Abstract：
:The non-nucleoside reverse transcriptase inhibitors (NNRTIs) are allosteric inhibitors of HIV-1 reverse transcriptase and are classified into generations depending on their discovery and resistance profiles. The NNRTIs are used in combination regimens with antiretroviral agents that target two or more enzymes in the viral life cycle. The combination regimens usually include a backbone of two nucleoside or nucleotide reverse transcriptase inhibitors and a third core agent among the NNRTIs or protease inhibitors. The combination regimens are maintained over long durations and consequently lead to long-term problems, including toxicity, drug-drug interactions, and increasing costs. This brief overview summarizes the pharmacokinetic profiles for NNRTIs and NNRTI-based combination regimens.
journal_name
Curr Opin Pharmacoljournal_title
Current opinion in pharmacologyauthors
Vanangamudi M,Kurup S,Namasivayam Vdoi
10.1016/j.coph.2020.10.009subject
Has Abstractpub_date
2020-10-01 00:00:00pages
179-187eissn
1471-4892issn
1471-4973pii
S1471-4892(20)30107-7journal_volume
54pub_type
杂志文章,评审abstract：:Interferon-alpha-based therapies are the mainstay of hepatitis C treatment. However, these broad immunomodulatory agents, already limited by their side effects, expense and route of administration, are not efficacious in all cases. Therefore, research efforts have focused on identifying additional drugs and therapeuti...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2004.07.003
更新日期：2004-10-01 00:00:00
abstract：:Heteromerization of dopamine receptors has been shown for both the D(1)/D(5) and D(2)/D(3)/D(4) receptor families, which couple positively and negatively, respectively, to adenylyl cyclase. The present article reviews data on dopamine heteromers formed by D(3), focusing in particular on associations with their D(2) co...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2009.10.001
更新日期：2010-02-01 00:00:00
abstract：:Successful cancer therapy requires the selective killing of cancer cells. Many molecular components of the pathways that lead to cell death have recently been identified and a number of these, including p53, Apaf-1, and members of the inhibitor of apoptosis protein and Bcl-2 gene families, have been found to be altere...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/s1471-4892(01)00059-5
更新日期：2001-08-01 00:00:00
abstract：:Bone remodelling is an essential process for shaping and maintaining bone mass in the mature skeleton. During our lifetime bone is constantly being removed by osteoclasts and new bone is formed by osteoblasts. The activities of osteoclasts and osteoblasts must be regulated under a strict balance to ensure that bone ho...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2016.02.003
更新日期：2016-06-01 00:00:00
abstract：:The molecular genetics of Barrett's esophagus (BE) and its evolution to esophageal adenocarcinoma (EAC) have been widely studied; however, the molecular mechanism of BE-EAC carcinogenesis has not been completely understood. MicroRNA (miRNA) is now essential to understand the molecular mechanism of cancer progression. ...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2009.08.009
更新日期：2009-12-01 00:00:00
abstract：:Stroke and multiple sclerosis (MS) illustrate how clinical imaging can facilitate early phase drug development and most effective medicine use in the clinic. Imaging has enhanced understanding of the dynamics of evolution of disease pathophysiology, better defining treatment targets. Imaging measures can enable strati...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2013.10.006
更新日期：2014-02-01 00:00:00
abstract：:Viral and non-viral gene transfer technologies have been used to efficiently generate therapeutic T cells with desired cancer-specificity. Chimeric antigen receptors (CARs) redirect T cell specificity toward antibody-recognized antigens expressed on the surface of cancer cells, while T cell receptors (TCRs) extend the...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2015.08.006
更新日期：2015-10-01 00:00:00
abstract：:Information about the activity of airway sensory afferent nerves in vivo can be obtained electrophysiologically by extracellular recording of action potentials. Apart from data capture, the basic techniques used for recording sensory nerve activity have not advanced greatly in 50 years. However, clearly they continue ...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/s1471-4892(02)00153-4
更新日期：2002-06-01 00:00:00
abstract：:The first therapeutic aptamer was approved for human use in 2004, and a range of chemical substitutions that improve the drug-like properties of aptamers has recently been shown to increase the utility of this modality. Currently there are both anticoagulant and antithrombotic aptamers in the clinic, and additionally ...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2007.12.005
更新日期：2008-04-01 00:00:00
abstract：:Pseudomonas aeruginosa is an opportunistic pathogen that significantly contributes to morbidity and mortality in patients with cystic fibrosis. Defective mucociliary clearance associated with the absence of the functional cystic fibrosis transmembrane conductance regulator in airway epithelium plays a critical role in...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2006.12.005
更新日期：2007-06-01 00:00:00
abstract：:In vitro surveillance data, which provide key information to interpret the results of pharmacokinetic/pharmacodynamics (PK-PD) target attainment studies, are used to support dose selection decisions and recommendations for in vitro susceptibility testing criteria for antibacterial agents during drug development. Consi...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2017.10.009
更新日期：2017-10-01 00:00:00
abstract：:Since its discovery in 1993 and subsequent development of selective antagonists, a growing number of studies support the use of serotonin 5-HT(6) receptor antagonism as a promising mechanism for treating cognitive dysfunction. Lately, several studies with structurally different compounds have shown that not only antag...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2011.01.004
更新日期：2011-02-01 00:00:00
abstract：:Treatment of complex diseases such as cancer, cardiovascular disease, diabetes or neurological disorders frequently warrants the utilization of drug combinations for therapeutic intervention. In fact, the most successful example is the current standard of care for HIV patients. However, identification of successful dr...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2018.07.008
更新日期：2018-10-01 00:00:00
abstract：:The CD28 and B7 protein families are critical regulators of immune responses and, in the past few years, several new family members have been identified. Preclinical studies exploring the role of members of the CD28 and B7 families support the targeting of these pathways for new therapeutic approaches. Indeed, recent ...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2005.02.003
更新日期：2005-08-01 00:00:00
abstract：:Neuropsychiatric disorders as schizophrenia, autism and mood disorders represent one of the leading causes of disability. The cost of bringing a drug to the market is increasing and becoming more risky. Pharmaceutical investments in neuroscience are decreasing. At the same time we are facing an unprecedented rate of d...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2011.08.003
更新日期：2011-10-01 00:00:00
abstract：:In recent decades there has been an upsurge of interest in mechanisms of cell death in the central nervous system. Much attention has been focused on two cell death processes - excitotoxicity and apoptosis - and much confusion has arisen regarding how one relates to the other, and how either relates to neurological di...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：
更新日期：2003-02-01 00:00:00
abstract：:Regulator of G protein signalling (RGS) proteins are GTPase-activating proteins for heterotrimeric G protein alpha subunits, and are therefore physiologically and pathophysiologically important negative regulators of G-protein-coupled receptor signalling in the cardiovascular system. Owing to the functional redundancy...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2006.11.007
更新日期：2007-04-01 00:00:00
abstract：:Myocardial apoptosis primarily triggered during reperfusion has been associated with cardiac dysfunction and extension of infarction. Although potential signaling pathways involved in triggering apoptosis remain to be clearly defined, an increasing number of experiments have implicated the generation of reactive oxyge...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2003.10.010
更新日期：2004-04-01 00:00:00
abstract：:Glucocorticoid excess induces hypertension, in which abnormal renal sodium homeostasis is implicated. It is common in industrialised nations where hypertension remains the major risk-factor for cardiovascular disease. Aldosterone is the dominant chronic regulator in sodium homeostasis, but glucocorticoids influence re...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2015.01.005
更新日期：2015-04-01 00:00:00
abstract：:Type 1 human ether-a-go-go-related gene (hERG1) potassium channels are a key determinant of normal repolarization of cardiac action potentials. Loss of function mutations in hERG1 channels cause inherited long QT syndrome and increased risk of cardiac arrhythmia and sudden death. Many common medications that block hER...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2013.11.006
更新日期：2014-04-01 00:00:00
abstract：:Blood vessels deliver nutrients and oxygen to cells and tissues in the body. When blood supply is insufficient new vessels form to meet the metabolic tissue requirements. Several studies have examined the cellular and molecular principles of blood vessel formation, yet little is known about how vessels sense and integ...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2010.01.001
更新日期：2010-04-01 00:00:00
abstract：PURPOSE OF THE REVIEW:Faecal microbiota transplantation (FMT) has emerged as a potent form of therapeutic microbial manipulation. There is much interest in exploring its potential in conditions such as inflammatory bowel disease (IBD) where disturbances in the gastrointestinal microbiota play a crucial role in disease ...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2020.08.009
更新日期：2020-12-01 00:00:00
abstract：:Inverse agonism has gone from an initial curiosity to a now well-recognized phenomenon. This has demanded expansion of receptor theory models to account for multiple receptor states and a re-definition of ligand efficacy. However, after several decades of discovery, the clinical importance of inverse agonist ligands i...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2006.10.005
更新日期：2007-04-01 00:00:00
abstract：:The dynamic regulation of the structure, function and turnover of mitochondria is recognized as an immutable control node maintaining cellular integrity and homeostasis. The term 'mitohormesis' has recently been coined to describe the adaptive reprogramming of mitochondrial biology in response to low levels of metabol...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2007.12.008
更新日期：2008-04-01 00:00:00
abstract：:There is a growing body of evidence that although medical or surgical castration blocks the generation of gonadal testosterone in prostate cancer, androgens originating from other sources may continue to drive androgen receptor (AR) signaling. Recent studies have demonstrated high intratumoral levels of androgens and ...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2008.06.004
更新日期：2008-08-01 00:00:00
abstract：:Reporter-gene assays offer an alternative to biochemical assays for following signal transduction pathways from receptors at the cell surface to nuclear gene transcription in living cells. Specific reporter-gene systems are now available for the study of ligand activity at G alpha(i/o), G alpha(s) and G alpha(q) G-pro...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/s1471-4892(01)00091-1
更新日期：2001-10-01 00:00:00
abstract：:A complex network operates in the spinal dorsal horn to integrate peripheral nociceptive inputs with local and descending control mechanisms, and to cross-talk with higher brain areas. Injury to peripheral sensory nerves can trigger a cascade of events within this relay which, in some cases, may turn into abnormal res...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2011.10.021
更新日期：2012-02-01 00:00:00
abstract：:White adipose tissue (WAT) is a highly dynamic organ that can vary considerably in mass depending on energy balance. Data from recent cross-sectional and prospective clinical studies have revealed a set of mechanisms that link WAT dysfunction to type 2 diabetes. This review focuses on three of the most important patho...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2020.09.008
更新日期：2020-12-01 00:00:00
abstract：:Over the past few years small molecule inhibitors of both Src family kinases and focal adhesion kinase (FAK) have entered clinical studies for the treatment of solid tumours. These adhesion-linked kinases are involved in a number of pathways that have impact on the behaviour of tumour cells and the challenge is now, h...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2008.06.012
更新日期：2008-08-01 00:00:00
abstract：:Over the past few years, several groups have used voltage-sensitive dyes or calcium-indicator dyes to optically monitor the activity of several enteric neurons simultaneously. Some of the initial practical problems have been solved and these studies have successfully shown the spread of electrical activation within th...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/s1471-4892(01)00097-2
更新日期：2001-12-01 00:00:00
