Nanodelivery systems for overcoming limited transportation of therapeutic molecules through the blood-brain barrier.

abstract：:Aim:   Histone deacetylases (HDACs) are one of the validated targets for cancer treatments. In our previous work, we designed a series of bis-substituted aromatic amide HDAC inhibitors (HDACis), among which compounds 7 and 8 showed promising anticancer effects. However, the low solubilities prevented their subsequent ...

journal_title：Future medicinal chemistry

authors： Yang F,Han L,Zhao N,Yang Y,Ge D,Zhang H,Chen Y

更新日期：2020-04-01 00:00:00

abstract：:This review aims to bring the reader up to date with the more recent ruthenium compounds that have been synthesized and tested for their cytotoxicity. The chemistry of these transition metal complexes will be introduced and the basic principles that govern their common behavior outlined. The recent history of establis...

journal_title：Future medicinal chemistry

authors： Page SM,Boss SR,Barker PD

更新日期：2009-06-01 00:00:00

abstract：:Fingolimod (FTY720) is a first-in-class, orally active, sphingosine 1-phosphate (S1P)-receptor modulator with a structure closely related to sphingosine. The compound was discovered by chemical modification of a natural product, myriocin. Phosphorylated form of FTY720 acts as a functional antagonist at S1P receptor ty...

journal_title：Future medicinal chemistry

authors： Chiba K,Adachi K

更新日期：2012-04-01 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

authors： Lin PJ,Tam YK

更新日期：2015-01-01 00:00:00

abstract：:More research effort needs to be invested in antimicrobial drug development to address the increasing threat of multidrug-resistant organisms. The enzyme DHPS has been a validated drug target for over 70 years as the target for the highly successful sulfa drugs. The use of sulfa drugs has been compromised by the wides...

journal_title：Future medicinal chemistry

authors： Hammoudeh DI,Zhao Y,White SW,Lee RE

更新日期：2013-07-01 00:00:00

abstract：:In comparison with other virus infections, such as HIV, HBV, HCV, influenza and herpes virus, dengue virus infections have received relatively little attention from a (chemo)therapeutic viewpoint, despite their global incidence (2.5 billion people estimated to be at risk) and absence of an effective prophylactic measu...

journal_title：Future medicinal chemistry

authors： De Clercq E

更新日期：2010-04-01 00:00:00

abstract：AIM:The use of 3D information has shown impact in numerous applications in drug design. However, it is often under-utilized and traditionally limited to specialists. We want to change that, and present an approach making 3D information and molecular modeling accessible and easy-to-use 'for the people'. METHODOLOGY/RES...

journal_title：Future medicinal chemistry

authors： Grebner C,Norrby M,Enström J,Nilsson I,Hogner A,Henriksson J,Westin J,Faramarzi F,Werner P,Boström J

更新日期：2016-09-01 00:00:00

abstract：:Mammalian target of rapamycin (mTOR) belongs to the atypical kinase family of phosphatidylinositol-3-kinase-related kinase and function as a master regulators of the switch between catabolic and anabolic metabolism. In the last decade mTOR has emerged as a therapeutic target for various diseases such as cancer, inflam...

journal_title：Future medicinal chemistry

authors： Roychowdhury A,Sharma R,Kumar S

更新日期：2010-10-01 00:00:00

abstract：:Spinal muscular atrophy (SMA) is an inherited neurodegenerative disease that results in progressive dysfunction of motor neurons of the anterior horn of the spinal cord. SMA is caused by the loss of full-length protein expression from the survival of motor neuron 1 (SMN1) gene. The disease has a unique genetic profile...

journal_title：Future medicinal chemistry

authors： Cherry JJ,Androphy EJ

更新日期：2012-09-01 00:00:00

abstract：:The pharmaceutical industry is facing numerous, well-documented challenges - from the effects of patent expirations to high attrition rates in the drug-development pipeline. Future Medicinal Chemistry has invited a group of leaders from academia and industry to express their views on where the industry is heading and ...

journal_title：Future medicinal chemistry

authors： Cottens S,Eaton M,Fuhr J,Geary S,Johnson DS,Li G,Raveglia L,Robertson GM,Westwell A

更新日期：2011-11-01 00:00:00

abstract：:New antibacterials that modulate less explored targets are needed to fight the emerging bacterial resistance. DNA gyrase and topoisomerase IV are attractive targets in this search. These are both type II topoisomerases that can cleave both DNA strands, and can thus alter DNA topology during replication or similar proc...

journal_title：Future medicinal chemistry

authors： Barančoková M,Kikelj D,Ilaš J

更新日期：2018-05-01 00:00:00

abstract：:The EGFR is one of the most popular targets for anticancer therapies and many drugs, such as erlotinib and gefitinib, have got enormous success in clinical treatments of cancer in past decade. However, the efficacy of these agents is often limited because of the quick emergence of drug resistance. Fundamental structur...

journal_title：Future medicinal chemistry

authors： Guan H,Du Y,Ning Y,Cao X

更新日期：2017-05-01 00:00:00

abstract：:Matrix metalloproteinases are zinc-dependent enzymes whose main function is to cleave the components of the extracellular matrix. Their overexpression is evident in all cancers but to date there is no satisfactory way to inhibit their actions. Here, we look at their types, their structures, their functions and the dev...

journal_title：Future medicinal chemistry

authors： King SE

更新日期：2016-01-01 00:00:00

abstract：:New Delhi Metallo β-lactamase-1 (NDM-1) is a member of the Metallo-β-lactamase family, capable of catalyzing the hydrolysis of all β-lactam antibiotics. The rapid dissemination of NDM producers, 'superbugs', has become a worldwide concern to health workers. Seventeen different variants of NDM have been reported so far...

journal_title：Future medicinal chemistry

authors： Khan S,Ali A,Khan AU

更新日期：2018-01-01 00:00:00

abstract：:The finding of promising drugs represents a huge challenge in cancer therapeutics, therefore it is important to seek out novel approaches and elucidate essential cellular processes in order to identify potential drug targets. Studies on DNA repair pathway suggested that an enzyme, PARP, which plays a significant role ...

journal_title：Future medicinal chemistry

authors： Kumar C,Rani N,Velan Lakshmi PT,Arunachalam A

更新日期：2017-01-01 00:00:00

abstract：:Chemokines and their receptors are integral components of the immune response, regulating lymphocyte development, homing and trafficking, and playing a key role in the pathophysiology of many diseases. Chemokine receptors have, therefore, become the target for both small-molecule, peptide and antibody therapeutics. Ch...

journal_title：Future medicinal chemistry

authors： Fricker SP,Metz M

更新日期：2014-01-01 00:00:00

abstract：:Diabetes mellitus is an increasing public health problem in the world. Type 2 diabetes is the most common type of diabetes whose complications contribute to its high death rate. It seriously impacts healthcare systems and patients' quality of life. Therefore, effective measures and new treatment strategies are needed ...

journal_title：Future medicinal chemistry

authors： Turdu G,Gao H,Jiang Y,Kabas M

更新日期：2018-05-01 00:00:00

abstract：:PEGylation is the covalent conjugation of PEG to therapeutic molecules. Protein PEGylation is a clinically proven approach for extending the circulation half-life and reducing the immunogenicity of protein therapeutics. Most clinically used PEGylated proteins are heterogeneous mixtures of PEG positional isomers conjug...

journal_title：Future medicinal chemistry

authors： Ginn C,Khalili H,Lever R,Brocchini S

更新日期：2014-01-01 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

authors： Hui M,Jian Z,Peiyuan Z,Zhenwei W,Huibin Z

更新日期：2018-04-01 00:00:00

abstract：:Several hundred genes associated or linked to obesity have been described in the scientific literature. Whereas many of these genes are potential targets for the treatment of obesity and associated conditions, none of them have permitted the developement of an efficient drug therapy. As proposed by the 'thrifty genoty...

journal_title：Future medicinal chemistry

authors： Braud S,Ciufolini M,Harosh I

更新日期：2010-12-01 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

authors： Lin MH,Hung CF,Hsu CY,Lin ZC,Fang JY

更新日期：2019-08-01 00:00:00

abstract：:Antibiotic drug discovery has been an essential field of research since the early 1900s, but the threat from infectious bacteria has only increased over the decades because of the emergence of widespread multidrug resistance. In this review, we discuss the recent advances in natural product, computational and medicina...

journal_title：Future medicinal chemistry

authors： Murphy KE,Sloan GF,Lawhern GV,Volk GE,Shumate JT,Wolfe AL

更新日期：2020-11-01 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

authors： Xiao X,He L,Chen Y,Wu L,Wang L,Liu Z

更新日期：2017-11-01 00:00:00

abstract：:Radiation-induced lung injury (RILI) is a common complication in cancer patients receiving local thoracic radiation and bone marrow transplantation conditioning. It is divided into early-stage radiation pneumonitis and advanced radiation fibrosis of the lung. This severely hampers the quality of life and survival of c...

journal_title：Future medicinal chemistry

authors： Xia C,Shi W,Zhang Y,Ding L,Gao L,Wang Q,Shao L,Dong L,Gao Y

更新日期：2020-12-01 00:00:00

abstract：:Retinal microvascular alterations have been observed during diabetic retinopathy (DR) due to the retinal susceptibility towards subtle pathological alterations. Therefore, retinal microvascular pathology is essential to understand the nature of retinal degenerations during DR. In this review, the role of retinal micro...

journal_title：Future medicinal chemistry

authors： Barot M,Gokulgandhi MR,Patel S,Mitra AK

更新日期：2013-03-01 00:00:00

abstract：:Aim: WHO Malaria report 2017 estimated 216 million cases of malaria and 445,000 deaths worldwide, with 91% of deaths affecting the African region. Results/methodology: Microwave promoted the synthesis of cycloalkyl amine substituted isoindoline-1,3-dione-4-aminoquinolines was urbanized for evaluating their antiplasmod...

journal_title：Future medicinal chemistry

authors： Rani A,Kumar S,Legac J,Adeniyi AA,Awolade P,Singh P,Rosenthal PJ,Kumar V

更新日期：2020-02-01 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

authors： Ripphausen P,Stumpfe D,Bajorath J

更新日期：2012-04-01 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

authors： Bessières M,Chevrier F,Roy V,Agrofoglio LA

更新日期：2015-01-01 00:00:00

abstract：:Aim: To determine the computer-predicted anticancer activity of mupirocin and to compare its activities with those determined for another polyene antibiotic, batumin. Materials & methods: Molecular docking, cytotoxicity assays, cell microscopy and cell cycle progression were studied in cancer and nontumorigenic cell l...

journal_title：Future medicinal chemistry

authors： Reva ON,Rademan S,Visagie MH,Lebelo MT,Gwangwa MV,Klochko VV,Joubert AM,Lall N

更新日期：2019-04-01 00:00:00

abstract：:FGFs and their receptors (FGFRs) are critical for many biologic processes, including angiogenesis, wound healing and tissue regeneration. Aberrations in FGFR signaling are common in cancer, making FGFRs a promising target in antitumor studies. To date, many FGFR inhibitors are being detected in clinical studies, and r...

journal_title：Future medicinal chemistry

authors： Xue WJ,Li MT,Chen L,Sun LP,Li YY

更新日期：2018-09-01 00:00:00