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 continued AR signaling in castration-resistant prostate cancer (CRPC), suggesting that androgens may also be synthesized de novo. Inhibiting the systemic biosynthesis of androgens in CRPC by targeting CYP17 may thus represent a rational therapeutic approach since this enzyme catalyses two key steroid reactions involving 17alpha-hydroxylase and C(17,20)-lyase in the androgen biosynthesis pathway. This review will discuss the rationale for and implications of targeting CYP17 in CRPC and focus on established and novel CYP17 inhibitors, including ketoconazole, abiraterone acetate, and VN/124-1, which are agents currently at different stages of development.
journal_name
Curr Opin Pharmacoljournal_title
Current opinion in pharmacologyauthors
Yap TA,Carden CP,Attard G,de Bono JSdoi
10.1016/j.coph.2008.06.004subject
Has Abstractpub_date
2008-08-01 00:00:00pages
449-57issue
4eissn
1471-4892issn
1471-4973pii
S1471-4892(08)00075-1journal_volume
8pub_type
杂志文章,评审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：:Cachexia is a multi-organ syndrome associated with cancer and other chronic diseases, characterized by body weight loss, muscle and adipose tissue wasting and inflammation, being often associated with anorexia. Skeletal muscle tissue represents more than 40% of body weight and seems to be one of the main tissues invol...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2015.04.003
更新日期：2015-06-01 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：:Introduction of biological agents for the treatment of the chronic inflammatory joint disease rheumatoid arthritis has reinvigorated research into this debilitating disease. These agents have been shown to both act on the signs and symptoms of disease, as well as retard the progression of joint destruction. However, t...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2004.04.001
更新日期：2004-06-01 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：:Acetylcholine, a major regulator of airway function, is not solely produced by neurons but also by a variety of non-neurons cells including various airway epithelial cells utilizing a molecular machinery of acetylcholine synthesis and release that differs from that of neurons. While canonical neuronal cholinergic sign...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2014.03.001
更新日期：2014-06-01 00:00:00
abstract：:New anti-infective drugs are an unmet necessity of modern medicine. The use of ∼omics technologies has exponentially increased the knowledge on active anti-infective structures, where to search for them and their mechanisms of action. Research involving extreme and unique environments (such as endophytes) revealed the...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2019.02.008
更新日期：2019-10-01 00:00:00
abstract：:Adiponectin, a novel hormone made by fat tissue, regulates energy metabolism and endothelial activation. Serum levels of adiponectin are reduced in conditions that are associated with an increased risk of cardiovascular disease, such as diabetes and the metabolic syndrome. Adiponectin trimers assemble into higher-orde...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2005.01.001
更新日期：2005-04-01 00:00:00
abstract：:Understanding the mechanisms of cell-cell interaction is a key unanswered question in modern pharmacology, given crosstalk defects are at the basis of many pathologies. Microfluidics represents a valuable tool for analyzing intercellular communication mediated by transmission of soluble signals, as occurring for examp...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2013.07.005
更新日期：2013-10-01 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
更新日期：2007-06-01 00:00:00
abstract：:Rhabdomyolysis is a clinical condition of potential life threatening destruction of skeletal muscle caused by diverse mechanisms including drugs and toxins. Given the fact that structurally not related compounds cause an identical phenotype pinpoints to common targets or pathways, responsible for executing rhabdomyoly...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2012.04.002
更新日期：2012-06-01 00:00:00
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
更新日期：2020-10-01 00:00:00
abstract：:Neurodegenerative diseases represent a large group of neurological disorders with heterogeneous clinical and pathological profiles. The majority of current therapeutic strategies provide temporary symptomatic relief but do not target the underlying disease pathobiology and thus do not affect disease progression. G pro...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2017.02.001
更新日期：2017-02-01 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：:Phosphodiesterase-5 (PDE5) inhibitors and other agents that modulate intracellular cGMP are now emerging as promising, safe, and easy to administer therapies for pulmonary hypertension, with relatively few side effects. Recent studies have shown that PDE5 inhibitors are potent acute pulmonary vasodilators in experimen...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2004.12.008
更新日期：2005-06-01 00:00:00
abstract：:The pharmaceutical industry is currently abandoning its antibacterial discovery research efforts. This seems to be part of a cyclical pattern in this therapeutic area. The reasons behind these ongoing cycles of feast and famine are multiple, but most revolve around the perception of market opportunities from the conti...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2003.04.003
更新日期：2003-10-01 00:00:00
abstract：:There have been significant developments in Ebola virus therapeutics. While the efficacy of several products was evaluated in the recent West Africa outbreak, a licensed treatment for EBOV disease remains elusive. Factors that negatively impacted the execution of clinical trials included an overall lack of world readi...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2016.08.016
更新日期：2016-10-01 00:00:00
abstract：:The inflammatory response is regulated by the production of different extracellular mediators, including lipids and extracellular nucleotides. In the extracellular environment, intermediate lipids activate specific G-protein-coupled receptors (GPCRs) in target cells and promote cell recruitment and activation. Extrace...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2019.02.004
更新日期：2019-08-01 00:00:00
abstract：:Inhibition of the DNA repair enzyme poly(ADP-ribose) polymerase-1 (PARP-1) has been extensively investigated in the pre-clinical setting as a strategy for chemo- or radio-potentiation. Recent evidence has suggested that PARP inhibitors might be active as single agents in certain rare inherited cancers that carry DNA r...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2006.02.004
更新日期：2006-08-01 00:00:00
abstract：:Airway epithelial cells provide mechanical and immune protection against pathogens and allergens. Following activation, these cells produce a wide range of cytokines including thymic stromal lymphopoietin (TSLP). Recently it was established that a high level of TSLP is associated with asthma in mice and in humans. The...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2008.03.002
更新日期：2008-06-01 00:00:00
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
更新日期：2012-12-01 00:00:00
abstract：:The development of genetic engineering technologies has today advanced to the point where the generation of high-affinity human antibodies against therapeutic targets is not a major hurdle. Rather, it is the selection of target molecules in, for example, cancer therapy that poses a challenge. Targets that are not mere...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/s1471-4892(01)00070-4
更新日期：2001-08-01 00:00:00
abstract：:CLEC-2 is a C-type lectin-like molecule that has recently been identified as a receptor on the surface of platelets. Ligand binding by CLEC-2 promotes phosphorylation of a tyrosine in the cytoplasmic domain YXXL motif of CLEC-2 by Src kinases and further downstream signalling events trigger platelet activation and agg...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2008.11.001
更新日期：2009-04-01 00:00:00
abstract：:Oligonucleotide-based therapeutics have been hailed as 'the next great wave of the biotechnology revolution' starting with antisense oligonucleotides (ASOs) nearly 20 years ago to RNA interference (RNAi) currently. Is RNAi just the latest research tool or does it have real potential as a therapeutic drug modality? As ...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2008.04.005
更新日期：2008-06-01 00:00:00
abstract：:Skeletal lesions contribute substantially to morbidity and mortality in patients with cancer. Emerging treatments for metastatic bone disease have arisen from our understanding of the biology of bone metastases. Tumour cells alter the functions of bone-resorbing (osteoclasts) and bone-forming (osteoblasts) cells, prom...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2015.04.004
更新日期：2015-06-01 00:00:00
abstract：:It is increasingly being appreciated that GABAA receptor subtypes, through their specific regional, cellular and subcellular localization, are linked to distinct neuronal circuits and consequently serve distinct functions. GABAA receptor subtype-selective drugs are therefore expected to provide novel pharmacological p...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2005.10.003
更新日期：2006-02-01 00:00:00
abstract：:During the past decade, evidence has accumulated for the involvement of purines and purine receptors in the pathogenesis and pathophysiology of asthma and chronic obstructive pulmonary diseases. In particular, the indirect bronchospasmic and inflammatory actions of purines via the activation and degranulation of mast ...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2004.01.010
更新日期：2004-06-01 00:00:00
abstract：:Mitochondria play a key role in energy metabolism in many tissues, including skeletal muscle and liver. Inherent disorders of mitochondria such as DNA deletions cause major disruption of metabolism and can result in severe impairment or death. However, the occurrence of such disorders is extremely rare and cannot acco...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2009.09.002
更新日期：2009-12-01 00:00:00
abstract：:Clinical trials of selective small-molecule inhibitors of epidermal growth factor receptor tyrosine kinase activity have shown that these targeted inhibitors of proliferative signal transduction provide well-tolerated antitumour activity in patients. Preclinical pharmacology studies illustrate the potential use of the...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/s1471-4892(02)00183-2
更新日期：2002-08-01 00:00:00
abstract：:Inhibition is a fundamental property of behaviour required for flexible responding and humans have evolved executive brain systems that can engage inhibitory processes in order to reduce interference from irrelevant distracting stimuli, block unwanted memories and emotions and suppress inappropriate choices and action...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2011.06.006
更新日期：2011-10-01 00:00:00
