Abstract：
:Heat shock proteins (HSPs) are involved in a number of cellular processes, including cell cycle, growth, and survival, apoptosis, stress responses, angiogenesis, and oncogenesis. Among the characterized HSPs, the molecular chaperone HSP90 has emerged as an exciting molecular target for cancer therapy since its discovery as the target protein of the antibiotic geldanamycin. The stress-inducible HSP70, which is upregulated in many cancers, contributing to tumor cell survival and resistance to therapy, has important roles as a housekeeper in the cell, assisting in the correct folding, trafficking, and degradation of many proteins. 2-Phenylethynesulfonamide (PES) physically interacts with HSP70 and disrupts the association between HSP70 and several of its cofactors and client proteins, leading to cancer cell death that is selectively mediated through caspase-independent mechanisms involving increased protein aggregation, impairment of lysosomal functions, and inhibition of autophagy. Mammalian HSP60 has several functions in the cell, including apoptosis, an immune-regulatory function, and cell spreading. HSP60 is a mitochondrial protein that is essential for the folding and assembly of newly imported proteins in the mitochondria. Epolactaene/ETB covalently binds to HSP60, inhibiting its chaperone activity. Molecular chaperone inhibitors are significantly valuable not only as tools to reveal the unknown cellular functions of molecular chaperones, but also as lead compounds for drug discovery. Thus, high-throughput screening systems are necessary for the discovery of more effective inhibitors. Here, we describe the methodology for 4 characteristic types of high-throughput screening systems for inhibitors of molecular chaperones, mainly HSP90 and HSP70: the colorimetric method, the fluorescence polarization method, the chemical array method, and the AlphaScreen® method.
journal_name
Curr Pharm Desjournal_title
Current pharmaceutical designauthors
Kondoh Y,Osada Hsubject
Has Abstractpub_date
2013-01-01 00:00:00pages
473-92issue
3eissn
1381-6128issn
1873-4286pii
CPD-EPUB-20120816-5journal_volume
19pub_type
杂志文章,评审abstract：:Opiates lack potent analgesic efficacy in neuropathic pain although it is now generally accepted that the poor effect of these drugs reflects a reduction in their potency. Reduction of morphine antinociceptive potency was postulated to be due to the fact that nerve injury altered the activity of opioid systems or opio...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/1381612054865055
更新日期：2005-01-01 00:00:00
abstract：:Naturally occurring and chemically modified ribonucleosides have interesting bioactive effects. Dietary ribonucleosides are ingested mainly as nucleoproteins and are converted in the course of intestinal digestion to monomeric compounds. Different bioactive effects of dietary ribonucleosides have been described, inclu...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/138161207780414269
更新日期：2007-01-01 00:00:00
abstract：:Gene therapy may be capable of treating a variety of diseases, a prerequisite of which is the successful delivery of polynucleic acids (e.g., DNA, RNA) to a patient's cells. Delivery can be achieved technologically (e.g., using electroporation), using viruses (natural gene delivery vectors) or non-viral vectors (e.g.,...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/1381612823666170710124137
更新日期：2017-01-01 00:00:00
abstract：:Uveitis is a sight threatening intraocular inflammation accounting for approximately 10% of blindness worldwide. On the basis of aetiology, disease can be classified as infectious or non-infectious; and by anatomical localization of inflammation as anterior, posterior and panuveitis. Non-infectious uveitis is believed...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/1381612821666150316122928
更新日期：2015-01-01 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：:Aquaporins (AQPs) are expressed in physiologically essential tissues and organs in which edema and fluid imbalances are of major concern. Potential roles in brain water homeostasis and edema, angiogenesis, cell migration, development, neuropathological diseases, and cancer suggest that this family of membrane proteins...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/138161207782341349
更新日期：2007-01-01 00:00:00
abstract：:Antimicrobial photodynamic therapy (aPDT) is an emerging alternative to antibiotics motivated by growing problems with multi-drug resistant pathogens. aPDT uses non-toxic dyes or photosensitizers (PS) in combination with harmless visible of the correct wavelength to be absorbed by the PS. The excited state PS can form...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/138161211795703735
更新日期：2011-01-01 00:00:00
abstract：:Inflammatory bowel disease (IBD) is a group of disorders characterized by chronic inflammation within the gastrointestinal tract. It is a multifactorial disease associated with immune-cell mediated oxidative damage to the intestinal mucosa. There is no cure for IBD, but anti-cytokine therapy can limit target inflammat...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/1381612824666180717110236
更新日期：2018-01-01 00:00:00
abstract：BACKGROUND:Intracerebral hemorrhage (ICH) is the most lethal subtype of stroke, a leading cause of death and disability in developed countries. Therapeutic options are notably limited. There is no specific pharmacological treatment, and early surgery has few indications that represent only a small clinically relevant s...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/1381612822666161221153937
更新日期：2017-01-01 00:00:00
abstract：:Circumstantial evidence has been provided of a role of the plasminogen/plasmin system in a variety of biological phenomena, including thrombolysis, vascular stenosis, reproduction, embryogenesis, cell invasion, angiogenesis, brain function and chronic lung or kidney inflammatory disorders. Inhibition of the system occ...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/138161206776056038
更新日期：2006-01-01 00:00:00
abstract：BACKGROUND:Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), termed coronavirus disease 2019 (COVID-19) by the World Health Organization, is a newly emerging zoonotic agent that emerged in China in December 2019. No specific treatment for COVID-19 is currently available. Usual palliative treatment includes ...
journal_title：Current pharmaceutical design
pub_type： 杂志文章
doi：10.2174/1381612826666200707121636
更新日期：2020-07-07 00:00:00
abstract：BACKGROUND:Progression of aortic valve calcifications (AVC) leads to aortic valve stenosis (AS). Importantly, the AVC degree has a great impact on AS progression, treatment selection and outcomes. Methods of AVC assessment do not provide accurate quantitative evaluation and analysis of calcium distribution and depositi...
journal_title：Current pharmaceutical design
pub_type： 杂志文章
doi：10.2174/1381612825666190930101258
更新日期：2019-01-01 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：:The discovery of the delicate role of endogenous nitric oxide in the homeostasis of various cellular functions and the dynamic behaviour of the airways, has led to a new, rapidly progressing area of physiological science, that has direct bearing for our understanding of multiple airway diseases. The potentially protec...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/138161206778194141
更新日期：2006-01-01 00:00:00
abstract：:Runx2/Cbfa/AML3 is a member of the runt homology domain family of transcription factors, essential for osteoblast differentiation and bone formation. Defining the molecular mechanisms by which Runx2 can function as a master regulatory gene for activating the program of osteoblastogenesis has provided novel insights fo...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/1381612033453659
更新日期：2003-01-01 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：:Cyclooxygenase-1 (COX-1) derived eicosanoids promote gastroprotective mucosal defenses and induce platelet aggregation. By sparing COX-1, COX-2 specific inhibitors provide effective anti-inflammatory and analgesic activity while substantially reducing the risk of peptic ulcer disease and GI bleeding compared to dual C...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/1381612033454018
更新日期：2003-01-01 00:00:00
abstract：:Prostacyclin (PGI(2)) is one of the major vascular protectors against thrombosis and vasoconstriction, caused by thromboxane A(2). Understanding the molecular mechanisms of PGI(2) biosynthesis and signaling is crucial to the development of therapeutic approaches to regulate PGI(2) functions. This review provides infor...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/138161206776055994
更新日期：2006-01-01 00:00:00
abstract：:Systemic hypersensitivity (HS) to corticosteroids (CS) is paradoxical but does exist. Some patients with a previous contact allergy to topical CS may develop a systemic contact dermatitis (SCD) while receiving CS orally or intravenously. However, a previous contact sensitization is not mandatory for developing a syste...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/1381612822666161013092339
更新日期：2016-01-01 00:00:00
abstract：:Opioids constitute the basis for pharmacological treatment of moderate to severe pain in cancer pain and non-cancer pain patients. Their action is mediated by the activation of opioid receptors, which integrates the pain modulation system with other effects in the central nervous system including cognition resulting i...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/138161212803582522
更新日期：2012-01-01 00:00:00
abstract：:Mass spectrometry information has long offered the potential of discovering biomarkers that would enable clinicians to diagnose disease, and treat it with targeted therapies. PeptideAtlas currently provides access to large-scale spectra data and identification information. This data, and the generation of targeted pep...
journal_title：Current pharmaceutical design
pub_type： 杂志文章
doi：10.2174/138161212799277833
更新日期：2012-01-01 00:00:00
abstract：:Schizophrenia is a complex pathology characterized by the occurrence of a variety of symptoms classified as positive, negative and cognitive. Although the exact etiopathogenesis of this disorder has not been unraveled yet, many theories have been endorsed during the last years. Among these, the neurochemical theories ...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/1381612821666150105122422
更新日期：2015-01-01 00:00:00
abstract：:Pancreatic cancer is hallmarked by aggressive biology and extreme lethality and very high mortality rates. The underlying molecular mechanism of its rapid development and progression is unclear, however. Recent identification and functional validation of nitric oxide (NO) production in pancreatic cancer suggest a role...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/138161210790232194
更新日期：2010-01-01 00:00:00
abstract：BACKGROUND:Carbon dioxide (CO2) exists in nature around us. In the middle of the 20th century, the intraluminal injection of CO2 demonstrated similar results to those of Digital Subtraction Angiography (DSA) with an iodinated contrast agent (ICA). Since then, the technology behind CO2 DSA has developed significantly. ...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/1381612825666191209124911
更新日期：2019-01-01 00:00:00
abstract：:Reverse transcriptase (RT) is one of the most important targets for HIV drug discovery. However, the emergence of resistant mutants has become one of the biggest challenges in HIV-1 RT drug discovery/development and attracted great research interests worldwide. It is particularly important to develop novel anti-HIV-1 ...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/138161282005140214163439
更新日期：2014-01-01 00:00:00
abstract：:Glucocorticoids are the first line medication used in the therapy of many severe inflammatory disorders. They exert their activity through binding to the glucocorticoid receptor, a ligand-dependent transcription factor, and result in either activation or repression of a large set of glucocorticoid responsive genes. Th...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/1381612043383610
更新日期：2004-01-01 00:00:00
abstract：:Repurposing already approved drugs as new anticancer agents is a promising strategy considering the advantages such as low costs, low risks and less time-consumption. Disulfiram (DSF), as the first drug for antialcoholism, was approved by the U.S. Food and Drug Administration (FDA) over 60 years ago. Increasing eviden...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/1381612825666190816233755
更新日期：2019-01-01 00:00:00
abstract：:In the early 1980s, an "atypical" beta-adrenergic receptor was discovered and subsequently called the beta (3)-adrenoceptor (beta(3)-AR). Agonists of the beta(3)-AR were observed to simultaneously increase lipolysis, fat oxidation, energy expenditure and insulin action leading to the belief that this receptor might se...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/1381612013397339
更新日期：2001-09-01 00:00:00
abstract：:Supraventricular tachycardias (SVTs) are observed in 0,1-0,4% of the paediatric population and represent an important clinical problem with related significant health and social issues. Most tachycardias are paroxysmal, being associated with sudden onset and termination, and only a relatively small number of them is p...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/138161208784007761
更新日期：2008-01-01 00:00:00
abstract：:There is a high rate of benzodiazepine use in the population. Benzodiazepines are used for multiple indications (anxiety, seizures, alcohol withdrawal, muscular relaxation and anesthesia). Benzodiazepines are also addictive substances and a non-negligible fraction of regular users will develop dependence. There is cur...
journal_title：Current pharmaceutical design
pub_type： 杂志文章,评审
doi：10.2174/1381612821666150619092039
更新日期：2015-01-01 00:00:00
