Abstract:
:Tuberculosis now ranks as the leading cause of death in the world due to a single infectious agent. Current standard of care treatment can achieve very high cure rates for drug-sensitive disease but requires a 6-month duration of chemotherapy. Drug-resistant disease requires significantly longer treatment durations with drugs associated with a higher risk of adverse events. Thus, there is a pressing need for a drug regimen that is safer, shorter in duration and superior to current front-line chemotherapy in terms of efficacy. The TB drug pipeline contains several candidates that address one or more of the required attributes of chemotherapeutic regimens that may redefine the standard of care of this disease. Several new drugs have been reported and novel targets have been identified allowing regimens containing new compounds to trickle into clinical studies. Furthermore, a recent paradigm-shift in understanding the pharmacokinetics of anti-tubercular drugs is revolutionizing the way we select compounds for clinical progression.
journal_name
Curr Opin Pharmacoljournal_title
Current opinion in pharmacologyauthors
J Libardo MD,Boshoff HI,Barry CE 3rddoi
10.1016/j.coph.2018.08.001subject
Has Abstractpub_date
2018-10-01 00:00:00pages
81-94eissn
1471-4892issn
1471-4973pii
S1471-4892(18)30066-3journal_volume
42pub_type
杂志文章,评审abstract::Metabotropic glutamate receptors (mGluRs) are heavily expressed throughout the basal ganglia (BG), where they modulate neuronal excitability, transmitter release and long term synaptic plasticity. Therefore, targeting specific mGluR subtypes by means of selective drugs could be a possible strategy for restoring normal...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2018.03.004
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abstract::Neuromuscular blocking drugs were introduced into clinical practice in 1942. Although these drugs made new surgical techniques possible, they also led to morbidity and mortality owing to respiratory muscle paralysis and paralysis in the face of inadequate anesthesia. Newer competitive antagonists at the neuromuscular ...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2004.12.009
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abstract::Dietary intake of marine n-3 polyunsaturated fatty acids (PUFA) has beneficial effects in various cardiac disorders. Few studies have, however, investigated the therapeutic potential of n-3 PUFA in patients undergoing coronary artery bypass grafting (CABG). Five heterogeneous randomized studies on n-3 PUFA for prevent...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2012.01.012
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abstract::Cholesterol epoxide hydrolase (ChEH) catalyzes the hydration of cholesterol-5,6-epoxides (5,6-EC) into cholestane-3β,5α,6β-triol. ChEH is a hetero-oligomeric complex called the anti-estrogen binding site (AEBS) comprising 3β-hydroxysterol-Δ(8)-Δ(7)-isomerase (D8D7I) and 3β-hydroxysterol-Δ(7)-reductase (DHCR7). D8D7I a...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
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abstract::Early animal, menstrual phase and gender comparative studies inconsistently support an oestrogen-induced increase in fat oxidation during exercise. Recent advances from studies of cellular signalling and gene expression provide evidence for inter-tissue and intramuscular mechanisms that demonstrate oestrogen's promoti...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2012.02.008
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abstract::Several mechanisms of resistance have been identified, underscoring the complex nature of estrogen receptor (ER) signaling and the many connections between this pathway and other essential signaling pathways in breast cancer cells. Many therapeutic targets of cell signaling and cell cycle pathways have met success wit...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2018.04.009
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abstract::The majority of kidney cancers are clear-cell carcinomas (ccRCC), characterized by the accumulation of cholesterol, cholesterol esters, other neutral lipids and glycogen. Rather than being a passive bystander, the clear-cell phenotype is suggested to be a biomarker of deregulated cholesterol and lipid biosynthesis, wh...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2012.08.002
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abstract::Toll-like receptors (TLRs) play a crucial role in host defence and inflammation. Given that a significant amount of evidence implicates TLRs in the pathogenesis of immune diseases and cancer, and their activation occurs early in the inflammatory cascade, they are attractive targets for novel therapeutic agents. Potent...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2012.06.002
更新日期:2012-08-01 00:00:00
abstract::Although only 5-10% of patients with asthma are relatively unresponsive to treatment with inhaled corticosteroids, refractory asthma represents an important condition, as these patients suffer considerable morbidity and mortality and consume a disproportionately large amount of health resource. Treatment options are l...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2007.03.001
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abstract::Hepatocellular carcinoma (HCC) is the 5th most common cancer, but the 3rd leading cause of cancer death globally with approximately 700,000 fatalities annually. The severity of this cancer arises from its difficulty to detect and treat. The major etiologies of HCC are liver fibrosis or cirrhosis from chronic viral inf...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2018.04.002
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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::Encapsulation is an important technology for pharmaceutical industry, food production, et cetera. Its current level of development requires capsule functionalization. One of the interesting ideas to provide new functionality to the microcapsule and nanocapsule is layer-by-layer deposition of functional species. This t...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2014.09.002
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abstract::Chronic liver diseases with different etiologies represent a major public health issue worldwide. Liver fibrosis is the common feature of almost all chronic liver diseases and remains a key determinant of clinical prognosis. Over the last two decades, basic science studies have uncovered molecular mechanisms underlyin...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2019.09.006
更新日期:2019-12-01 00:00:00
abstract::Human pluripotent stem cells can be differentiated into specific, relevant cell types of interest including the cells of the retina and optic nerve. These cells can then be used to study fundamental biology as well as disease modelling and subsequent screening of potential treatments. Many models of differentiation an...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2019.09.003
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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::Autophagy is a highly conserved catabolic pathway in which proteins and organelles are engulfed by vacuoles that are targeted to lysosomes for degradation. Defects in the autophagic machinery have been described in several neurodegenerative diseases uncovering the tight dependency of neuronal survival on the efficienc...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2012.09.004
更新日期:2013-02-01 00:00:00
abstract::Extracellular matrix (ECM) components, commonly thought to function purely as structural elements are now demonstrated to act as signaling molecules. With the identification of matrix-derived endogenous ligands of Toll-like and NOD-like receptors of innate immunity, a general question about the mechanisms of soluble E...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2009.11.007
更新日期:2010-04-01 00:00:00
abstract::Homomerization and heteromerization of 7 transmembrane spanning (7TM)/G-protein-coupled receptors (GPCRs) have been an important field of study. Whereas initial studies were performed in artificial cell systems, recent publications are shifting the focus to the in vivo relevance of heteromerization. This is especially...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2009.09.007
更新日期:2010-02-01 00:00:00
abstract::Gastroesophageal reflux disease (GERD) is increasingly common worldwide; symptoms differ between individuals and endoscopically visible injury is present in only about 50% of cases. Although GERD is a disorder of gastrointestinal motility and structure, the most effective therapy is based on the use of acid antisecret...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2005.09.001
更新日期:2005-12-01 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::Lysophosphatidic acid (LPA), a bioactive phospholipid, and its family of cognate G protein-coupled receptors have demonstrated roles in many biological functions in the nervous system. To date, five LPA receptors have been identified, and additional receptors may exist. Most of these receptors have been genetically de...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2008.11.010
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abstract::Nitric oxide (NO) produced by the enteric nervous system represents an important regulatory mechanism in gut homeostasis. Aberrant NO signaling contributes significantly toward enteric disease by altering gut motility, vascular tone, blood supply, mucosal barrier function, secretions and immunity. Consequently, there ...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2014.07.009
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abstract::The deployment of artemisinin-based combination therapies (ACTs) has been, and continues to be, integral to reducing the number of malaria cases and deaths. However, their efficacy is being increasingly jeopardized by the emergence and spread of parasites that are resistant (or partially resistant) to the artemisinin ...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2018.07.010
更新日期:2018-10-01 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
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abstract::Where we are on the road to 'tailor-made' precision medicine for drug-resistant cervical carcinoma? We explored studies about analyses of viral and human genomes, epigenomes and transcriptomes, DNA mutation analyses, their importance in detecting HPV sequences, mechanisms of drug resistance to established and targeted...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2020.09.013
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abstract::Chronic inflammation is a risk factor for several gastrointestinal malignancies, including colorectal cancer. Recent epidemiological studies and clinical trials demonstrate that long-term use of non-steroidal anti-inflammatory drugs (NSAIDs) markedly reduced the relative risk of colorectal cancer. Chronic inflammation...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2009.08.003
更新日期:2009-12-01 00:00:00
abstract::Fibrosis can occur in most organs and is characterised by excessive and progressive extracellular matrix deposition and destruction of normal tissue architecture and function. In many cases treatment options are limited. Fibrotic diseases are therefore associated with high morbidity and mortality. Tissue biopsies rema...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2019.09.010
更新日期:2019-12-01 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::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::Opiate drugs, such as morphine, are renowned for their analgesic properties. To date, opioid narcotics represent the largest and most potent class of pain relievers available to treat both acute and chronic pain conditions. The use of opiates, however, is severely limited by several adverse side effects. Upon chronic ...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2006.06.007
更新日期:2006-12-01 00:00:00