypnosis by Clark Leonard Hull and others extended the meaning of these words in a special and technical sense (Hull, 1933). The original neuropsychological theory of hypnotic suggestion was based upon the ideomotor reflex response that William B. Carpenter declared, in 1852, was the principle through which James Braid's hypnotic phenomena were produced. Émile Coué Émile Coué (1857–1926) was a significant pioneer in the development of an understanding of the application of therapeutic suggestion; ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Carbonyl Group
In organic chemistry, a carbonyl group is a functional group composed of a carbon atom double-bonded to an oxygen atom: C=O. It is common to several classes of organic compounds, as part of many larger functional groups. A compound containing a carbonyl group is often referred to as a carbonyl compound. The term carbonyl can also refer to carbon monoxide as a ligand in an inorganic or organometallic complex (a metal carbonyl, e.g. nickel carbonyl). The remainder of this article concerns itself with the organic chemistry definition of carbonyl, where carbon and oxygen share a double bond. Carbonyl compounds In organic chemistry, a carbonyl group characterizes the following types of compounds: Other organic carbonyls are urea and the carbamates, the derivatives of acyl chlorides chloroformates and phosgene, carbonate esters, thioesters, lactones, lactams, hydroxamates, and isocyanates. Examples of inorganic carbonyl compounds are carbon dioxide and carbonyl sulfide. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Carboxyl Group
In organic chemistry, a carboxylic acid is an organic acid that contains a carboxyl group () attached to an R-group. The general formula of a carboxylic acid is or , with R referring to the alkyl, alkenyl, aryl, or other group. Carboxylic acids occur widely. Important examples include the amino acids and fatty acids. Deprotonation of a carboxylic acid gives a carboxylate anion. Examples and nomenclature Carboxylic acids are commonly identified by their trivial names. They at oftentimes have the suffix ''-ic acid''. IUPAC-recommended names also exist; in this system, carboxylic acids have an ''-oic acid'' suffix. For example, butyric acid (C3H7CO2H) is butanoic acid by IUPAC guidelines. For nomenclature of complex molecules containing a carboxylic acid, the carboxyl can be considered position one of the parent chain even if there are other substituents, such as 3-chloropropanoic acid. Alternately, it can be named as a "carboxy" or "carboxylic acid" substituent on another ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Analog (chemistry)
A structural analog (analogue in modern traditional English; Commonwealth English), also known as a chemical analog or simply an analog, is a compound having a structure similar to that of another compound, but differing from it in respect to a certain component. It can differ in one or more atoms, functional groups, or substructures, which are replaced with other atoms, groups, or substructures. A structural analog can be imagined to be formed, at least theoretically, from the other compound. Structural analogs are often isoelectronic. Despite a high chemical similarity, structural analogs are not necessarily functional analogs and can have very different physical, chemical, biochemical, or pharmacological properties. In drug discovery, either a large series of structural analogs of an initial lead compound are created and tested as part of a structure–activity relationship study or a database is screened for structural analogs of a lead compound. Chemical analogues of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
By-product
A by-product or byproduct is a secondary product derived from a production process, manufacturing process or chemical reaction; it is not the primary product or service being produced. A by-product can be useful and marketable or it can be considered waste: for example, bran, which is a byproduct of the milling of wheat into refined flour, is sometimes composted or burned for disposal, but in other cases, it can be used as a nutritious ingredient in human food or animal feed. Gasoline was once a byproduct of oil refining that later became a desirable commodity as motor fuel. The plastic used in plastic shopping bags also started as a by-product of oil refining. In economics In the context of production, a by-product is the "output from a joint production process that is minor in quantity and/or net realizable value (NRV) when compared with the main products". Because they are deemed to have no influence on reported financial results, by-products do not receive allocations ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Author
An author is the writer of a book, article, play, mostly written work. A broader definition of the word "author" states: "''An author is "the person who originated or gave existence to anything" and whose authorship determines responsibility for what was created''." Typically, the first owner of a copyright is the person who created the work, i.e. the author. If more than one person created the work (i.e., multiple authors), then a case of joint authorship takes place. The copyright laws are have minor differences in various jurisdictions across the United States. The United States Copyright Office, for example, defines copyright as "a form of protection provided by the laws of the United States (title 17, U.S. Code) to authors of 'original works of authorship.'" Legal significance of authorship Holding the title of "author" over any "literary, dramatic, musical, artistic, rcertain other intellectual works" gives rights to this person, the owner of the copyright, especially ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Carboxypeptidase A
Carboxypeptidase A usually refers to the pancreatic exopeptidase that hydrolyzes peptide bonds of C-terminal residues with aromatic or aliphatic side-chains. Most scientists in the field now refer to this enzyme as CPA1, and to a related pancreatic carboxypeptidase as CPA2. Types In addition, there are 4 other mammalian enzymes named CPA-3 through CPA-6, and none of these are expressed in the pancreas. Instead, these other CPA-like enzymes have diverse functions. * CPA3 (also known as mast-cell CPA) is involved in the digestion of proteins by mast cells. * CPA4 (previously known as CPA-3, but renumbered when mast-cell CPA was designated CPA-3) may be involved in tumor progression, but this enzyme has not been well studied. * CPA5 has not been well studied. * CPA6 is expressed in many tissues during mouse development, and in adult shows a more limited distribution in brain and several other tissues. CPA6 is present in the extracellular matrix where it is enzymatically activ ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Potency (pharmacology)
In the field of pharmacology Pharmacology is a branch of medicine, biology and pharmaceutical sciences concerned with drug or medication action, where a drug may be defined as any artificial, natural, or endogenous (from within the body) molecule which exerts a biochemi ..., potency is a measure of drug activity expressed in terms of the amount required to produce an effect of given intensity. A highly potent drug (e.g., fentanyl, alprazolam, risperidone, bumetanide, bisoprolol) evokes a given response at low concentrations, while a drug of lower potency ( meperidine, diazepam, ziprasidone, furosemide, metoprolol) evokes the same response only at higher concentrations. Higher potency does not necessarily mean greater effectiveness or more side effects. The IUPHAR has stated that 'potency' is ''"an imprecise term that should always be further defined"'', for instance as EC_, IC_, ED_, LD_ and so on. See also * Reaction inhibitor § Potency References F ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Succinic Acid
Succinic acid () is a dicarboxylic acid with the chemical formula (CH2)2(CO2H)2. The name derives from Latin ''succinum'', meaning amber. In living organisms, succinic acid takes the form of an anion, succinate, which has multiple biological roles as a metabolic intermediate being converted into fumarate by the enzyme succinate dehydrogenase in complex 2 of the electron transport chain which is involved in making ATP, and as a signaling molecule reflecting the cellular metabolic state. It is marketed as food additive E363. Succinate is generated in mitochondria via the tricarboxylic acid cycle (TCA). Succinate can exit the mitochondrial matrix and function in the cytoplasm as well as the extracellular space, changing gene expression patterns, modulating epigenetic landscape or demonstrating hormone-like signaling. As such, succinate links cellular metabolism, especially ATP formation, to the regulation of cellular function. Dysregulation of succinate synthesis, and therefore ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
