Abstract:
:In the post-genome era, pathologies become associated with specific gene expression profiles and defined molecular lesions can be identified. The traditional therapeutic strategy is to block the identified aberrant biochemical activity. However, an attractive alternative could aim at antagonizing key transcriptional events underlying the pathogenesis, thereby blocking the consequences of a disorder, irrespective of the original biochemical nature. This approach, called transcription therapy, is now rendered possible by major advances in biophysical technologies. In the last two decades, techniques have evolved to become key components of drug discovery platforms, within pharmaceutical companies as well as academic laboratories. This review outlines the current biophysical strategies for transcription manipulation and provides examples of successful applications. It also provides insights into the future development of biophysical methods in drug discovery and personalized medicine.
journal_name
Int J Mol Scijournal_title
International journal of molecular sciencesauthors
Moustaqil M,Gambin Y,Sierecki Edoi
10.3390/ijms21072301subject
Has Abstractpub_date
2020-03-26 00:00:00issue
7issn
1422-0067pii
ijms21072301journal_volume
21pub_type
杂志文章,评审abstract::Cystic fibrosis (CF) is caused by mutations in the gene encoding the transmembrane conductance regulator (CFTR) protein. Some CF patients are compound heterozygous or homozygous for nonsense mutations in the CFTR gene. This implies the presence in the transcript of premature termination codons (PTCs) responsible for a...
journal_title:International journal of molecular sciences
pub_type: 杂志文章
doi:10.3390/ijms21134781
更新日期:2020-07-06 00:00:00
abstract::Endoplasmic reticulum stress (ERS) is one of the mechanisms of apoptotic cell death. Inhibiting the apoptosis induced by ERS may be a novel therapeutic target in cardiovascular diseases. Icariin, a flavonoid isolated from Epimedium brevicornum Maxim, has been demonstrated to have cardiovascular protective effects, but...
journal_title:International journal of molecular sciences
pub_type: 杂志文章
doi:10.3390/ijms140917845
更新日期:2013-08-30 00:00:00
abstract::We report here the successful fabrication of nano-whisker hydroxyapatite (nHA) coatings on Mg alloy by using a simple one-step hydrothermal process in aqueous solution. The nHA coating shows uniform structure and high crystallinity. Results indicate that nHA coating is promising for improving the in vitro corrosion an...
journal_title:International journal of molecular sciences
pub_type: 杂志文章
doi:10.3390/ijms16036113
更新日期:2015-03-17 00:00:00
abstract::WRKY transcription factors constitute one of the largest transcription factor families in plants, and play crucial roles in plant growth and development, defense regulation and stress responses. However, knowledge about this family in maize is limited. In the present study, we identified a drought-induced WRKY gene, Z...
journal_title:International journal of molecular sciences
pub_type: 杂志文章
doi:10.3390/ijms19103046
更新日期:2018-10-06 00:00:00
abstract::Bone adaptation or integration of an implant is characterized by a series of biological reactions that start with bone turnover at the interface (a process of localized necrosis), followed by rapid repair. The wound healing response is guided by a complex activation of macrophages leading to tissue turnover and new os...
journal_title:International journal of molecular sciences
pub_type: 杂志文章,评审
doi:10.3390/ijms11010354
更新日期:2010-01-25 00:00:00
abstract::The DNA excision repair protein ERCC-1-DNA repair endonuclease XPF (ERCC1-XPF) is a heterodimeric endonuclease essential for the nucleotide excision repair (NER) DNA repair pathway. Although its activity is required to maintain genome integrity in healthy cells, ERCC1-XPF can counteract the effect of DNA-damaging ther...
journal_title:International journal of molecular sciences
pub_type: 杂志文章
doi:10.3390/ijms19051328
更新日期:2018-04-30 00:00:00
abstract::Abnormal uterine function affects conception rate and embryo development, thereby leading to poor fertility and reproduction failure. Exosomes are a nanosized subclass of extracellular vesicles (EV) that have important functions as intercellular communicators. They contain and carry transferable bioactive substances i...
journal_title:International journal of molecular sciences
pub_type: 杂志文章,评审
doi:10.3390/ijms21239106
更新日期:2020-11-30 00:00:00
abstract::Wound healing is a physiological process, involving three successive and overlapping phases-hemostasis/inflammation, proliferation, and remodeling-to maintain the integrity of skin after trauma, either by accident or by procedure. Any disruption or unbalanced distribution of these processes might result in abnormal wo...
journal_title:International journal of molecular sciences
pub_type: 杂志文章,评审
doi:10.3390/ijms18112325
更新日期:2017-11-03 00:00:00
abstract::Calcium (Ca2+) is a universal and vital intracellular messenger involved in a diverse range of cellular and biological processes. Changes in the concentration of extracellular Ca2+ can disrupt the normal cellular activities and the physiological function of these systems. The calcium sensing receptor (CaSR) is a uniqu...
journal_title:International journal of molecular sciences
pub_type: 杂志文章,评审
doi:10.3390/ijms20215341
更新日期:2019-10-27 00:00:00
abstract::The kidney plays a primary role in maintaining homeostasis and detoxification of numerous hydrophilic xenobiotics as well as endogenous compounds. Because the kidney is exposed to a larger proportion and higher concentration of drugs and toxins than other organs through the secretion of ionic drugs by tubular organic ...
journal_title:International journal of molecular sciences
pub_type: 杂志文章,评审
doi:10.3390/ijms17111826
更新日期:2016-11-01 00:00:00
abstract::Internal transcribed spacer region (ITS) sequencing is the most extensively used technology for accurate molecular identification of fungal pathogens in clinical microbiology laboratories. Intra-genomic ITS sequence heterogeneity, which makes fungal identification based on direct sequencing of PCR products difficult, ...
journal_title:International journal of molecular sciences
pub_type: 杂志文章
doi:10.3390/ijms161025067
更新日期:2015-10-22 00:00:00
abstract::Our previous study indicated that the combination of salvianolic acid B (SalB) and ginsenoside Rg1 (Rg1), the main components of Salvia miltiorrhizae and Panax notoginseng, improves myocardium structure and ventricular function in rats with ischemia/reperfusion injury. The present study aimed to determine the safety o...
journal_title:International journal of molecular sciences
pub_type: 杂志文章
doi:10.3390/ijms161226176
更新日期:2015-12-09 00:00:00
abstract::In vitro chondrogenically differentiated mesenchymal stem cells (MSCs) have a tendency to undergo hypertrophy, mirroring the fate of transient "chondrocytes" in the growth plate. As hypertrophy would result in ossification, this fact limits their use in cartilage tissue engineering applications. During limb developmen...
journal_title:International journal of molecular sciences
pub_type: 杂志文章
doi:10.3390/ijms21041444
更新日期:2020-02-20 00:00:00
abstract::Radiation has a wide variety of effects on the liver. Fibrosis is a concern in medical fields as one of the acute effects of high-dose irradiation, such as with cancer radiotherapies. Cancer is also an important concern following exposure to radiation. The liver has an active metabolism and reacts to radiations. In ad...
journal_title:International journal of molecular sciences
pub_type: 杂志文章,评审
doi:10.3390/ijms19123855
更新日期:2018-12-03 00:00:00
abstract::Wallerian degeneration or nerve demyelination, arising from spinal nerve compression, is thought to bring on chronic neuropathic pain. The widely distributed metabotropic glutamate receptor subtype 5 (mGluR5) is involved in modulating nociceptive transmission. The purpose of this study was to investigate the potential...
journal_title:International journal of molecular sciences
pub_type: 杂志文章
doi:10.3390/ijms16034642
更新日期:2015-03-02 00:00:00
abstract::Besides being traditionally used to relieve hepatobiliary disorders, Cynara cardunculus L. has evidenced anticancer potential on triple-negative breast cancer (TNBC). This study highlights the antiproliferative effects of lipophilic extracts from C. cardunculus L. var. altilis (DC) leaves and florets, and of their maj...
journal_title:International journal of molecular sciences
pub_type: 杂志文章
doi:10.3390/ijms18010063
更新日期:2016-12-29 00:00:00
abstract::Balanced osteoclast and osteoblast activity is necessary for skeletal health, whereas unbalanced osteoclast activity causes bone loss in many skeletal conditions. A better understanding of pathways that regulate osteoclast differentiation and activity is necessary for the development of new therapies to better manage ...
journal_title:International journal of molecular sciences
pub_type: 杂志文章
doi:10.3390/ijms21031056
更新日期:2020-02-05 00:00:00
abstract::The juvenile hormone (JH) signalling and ecdysone signalling pathways are crucial endocrine signalling pathways that orchestrate the metamorphosis of insects. The metamorphic process, the morphological change from the immature to adult forms, is orchestrated by the dramatic reduction of JH and downstream transcription...
journal_title:International journal of molecular sciences
pub_type: 杂志文章
doi:10.3390/ijms20102431
更新日期:2019-05-16 00:00:00
abstract::Binding affinity prediction of potential drugs to target and off-target proteins is an essential asset in drug development. These predictions require the calculation of binding free energies. In such calculations, it is a major challenge to properly account for both the dynamic nature of the protein and the possible v...
journal_title:International journal of molecular sciences
pub_type: 杂志文章
doi:10.3390/ijms15010798
更新日期:2014-01-09 00:00:00
abstract::Background: Chronic skin wounds are a growing financial burden for healthcare providers, causing discomfort/immobility to patients. Whilst animal chronic wound models have been developed to allow for mechanistic studies and to develop/test potential therapies, such systems are not good representations of the human chr...
journal_title:International journal of molecular sciences
pub_type: 杂志文章
doi:10.3390/ijms19041001
更新日期:2018-03-27 00:00:00
abstract::Bacterial adhesion to the calcium phosphate surface is a serious problem in surgery. To prevent bacterial infection, the development of calcium-phosphate cements (CPCs) with bactericidal properties is indispensable. The aim of this study was to fabricate antibacterial CPCs and evaluate their biological properties. Sil...
journal_title:International journal of molecular sciences
pub_type: 杂志文章
doi:10.3390/ijms21113745
更新日期:2020-05-26 00:00:00
abstract::The emergence of multidrug resistance is always associated with more rapid tumor recurrence and metastasis. P-glycoprotein (P-gp), which is a well-known multidrug-efflux transporter, confers enhanced invasion ability in drug-resistant cells. Previous studies have shown that P-gp probably exerts its tumor-promoting fun...
journal_title:International journal of molecular sciences
pub_type: 杂志文章
doi:10.3390/ijms17101718
更新日期:2016-10-13 00:00:00
abstract::Understanding molecular interactions and regulatory mechanisms in tumor initiation, progression, and treatment response are key requirements towards advanced cancer diagnosis and novel treatment procedures in personalized medicine. Beyond decoding the gene expression, malfunctioning and cancer-related epigenetic pathw...
journal_title:International journal of molecular sciences
pub_type: 杂志文章
doi:10.3390/ijms18102066
更新日期:2017-09-28 00:00:00
abstract::The role of the gut microbiome in human health and disease is the focus of much attention. It has been widely agreed upon that our gut bacteria play a role in host immunity, nutrient absorption, digestion, metabolism, and other key drivers of health. Furthermore, certain microbial signatures and specific taxa have als...
journal_title:International journal of molecular sciences
pub_type: 杂志文章,评审
doi:10.3390/ijms21030924
更新日期:2020-01-30 00:00:00
abstract::A series of new 2-aminobenzamide derivatives (1-10) has been synthesized in good to excellent yields by adopting both conventional and/or a time-efficient microwave assisted methodologies starting from isatoic anhydride (ISA) and characterized on the basis of their physical, spectral and microanalytical data. Selected...
journal_title:International journal of molecular sciences
pub_type: 杂志文章
doi:10.3390/ijms15035115
更新日期:2014-03-21 00:00:00
abstract::Recent studies have shown that dexmedetomidine exerts an anti-inflammatory effect by reducing serum levels of inflammatory factors, however, the up-stream mechanism is still unknown. The transcription factor NF-κB enters the nucleus and promotes the transcription of its target genes, including those encoding the pro-i...
journal_title:International journal of molecular sciences
pub_type: 杂志文章
doi:10.3390/ijms15034049
更新日期:2014-03-06 00:00:00
abstract::Atherosclerosis is a multifactorial chronic disease that affects large arteries and may lead to fatal consequences. According to current understanding, inflammation and lipid accumulation are the two key mechanisms of atherosclerosis development. Animal models based on genetically modified mice have been developed to ...
journal_title:International journal of molecular sciences
pub_type: 杂志文章,评审
doi:10.3390/ijms21062097
更新日期:2020-03-18 00:00:00
abstract::Claudin-1 (CLDN1), a tight junctional protein, is highly expressed in lung cancer cells and may contribute to chemoresistance. A drug which decreases CLDN1 expression could be a chemosensitizer for enhancing the efficacy of anticancer drugs, but there is no such drug known. We found that PMTPV, a short peptide, which ...
journal_title:International journal of molecular sciences
pub_type: 杂志文章
doi:10.3390/ijms21165909
更新日期:2020-08-17 00:00:00
abstract::Endothelial cells and astrocytes preferentially express metabotropic P2Y nucleotide receptors, which are involved in the maintenance of vascular and neural function. Among these, P2Y1 and P2Y2 receptors appear as main actors, since their stimulation induces intracellular calcium mobilization and activates signaling ca...
journal_title:International journal of molecular sciences
pub_type: 杂志文章
doi:10.3390/ijms22020624
更新日期:2021-01-10 00:00:00
abstract::The aim of the present study was to determine aflatoxin levels in peanut products traded in the Northeast region of São Paulo, Brazil. To this end, 240 samples of peanut products traded in the cities of Araras, Leme, Pirassununga and Porto Ferreira were collected from June 2006 to May 2007. The samples were analyzed f...
journal_title:International journal of molecular sciences
pub_type: 杂志文章
doi:10.3390/ijms10010174
更新日期:2009-01-01 00:00:00