Abstract:
:Aim: Anticancer immunochemotherapy represents an attractive paradigm to improve therapeutic responses and reduce side effects. Results & methodology: Here, we show that a naturally occurring host defense peptide, HN-1 inhibited multiple malignant cells proliferation and tumor growth in a xenografted human breast tumor model. Acting through MAPK/NF-κB pathways, HN-1 induced a caspase-independent mitochondrial apoptosis, as indicated by a p53-dependent increase of Bax/Bcl-2 ratio and the nuclear translocation of apoptosis inducing factor. Besides, HN-1 augmented CD4+/CD8+ T cells in 4T1 mammary carcinoma model, by enhancing the serum levels of cancer immunity-associated effectors. Meanwhile, HN-1 decreased the angiogenesis and infiltration of the tumor-associated macrophages. Conclusion: HN-1 induces caspase-independent cancer cells apoptosis and boosts cancer-resolving immunity without inducing potentially harmful pro-inflammatory responses.
journal_name
Future Med Chemjournal_title
Future medicinal chemistryauthors
Qiao X,Yang H,Gao J,Cai S,Shi N,Wang M,Wang Y,Yu Hdoi
10.4155/fmc-2019-0100subject
Has Abstractpub_date
2019-10-01 00:00:00pages
2505-2525issue
19eissn
1756-8919issn
1756-8927journal_volume
11pub_type
杂志文章abstract::Richard H Ebright talks to Rachel Coleby, Commissioning Editor: Ebright is at Rutgers University (New Brunswick, NJ, USA), where he performs research on the structure, mechanism, and regulation of bacterial transcription and on antibacterial drug discovery targeting bacterial transcription. He has received research aw...
journal_title:Future medicinal chemistry
pub_type: 面试
doi:10.4155/fmc-2017-0188
更新日期:2017-10-01 00:00:00
abstract::Glioblastoma multiforme (GBM) is the most common primary malignant brain tumor in adults, associated with a high mortality rate and a survival of between 12 and 15 months after diagnosis. Due to current treatment limitations involving surgery, radiotherapy and chemotherapy with temozolamide, there is a high rate of tr...
journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc-2018-0521
更新日期:2019-09-01 00:00:00
abstract::Cancer, still in the limelight due to its dreadful nature, shows overexpression of multiple signaling macromolecules leading to failure of many chemotherapeutic agents and acquired resistance to chemotherapy. These factors highlight the significance of shifting toward targeted therapy in cancer research. Recently, ERK...
journal_title:Future medicinal chemistry
pub_type: 杂志文章
doi:10.4155/fmc-2019-0339
更新日期:2020-04-01 00:00:00
abstract::Although activity has been reported in vivo, free nucleic acid-based drugs are rapidly degraded and cleared following systemic administration. To address these challenges and improve the potency and bioavailability of genetic drugs, significant efforts have been made to develop effective delivery systems of which lipi...
journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc.15.108
更新日期:2015-01-01 00:00:00
abstract::Alzheimer's disease is a multifactorial syndrome, for which effective cures are urgently needed. Seeking for enhanced therapeutic efficacy, multitarget drugs have been increasingly sought after over the last decades. They offer the attractive prospect of tackling intricate network effects, but with the benefits of a s...
journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc-2016-0003
更新日期:2016-04-01 00:00:00
abstract::MRI has been recognized as one of the most applied medical imaging techniques in clinical practice. However, the presence of background signal coming from water protons in surrounding tissues makes sometimes the visualization of local contrast agents difficult. To remedy this, fluorine has been introduced as a reliabl...
journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc-2018-0463
更新日期:2019-05-01 00:00:00
abstract:AIM:Due to the complex nature of Alzheimer's disease, there is a renewed search for pleiotropic agents. RESULTS:Purine+coumarin hybrids have been synthesized and tested for the potential treatment of Alzheimer's disease. Hybrids 6, 4a-b, 14c and 14e inhibit significantly soybean lipoxygenase, whereas derivatives 14b, ...
journal_title:Future medicinal chemistry
pub_type: 杂志文章
doi:10.4155/fmc.14.158
更新日期:2015-01-01 00:00:00
abstract::Mammalian carbonic anhydrases (CAs; EC 4.2.1.1) of which 16 isoforms are known, are involved in important physiological functions. Their inhibition is exploited pharmacologically for the treatment of many diseases (glaucoma, edema, epilepsy, obesity, hypoxic tumors, neuropathic pain, etc.) but the activators were less...
journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc-2017-0223
更新日期:2018-03-01 00:00:00
abstract::Aim: Eight coumarin derivatives (1a-h) obtained from natural (-)-mammea A/BB (1) and 13 synthetic coumarins (2-14) had their cytotoxicity and biological activity evaluated against Mycobacterium tuberculosis H37Rv reference strain and multidrug-resistant clinical isolates. Materials & methods: Anti-M. tuberculosis acti...
journal_title:Future medicinal chemistry
pub_type: 杂志文章
doi:10.4155/fmc-2018-0281
更新日期:2020-09-01 00:00:00
abstract::Prodrug entrapment into nanocarriers for tumor delivery is a strategy to achieve a valid therapy with high efficiency. The prodrug contains anticancer agents conjugating with functional moieties or ligands so that the active component is released after metabolism in the body or tumor. The advantages of nanosystems for...
journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc-2018-0388
更新日期:2019-08-01 00:00:00
abstract:BACKGROUND:The F508del mutation impairs the trafficking of CFTR from endoplasmic reticulum to plasma membrane and is responsible of a severe form of cystic fibrosis. Trafficking can be improved by small organic molecules called 'correctors'. MATERIALS & METHODS:By different synthetic ways, we prepared 4-chloroanisole ...
journal_title:Future medicinal chemistry
pub_type: 杂志文章
doi:10.4155/fmc.14.118
更新日期:2014-01-01 00:00:00
abstract::The development of novel pharmaceutical treatments for disorders of the cerebral vasculature is a serious unmet medical need. These vascular disorders are typified by a disruption in the delicate Rho signaling equilibrium within the blood vessel wall. In particular, Rho kinase overactivation in the smooth muscle and e...
journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc.15.45
更新日期:2015-01-01 00:00:00
abstract::Existing therapies for allergic asthma are far from perfect: the global prevalence of disease increases despite them and they are poorly effective in dealing with the exacerbations that account for hospitalization and asthma deaths. Commercially, there are pressures on these existing medicines too--a growing threat fr...
journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc.12.204
更新日期:2013-02-01 00:00:00
abstract::It is increasingly clear that academic high-throughput screening (HTS) and virtual HTS triage suffers from a lack of scientists trained in the art and science of early drug discovery chemistry. Many recent publications report the discovery of compounds by screening that are most likely artifacts or promiscuous bioacti...
journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc.14.60
更新日期:2014-07-01 00:00:00
abstract::Nucleoside analogs are extremely useful for the development of therapeutic agents to control viral diseases and cancer. Among the numerous modifications on the nucleoside skeleton, replacement of the oxygen of the furanose ring by a CH2 group resulted in increased flexibility and higher resistance to phosphorylases an...
journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc.15.105
更新日期:2015-01-01 00:00:00
abstract:BACKGROUND:The acquirement of resistance by microorganisms to the antimicrobial arsenal is a threat to public health. A recent WHO report estimated that 1.3 million HIV-negative people and 0.38 million HIV-positive people died from TB in 2009. Various forms of cancer account for a high percentage of deaths in both wome...
journal_title:Future medicinal chemistry
pub_type: 杂志文章
doi:10.4155/fmc.12.57
更新日期:2012-06-01 00:00:00
abstract::The bromodomain proteins, known as the key targets in epigenetics, are 'readers' of acetylated lysine of histones. As a member of bromodomain proteins, bromodomain-containing protein 9 (BRD9) is a subunit of mammalian SWI/SNF chromatin remodeling complexes. However, the biological functions and the potential applicati...
journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc-2017-0243
更新日期:2018-04-01 00:00:00
abstract::Responsive optical probes play a vital role in following and understanding biological events. In this review, we focus on the use of lanthanide complexes as molecular probes, as they offer many advantages in imaging and assays, particularly when used in time-gated protocols. We describe systems that illustrate the key...
journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc.09.173
更新日期:2010-03-01 00:00:00
abstract::Camellia oleifera Abel is a member of Camellia, and its seeds are used to extract Camellia oil, which is generally used as cooking oil in the south of China. Camellia oil consists of unsaturated fatty acids, tea polyphenol, squalene, saponin, carrot element and vitamins, etc. The seed remains after oil extraction of C...
journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc-2017-0109
更新日期:2017-11-01 00:00:00
abstract::Kinetic and thermodynamic ligand-protein binding parameters are gaining growing importance as key information to consider in drug discovery. The determination of the molecular structures, using particularly x-ray and NMR techniques, is crucial for understanding how a ligand recognizes its target in the final binding c...
journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc-2016-0224
更新日期:2017-04-01 00:00:00
abstract:AIM:The present study was carried out to assess a new series of triazoloquinazolines 1-40 for their antioxidant activities using 1,1-diphenyl-2-picryl hydrazyl radical scavenging, ferric reduction antioxidant power and reducing power capability assays. RESULTS:All triazoloquinazolines 1-40 exhibited antioxidant activi...
journal_title:Future medicinal chemistry
pub_type: 杂志文章
doi:10.4155/fmc-2017-0224
更新日期:2018-02-01 00:00:00
abstract:BACKGROUND:The understanding of biomolecular interactions ultimately depends on knowledge about the structural and dynamic details of the interacting system. Rational structure-based drug design implements computational methodology in this rationale. DISCUSSION:Together with increasing throughput of structural biology...
journal_title:Future medicinal chemistry
pub_type: 杂志文章
doi:10.4155/fmc.09.7
更新日期:2009-04-01 00:00:00
abstract::Structure-based virtual screening makes explicit or implicit use of 3D target structure information to detect novel active compounds. Results of nearly 300 currently available original applications have been analyzed to characterize the state-of-the-art in this field. Compound selection from docking calculations is mu...
journal_title:Future medicinal chemistry
pub_type: 杂志文章
doi:10.4155/fmc.12.18
更新日期:2012-04-01 00:00:00
abstract::CDK12 and CDK13 are Ser/Thr protein kinases that regulate transcription and co-transcriptional processes. Genetic silencing of CDK12 is associated with genomic instability in a variety of cancers, including difficult-to-treat breast, ovarian, colorectal, brain and pancreatic cancers, and is synthetic lethal with PARP,...
journal_title:Future medicinal chemistry
pub_type: 杂志文章
doi:10.4155/fmc-2020-0240
更新日期:2021-01-01 00:00:00
abstract:AIM:Cancer is among the leading causes of death worldwide. Medical interest has focused on macrocyclic polyamines because of their properties as antitumor agents. Results/Methodology: We have designed and synthesized a series of 1,2-diaminocyclohexane derivatives with notable in vitro antiproliferative activities again...
journal_title:Future medicinal chemistry
pub_type: 杂志文章
doi:10.4155/fmc-2016-0212
更新日期:2017-03-01 00:00:00
abstract::Filamenting temperature-sensitive mutant Z (FtsZ), an essential cell division protein in bacteria, has recently emerged as an important and exploitable antibacterial target. Cytokinesis in bacteria is regulated by the assembly dynamics of this protein, which is ubiquitously present in eubacteria. The perturbation of F...
journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc-2016-0041
更新日期:2016-06-01 00:00:00
abstract::This review summarizes the basic milestones of the research of 5-azacytosine nucleosides chronologically from their discovery and anticancer activity identification, through to subsequent unveiling of their mechanism of action based on DNA hypomethylation and tumor-suppressor gene reactivation, to the final US FDA app...
journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc.12.36
更新日期:2012-05-01 00:00:00
abstract::At present, the polysaccharide antitumor research is focused on how to further improve the antitumor activity of polysaccharides. The structural modification of polysaccharides can enhance their antitumor activity to a certain extent. The antitumor mechanisms of polysaccharide derivatives mainly contain the inducing a...
journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc-2017-0132
更新日期:2017-10-01 00:00:00
abstract:BACKGROUND:Due to the complex nature of Alzheimer's disease, there is a renewed and growing search for multitarget drugs. RESULTS:Donepezil-ferulic acid hybrids (DFAHs) were prepared by the one-pot Ugi-4CR in low-to-moderate yields. DFAHs are potent antioxidant agents, showing oxygen radical absorbance capacity values...
journal_title:Future medicinal chemistry
pub_type: 杂志文章
doi:10.4155/fmc.14.148
更新日期:2015-01-01 00:00:00
abstract:BACKGROUND:Traditional and current opioid pharmacology is fundamentally based on interactions between opioid receptors and compounds isolated from natural sources. Adverse effects associated with opioids have led to the search for compounds with diminished side effects. DISCUSSION:Recent discoveries of non-nitrogenous...
journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc.09.22
更新日期:2009-05-01 00:00:00