PAAP: a web server for predicting antihypertensive activity of peptides.

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：AIM:Alzheimer's disease is a progressive and neurodegenerative disorder of the CNS, affecting elderly people. The current pharmacological approach is based on the improvement of cholinergic neurotransmission by inhibiting acetylcholinesterase (AChE) with AChE inhibitors. The disease is also characterized by the acceler...

journal_title：Future medicinal chemistry

authors： de Almeida JR,Figueiro M,Almeida WP,de Paula da Silva CHT

更新日期：2018-05-01 00:00:00

abstract：:Around 70-80% of drugs used in traditional Tibetan medicine (TTM) come from Qinghai Tibet Plateau, the majority of which are plants. The biological and medicinal culture diversity on Qinghai Tibet Plateau are amazing and constitute a less tapped resource for innovative drug research and development. Meanwhile, the pro...

journal_title：Future medicinal chemistry

authors： Hao DC,Xiao PG,Liu C

更新日期：2018-11-30 00:00:00

abstract：:Metal complexes have been the subject of numerous investigations in oncology but, despite the plethora of newly synthesized compounds, their precise mechanisms of action remain generally unknown or, for the best, incompletely determined. The continuous development of efficient and sensitive techniques in analytical ch...

journal_title：Future medicinal chemistry

authors： Marloye M,Berger G,Gelbcke M,Dufrasne F

更新日期：2016-12-01 00:00:00

abstract：:The emergence of antimicrobial resistance has created a need for the development of novel antibacterial therapies to treat infection. Natural products that exhibit antibacterial activity offer validated starting points for library generation, and the authors report here that small molecule mimics of tetramate-containi...

journal_title：Future medicinal chemistry

authors： Jeong YC,Moloney MG

更新日期：2015-01-01 00:00:00

abstract：:Every organism is in contact with numerous small molecules (<1000 Da). Chemicals may cause or trigger adverse health effects, including diseases of the immune system. They may also be exploited as drugs. In this review, we look at the interaction between small molecules and the immune system. We discuss the hapten and...

journal_title：Future medicinal chemistry

authors： Kadow S,Jux B,Chmill S,Esser C

更新日期：2009-12-01 00:00:00

abstract：:Nicotinic receptors are membrane proteins involved in several physiological processes. They are considered suitable drug targets for various CNS disorders or conditions, as shown by the large number of compounds which have entered clinical trials. In recent years, nonconventional agonists have been discovered: positiv...

journal_title：Future medicinal chemistry

authors： Manetti D,Bellucci C,Chiaramonte N,Dei S,Teodori E,Romanelli MN

更新日期：2018-02-01 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：: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

authors： Krečmerová M,Otmar M

更新日期：2012-05-01 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：:Carbonic anhydrases (CAs; EC 4.2.1.1) are well known zinc metalloproteins involved in the catalysis of a very simple but essential physiological reaction: carbon dioxide hydration to bicarbonate and proton. These enzymes are of clinical relevance in cancer therapy as among the 15 isoforms known in humans, two cell sur...

journal_title：Future medicinal chemistry

authors： Supuran CT,Winum JY

更新日期：2015-01-01 00:00:00

abstract：:Many natural products that consist of quinoline core are found to be bioactive and the versatility of quinoline and its derivatives have attracted great attention in the field of drug development. As a result, in recent years, many green and sustainable synthetic approaches for the synthesis of structurally diverse qu...

journal_title：Future medicinal chemistry

authors： Chung PY,Bian ZX,Pun HY,Chan D,Chan AS,Chui CH,Tang JC,Lam KH

更新日期：2015-01-01 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

authors： Skjevik AA,Teigen K,Martinez A

更新日期：2009-04-01 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：AIM:Triterpenes are natural compounds, whose wide biological activity predestines them for application as promising new chemotherapeutics. In this paper, we report the results of our investigations into the substitution of oleanolic acid with aromatic and nitroaromatic moieties acting as bioreducing agents. RESULTS:Th...

journal_title：Future medicinal chemistry

authors： Bednarczyk-Cwynar B,Ruszkowski P,Jarosz T,Krukiewicz K

更新日期：2018-03-01 00:00:00

abstract：BACKGROUND:Benzimidazole derivatives are promising compounds for the treatment of parasitic infections. The structure-activity relationships of 91 benzimidazoles with activity against Trichomonas vaginalis and Giardia intestinalis were analyzed using a novel activity landscape modeling approach. RESULTS:We identified ...

journal_title：Future medicinal chemistry

authors： Aguayo-Ortiz R,Pérez-Villanueva J,Hernández-Campos A,Castillo R,Meurice N,Medina-Franco JL

更新日期：2014-03-01 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：: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：: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：:The cystic fibrosis transmembrane conductance regulator (CFTR) is a cAMP-regulated chloride channel localized primarily at the apical surfaces of epithelial cells lining airway, gut and exocrine glands, where it is responsible for transepithelial salt and water transport. Several human diseases are associated with an ...

journal_title：Future medicinal chemistry

authors： Zhang W,Fujii N,Naren AP

更新日期：2012-03-01 00:00:00

abstract：:The use of electron density-based molecular descriptors in drug research, particularly in quantitative structure--activity relationships/quantitative structure--property relationships studies, is reviewed. The exposition starts by a discussion of molecular similarity and transferability in terms of the underlying elec...

journal_title：Future medicinal chemistry

authors： Matta CF,Arabi AA

更新日期：2011-06-01 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：:Mycobacterium tuberculosis (Mtb) acquires non-heme iron through salicylate-derived siderophores termed mycobactins whereas heme iron is obtained through a cascade of heme uptake proteins. Three proteins are proposed to mediate Mtb heme iron uptake, a secreted heme transporter (Rv0203), and MmpL3 and MmpL11, which are ...

journal_title：Future medicinal chemistry

authors： Owens CP,Chim N,Goulding CW

更新日期：2013-08-01 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：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

authors： Benchekroun M,Ismaili L,Pudlo M,Luzet V,Gharbi T,Refouvelet B,Marco-Contelles J

更新日期：2015-01-01 00:00:00

abstract：BACKGROUND:Histone lysine demethylases (KDMs) are well-recognized targets in oncology drug discovery. They function at the post-translation level controlling chromatin conformation and gene transcription. KDM1A is a flavin adenine dinucleotide-dependent amine oxidase, overexpressed in several tumor types, including acu...

journal_title：Future medicinal chemistry

authors： Trifirò P,Cappa A,Brambillasca S,Botrugno OA,Cera MR,Zuffo RD,Dessanti P,Meroni G,Thaler F,Villa M,Minucci S,Mercurio C,Varasi M,Vianello P

更新日期：2017-07-01 00:00:00

abstract：:Solomon Nwaka was born in Nigeria and grew up seeing at first hand the impact of neglected diseases. His research efforts have taken him across the globe, in both the developed and developing world. Following posts in academia, industry and at the Medicines for Malaria Venture, he is now at the WHO where he is engaged...

journal_title：Future medicinal chemistry

authors： Nwaka S

更新日期：2011-09-01 00:00:00

abstract：AIM:Research of the antitumor properties of biscationic compounds has received significant attention over the last few years. RESULTS:A novel family of 1,1'-([2,2'-bipyridine]-5,5'-diylbis(methylene))bis-substituted bromide (9a-k), containing two nitrogen atoms in the linker, considered as hypothetical hydrogen bond a...

journal_title：Future medicinal chemistry

authors： Castro-Navas FF,Schiaffino-Ortega S,Carrasco-Jimenez MP,Ríos-Marco P,Marco C,Espinosa A,Gallo MA,Mariotto E,Basso G,Viola G,Entrena-Guadix A,López-Cara LC

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：:Cyclin-dependent kinase 7 (CDK7) plays crucial roles in the regulation of cell cycle and transcription that are tightly associated with cancer development and metastasis. The recent identification of the first covalent inhibitor which possesses high specificity against CDK7 prompts intense studies on designing highly ...

journal_title：Future medicinal chemistry

authors： Wang M,Wang T,Zhang X,Wu X,Jiang S

更新日期：2020-05-01 00:00:00