Careful analysis of the sEH N -terminal domain architectural and structural features combined with preliminary results obtained by Grant and coworkers on farnesol derivative inhibitors, allowed us to design potential inhibitors for the catalytic function of this part of the enzyme. (uconn.edu)
The most potent arylquinuclidine derivative (3-[1'-{4'-(benzyloxy)-phenyl}]-quinuclidine-2-ene) (WSP1267) had a MIC 50 of 2 μg/ml for all species tested and MIC 90 varying from 4 μg/ml to 8 μg/ml. (biomedcentral.com)
Antifungal2
BACKGROUND: Farnesol is a Candida-secreted quorum-sensing molecule of great interest as a potential antifungal agent for serious and hardly curable infections-candidiasis, especially vulvovaginal candidiasis (VVC). (bvsalud.org)
The aim of this study was to evaluate the antifungal activity of SQS inhibitors on Candida albicans , Candida tropicalis and Candida parapsilopsis strains. (biomedcentral.com)
Antiproliferative1
Ten arylquinuclidines that act as SQS inhibitors were tested as antiproliferative agents against three ATCC strains and 54 clinical isolates of Candida albicans , Candida tropicalis and Candida parapsilopsis . (biomedcentral.com)
METHODS1
METHODS: The effect of farnesol on cellular morphology and viability and evaluated the production of Th1 (IL-2), Th2 (IL-4), proinflammatory (IL-6), chemotactic (IL-8), and Th17 (IL-17) cytokines in the culture supernatants of vaginal epithelial cell line (VK2) were evaluated. (bvsalud.org)
In addition, farnesol and farnesyl acetone fulfilled most of the ADME and drug-likeness properties, indicating their activity. (bvsalud.org)
SAR analysis that analogues with three or more isoprene units or a long aliphatic chain exhibited the most potent activity. (bvsalud.org)
Squalene3
Description: NB-598 is a potent competitive inhibitor of squalene epoxidase (SE). (10genomics.com)
The squalene synthase inhibitor squalestatin 1 (Squal1) is a potent and efficacious inducer of CYP2B expression in primary cultured rat hepatocytes and rat liver. (nih.gov)
A capillary gas chromatography-mass spectrometric (GC-MS) method in human urine has been developed and validated for the quantitative determination of dicarboxylic acids (dioic acids) which are produced in the body as a consequence of the administration of an inhibitor of the enzyme squalene synthase, which is involved in the biosynthesis of cholesterol. (nih.gov)
Mycobacterium1
Geranylgeraniol is a potent inhibitor of Mycobacterium tuberculosis in vitro. (wikipedia.org)
Protease2
Thus, remnant chymase (but not isolated chymase) was able to resist the natural protease inhibitors present in serum and in intimal fluid. (jci.org)
DDL-701 thus represents an excellent drug candidate that can immediately be repurposed and undergo clinical evaluation as a PL pro inhibitor, that most effectively in the clinic may be used in a protease inhibitor cocktail with an M pro inhibitor such as nirmatrelvir (Paxlovid) for the treatment of COVID-19. (fortunejournals.com)
Geranylgeraniol1
In the protocol presented here, the monophosphates and diphosphates of farnesol, geranylgeraniol and phytol are isolated from plant material with an isopropanol-containing buffer and quantified by LC-MS using citronellyl-P and citronellyl-PP as internal standards. (bvsalud.org)
Pathway3
The mevalonate/isoprenoid pathway inhibitor apomine (SR-45023A) is antiproliferative and induces apoptosis similar to farnesol. (ncats.io)
NB-598 suppresses triglyceride biosynthesis through the farnesol pathway. (10genomics.com)
2. Chemopreventive effect of farnesol on DMBA/TPA-induced skin tumorigenesis: involvement of inflammation, Ras-ERK pathway and apoptosis. (nih.gov)
Biosynthesis1
Treatment with inhibitors of different steps of cholesterol biosynthesis attenuated CITCO-mediated CYP2B6 induction in HepaRG cells, and Prava treatment increased HMGCR expression and inhibited CYP2B6 induction with comparable potency. (nih.gov)
Induce1
Further, the potent abilities of tocotrienols to induce cell cycle arrest (Wada et al. (biomedcentral.com)
Therapeutic2
These inhibitors may have therapeutic application in the treatment of various types of cancers. (c-metinhibitors.com)
Melanoma differentiation-associated gene-7/interleukin-24 ( mda -7/IL-24) is a potent cancer gene therapeutic because of its broad-spectrum cancer-specific apoptosis-inducing properties as well as its multipronged indirect antitumor activities. (aacrjournals.org)
Vitro2
Farnesol is glucuronidated in human liver, kidney and intestine in vitro, and is a novel substrate for UGT2B7 and UGT1A1. (ncats.io)
Although PPi was unable to do this, BPs turned out to be remarkably effective inhibitors of bone resorption, both in vitro and in vivo experimental systems, and eventually in humans. (nih.gov)
Cholesterol1
The belief that low-density lipoprotein (LDL) cholesterol causes atherosclerosis and subsequent heart disease is a fundamental Cholesterol, contrary to its popular image as a potent enemy of precept of modern medicine. (onlinepdfcatalog.com)
Farnesol, (2E,6E)- is an isoprenoid found in many aromatic plants and is also produced in humans, where it acts on numerous nuclear receptors and has received considerable attention due to its apparent anticancer properties. (ncats.io)
As ever more potent BPs were synthesised and studied, it became apparent that physico-chemical effects were insufficient to explain their biological effects, and that cellular actions must be involved. (nih.gov)
Resist1
Bisphosphonates are chemically stable analogues of inorganic pyrophosphate (PPi), and it was studies on the role of PPi as the body's natural 'water softener' in the control of soft tissue and skeletal mineralisation that led to the need to find inhibitors of calcification that would resist hydrolysis by alkaline phosphatase. (nih.gov)
Clinical2
Safety So far, Decitabine 1069-66-5 the safety profile of SGLT2 inhibitors reported from clinical studies seems to meet expectations.33,34,55,40,58 SGLT2 inhibitors are,intended, to target a very certain membrane transporter that is definitely practically exclusively expressed inside the renal tubules. (c-metinhibitors.com)
Through screening of a custom clinical compound library, we identified eltrombopag (DDL-701), a thrombopoietin receptor agonist, as having PL pro inhibitory activity that is sustained in the presence of the M pro inhibitor nirmatrelvir. (fortunejournals.com)
Identification1
Identification of a nuclear receptor that is activated by farnesol metabolites. (ncats.io)
Humans1
Farnesol is subject to restrictions on its use in perfumery as some people may become sensitized to it, however, the evidence that farnesol can cause an allergic reaction in humans is disputed. (ncats.io)
Natural1
Farnesol is a natural pesticide for mites and is a pheromone for several other insects. (ncats.io)
Agent1
Farnesol has been suggested to function as a chemopreventative and anti-tumor agent. (ncats.io)
Effect2
12. Chemopreventive effect of a novel, selective TACE inhibitor on DMBA- and TPA-induced skin carcinogenesis. (nih.gov)
In the current study, we described the design and synthesis of 2,3,4,6-tetrachloro-5-cyanophenyl GSL (TCPG), an artificial GSL bearing a chlorothalonil moiety as a potent inhibitor of GTRs, and evaluated its inhibitory effect on the substrate uptake mediated through GTR1 and GTR2. (bvsalud.org)