Abstract:
:The oncoproteins MDM2 and MDMX negatively regulate the activity and stability of the p53 tumor suppressor, directly contributing to the development and progression of many tumors harboring wild type p53. Antagonizing MDM2 and MDMX to activate the p53 pathway has thus become an attractive new strategy for anticancer drug design. Several different classes of MDM2 and MDMX antagonists have been reported, including low molecular weight compounds, small peptides, miniature proteins, and peptidomimetics. This review aims to summarize the latest progress in the design of peptide activators of the p53 tumor suppressor.
journal_name
Curr Pharm Desjournal_title
Current pharmaceutical designauthors
Zhan C,Lu Wdoi
10.2174/138161211795222577subject
Has Abstractpub_date
2011-01-01 00:00:00pages
603-9issue
6eissn
1381-6128issn
1873-4286pii
BSP/CPD/E-Pub/000352journal_volume
17pub_type
杂志文章,评审abstract:BACKGROUND:The global burden of gastrointestinal cancers, including colorectal, stomach, and esophageal cancers is rising steadily. Several therapeutic approaches have been considered for the treatment of GI carcinomas. However, none showed to halt or cure the disease. There is a need to develop effective targeted mole...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612823666170124115159
更新日期:2017-01-01 00:00:00
abstract::Proper understanding of blood-brain barrier (BBB) regulation is crucial to reduce/prevent its disruption during injury. Since high brain complexity makes interpretation of in vivo data challenging BBB studies are frequently performed using simplified in vitro models. Although such models represent an important and fre...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161211797440159
更新日期:2011-01-01 00:00:00
abstract::Despite the development of strong antibiotics, the pneumonia death is increasing all over the world in these decades. Among the people who died of pneumonia, the majority were 65 years old or over. Although pneumonia is recently categorized into several entities, aspiration pneumonia includes all entities. Therefore, ...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/13816128113199990567
更新日期:2014-01-01 00:00:00
abstract::Histone deacetylases (HDACs), which act on acetylated histones and/or other non-histone protein substrates, represent validated epigenetic targets for the treatment of cancer and other human diseases. The inhibition of HDAC activity was shown to induce cell cycle arrest, differentiation, apoptosis as well as a decreas...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612820666141110164604
更新日期:2015-01-01 00:00:00
abstract::Manufacturing of pharmaceutical solids involves different unit operations and processing steps such as powder blending, fluidization, sieving, powder coating, pneumatic conveying and spray drying. During these operations, particles come in contact with other particles, different metallic, glass or polymer surfaces and...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612821666151008124811
更新日期:2015-01-01 00:00:00
abstract::Over the past five decades, the pharmacological treatment of depression has been based on the pathophysiological hypothesis of a deficiency in monoamines, mainly serotonin and noradrenaline. Antidepressant prescribed today, all of them designed to enhance central monoaminergic tone, present several important limitatio...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161211795164086
更新日期:2011-01-01 00:00:00
abstract::Microdialysis is a technique for sampling the chemistry of the interstitial fluid of tissues and organs in animal and man. It is minimally invasive and simple to perform in a clinical setting. Although microdialysis samples essentially all small molecular substances present in the interstitial fluid the use of microdi...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612043384105
更新日期:2004-01-01 00:00:00
abstract::A severe atypical pneumonia designated as severe acute respiratory syndrome (SARS) by The World Health Organization broke out in China and menaced to more than other 30 countries between the end of the year 2002 and June of the year 2003. A novel coronavirus called severe acute respiratory syndrome coronavirus (SARS-C...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161206779010459
更新日期:2006-01-01 00:00:00
abstract:PURPOSE:Ultrasound contrast agents involving a therapeutic drug applied during enhanced imaging can be used for targeted therapy. The preparation of contrast agents is a precondition and basis for the use of multifunctional contrast agents in molecular imaging. METHODS:This study uses thin-film hydration-mechanical vi...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/1381612824666181011120031
更新日期:2018-01-01 00:00:00
abstract:BACKGROUND:Central serous chorioretinopathy (CSC) is the fourth most frequent retinal disorder in terms of prevalence. It typically occurs in young subjects and affects men more often than women. CSC is characterized by serous retinal detachment (SRD) involving mainly the macular area. The clinical course is usually se...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612825666190123165914
更新日期:2018-01-01 00:00:00
abstract::In the third millennium preventive medicine is becoming a corner stone in our concept of health. Colorectal cancer (CRC) fits the criteria of a disease suitable for prevention interventions. It is a prevalent disease that is associated with considerable mortality and morbidity rates, with more than 1,000,000 new cases...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161207781368783
更新日期:2007-01-01 00:00:00
abstract::Mitochondria are involved in different physiological and pathological processes that are crucial for tumor cell physiology, growth and survival. Since cancer cells have frequently disrupted different cell death pathways that promote their survival, mitochondria may be key organelles to promote cell death in cancer cel...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161211796904803
更新日期:2011-01-01 00:00:00
abstract::Mechanical loading provides an anabolic stimulus for bone. More importantly, the mechanosensing apparatus in bone directs osteogenesis to where it is most needed for improving bone strength. The biological processes involved in bone mechanotransduction are poorly understood and further investigation of the molecular m...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612043383755
更新日期:2004-01-01 00:00:00
abstract::Chloride channels play important roles in vital cellular signalling processes contributing to homeostasis in both excitable and non-excitable cells. Since 1987, more than ten ion channel genes have been identified as causing human hereditary diseases among them the genes for the voltage-dependent chloride channel ClC-...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161206775474459
更新日期:2006-01-01 00:00:00
abstract::Philosophers have been trying to solve the mind-body problem for hundreds of years. Consciousness is the core of this problem: How do subjective conscious sensations, perceptions, feelings, and thoughts arise out of objective physical brain activities? How is this subjective conscious world in causal interaction with ...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:
更新日期:2014-01-01 00:00:00
abstract:BACKGROUND:The use of aromatic plants to relief different illness is not a new therapy. Actually aromatic plants have been used for many centuries by different cultures around the world. Pharmacological studies provide scientific support to the traditional use of aromatic medicinal plants and aromatherapy; nevertheless...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612822666160607065917
更新日期:2016-01-01 00:00:00
abstract::Macrophages are professional scavengers of apoptotic and necrotic cells, and hence constantly take up self antigens. Paradoxically, macrophages are also professional antigen-presenting cells, which would seem to invite autoimmune disorders. Moreover, macrophages are effector cells in the tissue-destruction phase of au...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612033392026
更新日期:2003-01-01 00:00:00
abstract:BACKGROUND:The objective of this study was to apply Quality by Design (QbD) principles on process parameter optimization for the development of hybrid delivery system (combination of (SLNs) and In-situ gelling system) for hydrophilic drug Moxifloxacin Hydrochloride (MOX) to achieve its controlled delivery, which otherw...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/1381612824666180403115106
更新日期:2018-01-01 00:00:00
abstract::We have synthesized a novel series of N-substituted sarcosines, analogues of NFPS (N-[3-(biphenyl-4- yloxy)-3-(4-fluorophenyl)propyl]-N-methylglycine), as type-1 glycine transporter (GlyT-1) inhibitors. Several compounds incorporated a diazine ring inhibited recombinant hGlyT-1b expressed permanently in CHO cells and ...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/1381612821666150109125623
更新日期:2015-01-01 00:00:00
abstract:AIMS:To compare the efficacy of pemafibrate (PF) and fenofibrate (FF) in treating dyslipidemia. METHODS:A comprehensive search was performed on the public database to identify relevant randomized controlled trials (RCTs), which compared the effects of PF and FF treatment in lipid parameters among patients with dyslipi...
journal_title:Current pharmaceutical design
pub_type: meta分析
doi:10.2174/1381612825666191126102943
更新日期:2019-01-01 00:00:00
abstract:BACKGROUND:Vaginal infections caused by non-albicans species have become common in women of all age groups. The resistance of species such as Candida parapsilosis to the various antifungal agents is a risk factor attributed to these types of infections, which instigates the search for new sources of active compounds in...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/1381612826666200317131041
更新日期:2020-01-01 00:00:00
abstract::Alzheimer disease (AD) is characterized by excessive deposition of amyloid beta-peptides (Abeta peptides) in the form of senile plaques as well as neurofibrillary tangles (NFTs) in the brain. In the amyloidogenic pathway, the amyloid-beta precursor protein (APP) is cleaved by beta-secretase first, followed by gamma-se...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161206778792994
更新日期:2006-01-01 00:00:00
abstract::The search for methods to control physiological levels of carbon monoxide (CO), a vasoactive molecule, and bilibrubin, an antioxidant, have improved our understanding of the protective role of heme oxygenase (HO) against oxidative injury. HO activity can assist other antioxidant systems in diminishing the overall prod...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612033453758
更新日期:2003-01-01 00:00:00
abstract::Early life stress is considered a risk factor for the development of many diseases in both adolescence and adulthood. It has been reported that chronic stress (for instance, due to maternal separation during breast feeding), causes damage to the central nervous system at the level of neurons and glial cells, which are...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612823666170224111641
更新日期:2018-02-12 00:00:00
abstract:BACKGROUND:Reversible cholinesterase inhibitors, when given prophylactically before exposure to organophosphates, are able to decrease organophosphate-induced mortality. However, the efficacy of pyridostigmine, the only pre-treatment substance approved by the US Federal Drug Administration, is unsatisfactory. METHODS:...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/1381612822666161027154303
更新日期:2017-01-01 00:00:00
abstract::During the last two decades, the studies on ubiquitination in regulating transcription factor NF-κB activation have elucidated the expanding role of ubiquitination in modulating cellular events by non-proteolytic mechanisms, as well as by proteasomal degradation. The significance of ubiquitination has also been recogn...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612811319180010
更新日期:2013-01-01 00:00:00
abstract::Immunosenescence is considered a major contributory factor to the increased frequency of morbidity and mortality among elderly. On the other hand centenarians are considered the best example of successful ageing. To gain insight into mechanisms of immunosenescence and its clinical relevance, a possible model is repres...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/138161210790883750
更新日期:2010-01-01 00:00:00
abstract::Atrial fibrillation (AF) is the most common sustained rhythm disturbance, increasing prevalence with age, in particular in patients with cardiovascular disease. On the other hand, a subset of patients with AF being <60 years old and no evidence of underlying cardiovascular disease, and laboratory tests including thyro...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612820666140825142206
更新日期:2015-01-01 00:00:00
abstract::Gene therapy, currently, represents one of the new therapies that have emerged for the treatment of different diseases. Between the different approaches that can be chosen concerning this therapy, gene delivery with non-viral systems has focused the attention during the past decades, because of the reduced toxicity co...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612821666150901100037
更新日期:2015-01-01 00:00:00
abstract::The acid-base balance of cells is related to the concentration of free H⁺ ions. These are highly reactive, and their intracellular concentration must be regulated to avoid detrimental effects to the cell. H⁺ ion dynamics are influenced by binding to chelator substances ('buffering'), and by the production, diffusion a...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161212799504920
更新日期:2012-01-01 00:00:00