Abstract：
:Mammalian cells are commonly employed in screening assays to identify active compounds that could potentially affect the progression of different human diseases including retinitis pigmentosa (RP), a class of inherited diseases causing retinal degeneration with compromised vision. Using transcriptome analysis, we compared NIH3T3 cells expressing wildtype (WT) rod opsin with a retinal disease-causing single P23H mutation. Surprisingly, heterologous expression of WT opsin in NIH3T3 cells caused more than a 2-fold change in 783 out of 16,888 protein coding transcripts. The perturbed genes encoded extracellular matrix proteins, growth factors, cytoskeleton proteins, glycoproteins and metalloproteases involved in cell adhesion, morphology and migration. A different set of 347 transcripts was either up- or down-regulated when the P23H mutant opsin was expressed suggesting an altered molecular perturbation compared to WT opsin. Transcriptome perturbations elicited by drug candidates aimed at mitigating the effects of the mutant protein revealed that different drugs targeted distinct molecular pathways that resulted in a similar phenotype selected by a cell-based high-throughput screen. Thus, transcriptome profiling can provide essential information about the therapeutic potential of a candidate drug to restore normal gene expression in pathological conditions.
journal_name
Pharmacol Resjournal_title
Pharmacological researchauthors
Chen Y,Brooks MJ,Gieser L,Swaroop A,Palczewski Kdoi
10.1016/j.phrs.2016.10.031subject
Has Abstractpub_date
2017-01-01 00:00:00pages
1-13eissn
1043-6618issn
1096-1186pii
S1043-6618(16)30959-8journal_volume
115pub_type
杂志文章abstract：:Diabetic erectile dysfunction (DED) hugely affected the patients' sexual life quality. However, there are no satisfactory therapeutic methods and intervention targets for this subtype of erectile dysfunction (ED). Inspired by the clinical practice of traditional Chinese medicine (TCM), we found that hirudin, the main ...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2020.105244
更新日期：2021-01-01 00:00:00
abstract：:Excess fructose consumption causes high prevalence of metabolic syndrome and inflammatory liver diseases. The aim of the current study was to investigate the therapeutic effects and underlying molecular mechanisms of curcumin and allopurinol in high fructose-induced hepatic inflammation. Male Sprague-Dawley rats were ...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2018.09.021
更新日期：2018-11-01 00:00:00
abstract：:Outbreak and pandemic of coronavirus SARS-CoV-2 in 2019/2020 will challenge global health for the future. Because a vaccine against the virus will not be available in the near future, we herein try to offer a pharmacological strategy to combat the virus. There exists a number of candidate drugs that may inhibit infect...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2020.104859
更新日期：2020-07-01 00:00:00
abstract：:Recent studies have shown that a higher consumption of green tea leads to a lower prevalence of depressive symptoms in elderly individuals. However, no studies have explored the antidepressant-like effect of green tea in preclinical models of depression. The aim of this study was to investigate the antidepressant-like...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2011.09.007
更新日期：2012-01-01 00:00:00
abstract：:The aim of this review is to underline the redundancy of down-regulation pathways for p53, at the light of the two more important degradative systems: calpains and ubiquitin-dependent pathways. The MDM2 feed-back loop is also illustrated, as well as the phosphorylative/dephosphorylative regulation of the latent and ac...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1006/phrs.1997.0269
更新日期：1998-02-01 00:00:00
abstract：:Changes in vascular responsiveness are the basis for some of the cardiovascular complications in cholestasis. Since the duration of cholestasis is important in determining the degree of the complications, we investigated the time-course dependent evolution of vascular relaxation responsiveness in the aortic rings of c...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.2001.0892
更新日期：2001-12-01 00:00:00
abstract：:Endothelial dysfunction (ED), an established response to cardiovascular risk factors, is characterized by increased levels of soluble molecules secreted by endothelial cells (EC). Evidence suggest that ED is an independent predictor of cardiac events and that it is associated with a deficiency in production or bioavai...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2017.01.022
更新日期：2017-05-01 00:00:00
abstract：:We aimed to elucidate the role of vitamin D supplementation on adipokines through a systematic review and a meta-analysis of randomized placebo-controlled trials (RCTs). The search included PUBMED, Scopus, Web of Science and Google Scholar through July 1st, 2015. Finally we identified 9 RCTs and 484 participants. Meta...
journal_title：Pharmacological research
pub_type： 杂志文章,meta分析,评审
doi：10.1016/j.phrs.2016.03.035
更新日期：2016-05-01 00:00:00
abstract：:The effects of ethanol (EEP) and water (WSD) extracts of propolis collected from north China on blood glucose, blood lipid and free radicals in rats with diabetes mellitus were studied. The results show that EEP and WSD led to decreased levels of blood glucose (FBG), fructosamine (FRU), malonaldehyde (MDA), nitric oxi...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2004.06.011
更新日期：2005-02-01 00:00:00
abstract：:Progressive neuronal death is the key pathogenic event leading to clinical symptoms in neurodegenerative disorders (NDDs). Neuroprotective treatments are virtually unavailable, partly because of the marked internal heterogeneity of the mechanisms underlying pathology. Targeted neuroprotection would require deep mechan...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2019.104343
更新日期：2019-09-01 00:00:00
abstract：:Oxidative stress is related to the progression of renal diseases and modulation of oxidative stress can lead to a reduction in vascular events in patients with chronic renal insufficiency (CRI). Indoxyl sulfate (IS) and xanthine oxidase (XO) are related to impaired neovasculogenesis in CRI. Hydralazine is suggested fo...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2019.104509
更新日期：2020-01-01 00:00:00
abstract：:In the isolated myometrium obtained from pregnant women, diphenylhydantoin inhibited both spontaneous and K(+)-evoked contractions within the same range of potency. Nicardipine was less effective in inhibiting spontaneous than K(+)-induced contractions, whereas trifluoperazine was only effective against spontaneous co...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/s1043-6618(05)80051-9
更新日期：1990-09-01 00:00:00
abstract：:The formation of reactive oxygen species (ROS) appears to play a significant role in many pathological states including cystic fibrosis and asthma. Although stimulated inflammatory cells represent a major source of oxygen metabolites and these cells are able to generate the potent oxidant hypochlorous acid (HOCl) effe...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.1999.0628
更新日期：2000-05-01 00:00:00
abstract：:Cosmetics are largely diffused substances topically applied to wash, to perfume or to improve the look, nevertheless the number of reported adverse reactions is very low, probably because of underreporting. This could be due to self-diagnosis and self-medication that is common in the presence of not severe reactions. ...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2005.08.003
更新日期：2006-01-01 00:00:00
abstract：:Sumatriptan is a 5-HT1B/D receptor agonist of documented efficacy in relieving migraine and associated symptoms such as nausea and vomiting. In the past decade, several studies reported an important delay of gastric emptying induced by sumatriptan in healthy humans. The impact of this gastric motor effect of sumatript...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1006/phrs.2000.0766
更新日期：2001-03-01 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：:There is evidence that hydrazine, a metabolite of isoniazid, plays an important role in the mechanism of isoniazid-induced hepatotoxicity. Hydrazine has been reported to be metabolised by NADPH cytochrome P-450 reductase (reductase) to reactive and potentially toxic intermediates. The present study was designed, using...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.1998.0347
更新日期：1998-09-01 00:00:00
abstract：AIM:Acute myocardial infarction and subsequent post-infarction heart failure are among the leading causes of mortality worldwide. The endocannabinoid system has emerged as an important modulator of cardiovascular disease, however the role of endocannabinoid metabolic enzymes in heart failure is still elusive. Herein, w...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/j.phrs.2019.104578
更新日期：2020-01-01 00:00:00
abstract：:In previous studies we observed an enhanced anti-inflammatory activity of MPEG-SOD derivatives in acute inflammation in rat. To assess the activity in chronic inflammation we tested the compound with longer half-life (MPEG-SOD 18) in complete adjuvant arthritis in rat. According to the prophylactic schedule of treatme...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1016/s1043-6618(05)80106-9
更新日期：1991-01-01 00:00:00
abstract：:Boldo (Peumus boldus Mol.), a Chilean tree traditionally employed in folk medicine and recognized as a herbal remedy in a number of pharmacopoeias, mainly for the treatment of liver ailments, has recently been the subject of increasing attention. Boldine, in particular, the major and most characteristic alkaloidal con...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/1043-6618(94)80093-6
更新日期：1994-01-01 00:00:00
abstract：UNLABELLED:The purpose of this study was an attempt to extrapolate favorable observations on the effects of magnesium on platelets and haemostasis from animal models to humans. Intravenous magnesium in the treatment of acute myocardial infarction has been tested in several large clinical trials and remains controversia...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.1997.0212
更新日期：1997-07-01 00:00:00
abstract：:The epidemic of pneumonia (COVID-19) caused by novel coronavirus (SARS-CoV-2) infection has been listed as a public health emergency of international concern by the World Health Organization (WHO), and its harm degree is defined as a global "pandemic". At present, the efforts of various countries focus on the rapid di...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2020.104929
更新日期：2020-08-01 00:00:00
abstract：:Pulsatilla Decoction (Bai-Tou-Weng-Tang) has been used medically in China for thousands of years for the treatment of diseases caused by bacteria. In recent decades, Pulsatilla Decoction is becoming a well-known formula prescription used for the treatment of ulcerative colitis in traditional Chinese medicine. Pulsatil...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2020.105079
更新日期：2020-10-01 00:00:00
abstract：:This study was performed in order to investigate the cholinomimetic response of seminal vesicles isolated from rats treated with hydrocortisone acetate during perinatal life. At the adult phase, the body weight and the wet weight of the seminal vesicle of these animals were unchanged. However, these male rats exhibite...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：
更新日期：2003-07-01 00:00:00
abstract：:The role of the angiotensin AT1 receptors in certain behavioural effects of angiotensin II (Ang II), using their selective antagonist losartan (DuP 753), was assessed. Ang II, given intracerebroventricularly (ICV) at the dose of 1 nmole, significantly improved object recognition, learning of conditioned avoidance resp...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.1996.0073
更新日期：1996-09-01 00:00:00
abstract：:As an essential component of the innate immune system, Toll-like receptors (TLRs) are a family of well-recognized ligand-binding receptors found in various organisms and initiate host immune responses. Activation of TLRs signaling pathways lead to the induction of numerous genes that function in host defense. Baicalin...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2020.104890
更新日期：2020-08-01 00:00:00
abstract：:The investigation was aimed at investigating whether the dopaminergic projection arriving at the nucleus septi lateralis (NSL) is involved in the facilitatory effect of vasopressin (AVP) on memory retrieval. The bilateral 6-OHDA lesions to the NSL were made in 20 male Wistar rats before testing the intracerebroventric...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.1997.0280
更新日期：1998-02-01 00:00:00
abstract：:Hypercalcemia and hypercalciuria observed both in humans and in animals who were on long-term theophylline therapy, prompted us to investigate whether oral theophylline treatment at optimal doses causes any adverse side effects on bone metabolism in mild asthmatics. Therefore, serum osteocalcin (BGP) and total alkalin...
journal_title：Pharmacological research
pub_type： 杂志文章
doi：10.1006/phrs.1999.0486
更新日期：1999-08-01 00:00:00
abstract：:A pharmacokinetic study of the metabolic profile of resveratrol has been performed in healthy men after moderate red wine (RW) consumption. The bioavailability of resveratrol is highly influenced by several factors such as the food matrix and, therefore, this study has been compared with a pilot study in which men ing...
journal_title：Pharmacological research
pub_type： 杂志文章,随机对照试验
doi：10.1016/j.phrs.2012.08.001
更新日期：2012-11-01 00:00:00
abstract：:Protein kinase C (PKC) is a family of kinases that are critical in many cellular events. These enzymes are activated by lipid-derived second messengers, are dependent on binding to negatively charged phospholipids and some members also require calcium to attain full activation. The interaction with lipids and calcium ...
journal_title：Pharmacological research
pub_type： 杂志文章,评审
doi：10.1016/j.phrs.2007.04.014
更新日期：2007-06-01 00:00:00
