Abstract：
:A substantial number of G-protein coupled receptors (GPCRs) genetic disorders are due to mutations that cause misfolding or dysfunction of the receptor product. Pharmacological chaperoning approaches can rescue such mutant receptors by stabilizing protein conformations that behave similar to the wild type protein. For example, this can be achieved by improving folding efficiency and/or interaction with chaperone proteins. Although efficacy of pharmacological chaperones has been demonstrated in vitro for a variety of GPCRs, translation to clinical use has been limited. In this paper we discuss the history of pharmacological chaperones of GPCR's and other membrane proteins, the challenges in translation to the clinic, and the use of different assays for pharmacological chaperone discovery.
journal_name
Pharmacol Resjournal_title
Pharmacological researchauthors
Beerepoot P,Nazari R,Salahpour Adoi
10.1016/j.phrs.2016.12.036subject
Has Abstractpub_date
2017-03-01 00:00:00pages
242-251eissn
1043-6618issn
1096-1186pii
S1043-6618(16)31409-8journal_volume
117pub_type
杂志文章,评审abstract：:ABT-737, ABT-263 (Navitoclax) and ABT-199 (Venetoclax) are under intensive preclinical and clinical investigation as treatments for hematologic and other malignancies. These small molecules mimic pro-death B-cell lymphoma-2 (Bcl-2) Homology 3 (BH3) domain-only proteins. They also bear a structural resemblance to certa...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2019.01.040
更新日期：2019-04-01 00:00:00
abstract：:Postnatal bone marrow contains a subtype of unique progenitor cells that have the capacity to differentiate into functional endothelial cells. Hence, these cells have been termed endothelial progenitor cells (EPCs). In general, circulating EPCs were characterized by the expression of CD133, CD34 and the vascular endot...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2008.07.008
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abstract：:Despite the evolving advances in clinical approaches to obesity and its inherent comorbidities, the therapeutic challenge persists. Among several pharmacological tools already investigated, recent studies suggest that melatonin supplementation could be an efficient therapeutic approach in the context of obesity. In th...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2020.105254
更新日期：2021-01-01 00:00:00
abstract：:TNF-related apoptosis-inducing ligand (TRAIL) selectively induces the apoptosis pathway in tumor cells leading to tumor cell death. Because TRAIL induction can kill tumor cells, cancer researchers have developed many agents to target TRAIL and some of these agents have entered clinical trials in oncology. Unfortunatel...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
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abstract：:Pulmonary fibrosis is a chronic condition characterized by progressive scarring of lung parenchyma. The aim of this study was to examine the effects of an ultramicronized preparation of palmitoylethanolamide (PEA-um(®)), an endogenous fatty acid amide, in mice subjected to idiopathic pulmonary fibrosis. Idiopathic pul...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2016.07.010
更新日期：2016-09-01 00:00:00
abstract：:Since the regenerative capacity of the adult mammalian heart is limited, cardiac injury leads to the formation of scar tissue and thereby increases the risk of developing compensatory heart failure. Stem cell therapy is a promising therapeutic approach but is facing problems with engraftment and clinical feasibility. ...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2017.07.020
更新日期：2018-01-01 00:00:00
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journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2018.11.040
更新日期：2019-01-01 00:00:00
abstract：:Macroscale delivery systems that can be locally implanted on the tumor tissue as well as avoid all the complications associated to the systemic delivery of therapeutics have captured researchers' attention, in recent years. Particularly, the microneedle-based devices can be used to efficiently deliver both small and m...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
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abstract：:HMG-CoA reductase inhibitors (statins) have been shown to improve cardiovascular (CV) outcomes in the general population as well as in patients with cardiovascular disease (CVD). Statins' beneficial effects have been attributed to both cholesterol-lowering and cholesterol-independent "pleiotropic" properties. By their...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2014.06.011
更新日期：2014-10-01 00:00:00
abstract：:A global transcriptional regulator, MgrA, was previously identified as a key determinant of virulence in Staphylococcus aureus. An 80% EtOH extract of Uncaria gambier was found to attenuate the virulence of S. aureus via its effects on MgrA. Using bioassay-guided fractionation, a polyphenolic polymer, uncariitannin, w...
journal_title：Pharmacological research
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abstract：:Photodynamic therapy (PDT) using 5-aminolevulinic acid (ALA)-induced protoporphyrin IX may play a role in the treatment of dysplastic Barrett's oesophagus. An ALA thermosetting gel Pluronic F-127) was developed and evaluated in an in vivo mouse model for potential use in PDT of Barrett's mucosa. In vitro studies of th...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.2001.0934
更新日期：2002-02-01 00:00:00
abstract：:The pharmacokinetics of doxycycline hydrochloride (DoxHcl) at a dose of 5 mg kg-1 BW was studied after an intravenous (i.v.) bolus and intramuscular (i.m.) injections in non lactating goats. A microbiological assay employing Bacillus subtilis as the test organism was used to measure its concentrations in serum and uri...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2003.10.012
更新日期：2004-05-01 00:00:00
abstract：:Perfusion of all mammalian heart muscle except hamster with Ca(2+)-free Tyrode and thereafter reperfusion with normal Tyrode causes irreversible damage, the calcium paradox. Our study aims at deciphering the role of creatine kinase, high energy phosphates and Ca(2+)influx in the genesis of myocardial injury in the rat...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.1999.0595
更新日期：2000-03-01 00:00:00
abstract：:We aimed to investigate the cardiac changes in patients with human epidermal growth factor receptor 2 (HER2)-positive breast cancer treated with trastuzumab in an adjuvant setting. Two hundred and fifty-three women with HER2-positive breast cancer were included. The assessment of cardiovascular system and echocardiogr...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2013.10.001
更新日期：2013-12-01 00:00:00
abstract：:The intestinal barrier function depends on an adequate response to pathogens by the epithelium. Toll-like receptor 3 (TLR-3) recognizes double-stranded RNA, a virus-associated molecular pattern. Activation of TLR-3 with Poly(I:C), a synthetic agonist, modulates tissue repair and permeability in other epithelia; howeve...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2015.06.016
更新日期：2015-11-01 00:00:00
abstract：:Quiescent hepatic stellate cell (HSC) activation and subsequent conversion into myofibroblasts is the central event in hepatic fibrosis pathogenesis. Epithelial-mesenchymal transition (EMT), another vital participant in liver fibrosis, has the potential to initiate HSC activation, which promotes abundant myofibroblast...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2017.10.013
更新日期：2018-02-01 00:00:00
abstract：:Plasma lipid and lipoprotein levels were evaluated in 27 adults with essential hypertension at four different periods during a 12-month treatment with doxazosin. Mean plasma total cholesterol (TC), low-density lipoprotein-cholesterol (LDLC), triglyceride (TG), very low density lipoprotein-cholesterol (VLDLC) and the L...
journal_title：Pharmacological research
pub_type： 临床试验,杂志文章
doi：10.1016/1043-6618(94)80108-8
更新日期：1994-10-01 00:00:00
abstract：:To assess the potential role of vasoactive cardiac eicosanoids in the modulation of coronary flow, we measure thromboxane(TX)B2, 6-keto-prostaglandin(PG)F1 alpha, PGE2 and sulphido-peptide leukotrienes (LTC4, D4, E4) in the coronary effluent of isolated perfused rat heart in both baseline and post-ischaemic conditions...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/1043-6618(92)90233-2
更新日期：1992-12-01 00:00:00
abstract：:Tumor metastasis is a key cause of cancer mortality, and inhibiting migration of cancer cells is one of the major directions of anti-metastatic drug development. Calumenin and fibulin-1 are two extracellular proteins that synergistically inhibit cell migration and tumor metastasis, and could potentially be served as t...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2015.05.001
更新日期：2015-09-01 00:00:00
abstract：:Leukocyte arylsulphatase A (AS-A) was shown to be significantly high in newly-diagnosed breast cancer patients. Previous reports imply a connection between serum interleukin-6 (IL-6) and breast cancer, possibly through a modulation of enzymes involved in estrogen synthesis. Abnormal distribution of heparan sulphate pr...
journal_title：Pharmacological research
pub_type： 临床试验,杂志文章
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更新日期：2005-10-01 00:00:00
abstract：:The antinociceptive and motor effects of the hydrophilic alpha 2-adrenoceptor agonist ST-91 were studied after intrathecal administration to male Wistar rats in different heat-pain tests and different test settings. Intrathecal administration of ST-91 caused a dose-dependent increase in hind paw licking latency in the...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.1997.0188
更新日期：1997-06-01 00:00:00
abstract：:This paper examines the effect of biphenylacetic acid on the antagonistic action of norfloxacin and enoxacin on the GABA(A)-mediated responses of the isolated guinea-pig ileum. GABA produced transient contractions followed by relaxation. The contractile effect of exogenously applied GABA was concentration-dependent wi...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.2001.0853
更新日期：2001-09-01 00:00:00
abstract：:Possible interaction between adenosine and L type Ca2+ channel in the locomotor activity of rats was investigated. R-PIA (0.05 mg kg-1), an adenosine analogue, and caffeine (20 mg kg-1), an adenosine receptor antagonist, significantly decreased and increased locomotor activity, respectively. Ca2+ channel blocker nifed...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.1996.0021
更新日期：1996-02-01 00:00:00
abstract：:Alzheimer's disease is the fourth largest cause of death for people over 65 years of age. Dementia of Alzheimer's type is the commonest form of dementia, the other two forms being vascular dementia and mixed dementia. At present, the therapy of Alzheimer's disease is aimed at improving both, cognitive and behavioural ...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2004.05.005
更新日期：2005-01-01 00:00:00
abstract：:Pharmacokinetics is a relatively young branch of the life sciences, which has developed rapidly in the last 15-20 years, thanks to a series of analytical achievements that have allowed drug concentrations to be measured in biological matrices with highly selective and sensitive methods. Most old drugs and all new drug...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1006/phrs.1997.0254
更新日期：1997-12-01 00:00:00
abstract：:The first studies of histamine and diabetes date back to the 1950s. Since that time the involvement of histamine in diabetes was related to its well known vasoactive properties and permeability leakage effects. In particular, the first evidence for a correlation between histamine and diabetes arose in 1989 when an inc...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2016.06.021
更新日期：2016-09-01 00:00:00
abstract：:QiShenYiQi Pills (QSYQ) is a compound Chinese medicine widely used in China for treatment of cardiovascular disease. However, limited data are available regarding the anti-fibrotic role of QSYQ after ischemia/reperfusion (I/R) injury. This study aimed to investigate the effect of post-treatment with QSYQ on myocardial...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2019.104272
更新日期：2019-08-01 00:00:00
abstract：:The hepatoprotective effects of acetylbergenin were examined against D -galactosamine (GalN)-induced liver damage in rats, compared with that of bergenin reported previously. Acetylbergenin was synthesized from acetylation of bergenin, isolated from Mallotus japonicus, to increase lipophilic and physiological activiti...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.2000.0730
更新日期：2000-11-01 00:00:00
abstract：:As Traditional Chinese Medicine (TCM) transcends its cultural boundaries and becomes widely used in many countries around the world, one of the major risks to the growing use of TCM internationally is the damage caused to its reputation and to community safety when TCM practitioners are not adequately trained. Ensurin...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2020.105217
更新日期：2020-11-01 00:00:00
abstract：:Cancer cell mutations can be identified by genomic and transcriptomic techniques. However, they are not sufficient to understand the full complexity of cancer heterogeneity. Analyses of proteins expressed in cancers and their modification profiles show how these mutations could be translated at the functional level. P...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2020.105091
更新日期：2020-10-01 00:00:00
