About: Decades-old renin inhibitors are still struggling to find a niche in antihypertensive therapy. A fleeting look at the old and the promising new molecules

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About: Decades-old renin inhibitors are still struggling to find a niche in antihypertensive therapy. A fleeting look at the old and the promising new molecules Goto Sponge NotDistinct Permalink

An Entity of Type : schema:ScholarlyArticle, within Data Space : wasabi.inria.fr associated with source document(s)

Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	Decades-old renin inhibitors are still struggling to find a niche in antihypertensive therapy. A fleeting look at the old and the promising new molecules
Creator	Prashantha Kumar, B Ramya, Krishnappa Sridhara Murthy, N Suresh, Ramalingam Yogish Kumar, Honnavalli
Source	Elsevier; Medline; PMC
abstract	Hypertension is a diverse illness interlinked with cerebral, cardiovascular (CVS) and renal abnormalities. Presently, the malady is being treated by focusing on Renin- angiotensin system (RAS), voltage-gated calcium channels, peripheral vasodilators, renal and sympathetic nervous systems. Cardiovascular and renal abnormalities are associated with the overactivation of RAS, which can be constrained by angiotensin- converting enzyme inhibitors (ACEIs), angiotensin II (Ang-II) -AT1 receptor blockers (ARBs) and renin inhibitors. The latter is a new player in the old system. The renin catalyzes the conversion of angiotensinogen to Angiotensin I (Ang-I). This can be overcome by inhibiting renin, a preliminary step, eventually hinders the occurrence of the cascade of events in the RAS. Various peptidomimetics, the first-generation renin inhibitors developed six decades ago have limited drug-like properties as they suffered from poor intestinal absorption, high liver first-pass metabolism and low oral bioavailability. The development of chemically diverse molecules from peptides to nonpeptides expanded the horizon to achieving direct renin inhibition. Aliskiren, a blockbuster drug that emerged as a clinical candidate and got approved by the US FDA in 2007 was developed by molecular modeling studies. Aliskiren indicated superior to average efficacy and with minor adverse effects relative to other RAS inhibitors. However, its therapeutic use is limited by poor oral bioavailability of less than 2% that is similar to first-generation peptidic compounds. In this review, we present the development of direct renin inhibitors (DRIs) from peptidic to nonpeptidics that lead to the birth of aliskiren, its place in the treatment of cardiovascular diseases and its limitations.
has issue date	2020-03-28(xsd:dateTime)
bibo:doi	10.1016/j.bmc.2020.115466
bibo:pmid	32247750
has license	no-cc
sha1sum (hex)	19e18a7c27512439dac91fc1096937fd03496c13
schema:url	https://doi.org/10.1016/j.bmc.2020.115466
resource representing a document's title	Decades-old renin inhibitors are still struggling to find a niche in antihypertensive therapy. A fleeting look at the old and the promising new molecules
has PubMed Central identifier	PMC7112834
has PubMed identifier	32247750
schema:publication	Bioorg Med Chem
resource representing a document's body	covid:19e18a7c27512439dac91fc1096937fd03496c13#body_text
is schema:about of	named entity 'FLEETING' named entity 'conversion' named entity 'catalyzes' named entity 'suffered' named entity 'Cardiovascular' named entity 'ARBs' named entity 'developed' named entity 'FDA' named entity 'STEP' named entity 'ANGIOTENSIN II' named entity 'EXPANDED ' named entity 'RENAL ABNORMALITIES' named entity 'SYSTEM' named entity 'PRESENTLY' named entity 'REVIEW' named entity 'RENAL' named entity 'HYPERTENSION' named entity 'DEVELOPMENT' named entity 'HORIZON' named entity 'LEAD' named entity 'CLINICAL' named entity 'ASSOCIATED WITH' named entity 'APPROVED BY' named entity 'NICHE' named entity 'GENERATION' named entity 'CEREBRAL' named entity 'ADVERSE EFFECTS' named entity 'MOLECULES' named entity 'RENIN INHIBITORS' named entity 'OLD' named entity 'MOLECULAR MODELING' named entity 'MOLECULES' named entity 'THERAPEUTIC USE' named entity 'LIKE' named entity 'RENIN-ANGIOTENSIN SYSTEM' named entity 'ILLNESS' named entity 'SUFFERED' named entity 'CHEMICALLY' named entity 'DRUG' named entity 'RENIN' named entity 'LOOK' named entity 'NEW' named entity 'CONSTRAINED' named entity 'INTESTINAL ABSORPTION' named entity 'MINOR' named entity 'BEING' named entity 'PRELIMINARY' named entity 'SIMILAR' named entity 'EFFICACY' named entity 'TREATMENT' named entity 'ANTIHYPERTENSIVE THERAPY' named entity 'TREATED' named entity 'LIMITED BY' named entity 'RELATIVE TO' named entity 'VARIOUS' named entity 'CANDIDATE' named entity 'CONVERSION' named entity 'CARDIOVASCULAR' named entity 'LESS THAN' named entity 'INHIBITING' named entity 'SUPERIOR' named entity 'AGO' named entity 'LIMITATIONS' named entity 'ORAL BIOAVAILABILITY' named entity 'ITS' named entity 'MALADY' named entity 'INDICATED' named entity 'INHIBITORS' named entity 'LIVER' named entity 'BIRTH' named entity 'FOCUSING' named entity 'EVENTS' named entity 'ANGIOTENSINOGEN' named entity 'LOW' named entity 'CARDIOVASCULAR DISEASES' named entity 'PROPERTIES' named entity 'SYMPATHETIC NERVOUS SYSTEMS'

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