Dipeptidyl peptidase-4 inhibition: linking chemical properties to clinical safety.

abstract：:Among the members of the 5'-nucleotidase family, there is only one membrane-bound ectosolic isoenzyme. This esterase prefers AMP as substrate but can hydrolyze a number of purine and pyrimidine phosphorylated compounds, indicating that no evolutive pressure to develop a more restricted specificity was exerted on this ...

journal_title：Current medicinal chemistry

authors： Tozzi MG,Pesi R,Allegrini S

更新日期：2013-01-01 00:00:00

abstract：:Staphylococcus aureus is a notorious pathogenic bacterium causing a wide range of diseases from soft-tissue contamination, to more serious and deep-seated infections. This species is highlighted by its ability to express several kinds of virulence factors and to acquire genes related to drug resistance. Target this nu...

journal_title：Current medicinal chemistry

authors： Diniz RC,Soares LW,Nascimento da Silva LC

更新日期：2018-01-01 00:00:00

abstract：:Drug-loaded nanoparticles have shown great potential in the study of carriers for disease-targeting drug delivery. Drug-loaded nanoparticles are excellent in keeping the drug in the systemic circulation for a prolonged period of time, introducing targeting molecules to improve targeting efficiency and to reduce side e...

journal_title：Current medicinal chemistry

authors： Tu Q,Zhang Y,Liu R,Wang JC,Li L,Nie N,Liu A,Wang L,Liu W,Ren L,Wang X,Wang J

更新日期：2012-01-01 00:00:00

abstract：:Chagas disease is one of the most important endemic diseases in Latin America, caused by Trypanosoma cruzi. The drugs used for the treatment of this disease, nifurtimox and benznidazole, are toxic and present severe side effects. The need of effective drugs, without adverse effects, has stimulated the search for new c...

journal_title：Current medicinal chemistry

authors： Salas CO,Faúndez M,Morello A,Maya JD,Tapia RA

更新日期：2011-01-01 00:00:00

abstract：:In the course of studying human mucin MUC1, the attitude towards this molecule has been changing time and again. Initially, the list of presumable functions of MUC1 was restricted to protecting and lubricating epithelium. To date, it is assumed to play an important role in cell signaling as well as in all stages of on...

journal_title：Current medicinal chemistry

authors： Syrkina MS,Vassetzky YS,Rubtsov MA

更新日期：2019-01-01 00:00:00

abstract：:Rubus species (family Rosaceae) have been cultivated for centuries for their fruits. These and other parts of the plants have been used traditionally for therapeutic purposes. This article highlights these and the potential they can offer. The constituents reported in the various species and those demonstrated to exhi...

journal_title：Current medicinal chemistry

authors： Patel AV,Rojas-Vera J,Dacke CG

更新日期：2004-06-01 00:00:00

abstract：:β-Aryl-β-amino acids constitute very useful scaffolds able to lead, via various intra-molecular cyclisation reactions, to a great diversity of cyclic derivatives with numerous biological and therapeutic properties. The present article aims at reporting an exhaustive overview of these ring-closure sequences and their a...

journal_title：Current medicinal chemistry

authors： Rochais C,Rault S,Dallemagne P

更新日期：2010-01-01 00:00:00

abstract：:Type 2 diabetes mellitus (DM) is a public health burden and its co-existence with hypertension is long established in the context of the metabolic syndrome. Both DM and hypertension are major risk factors, for end-stage renal disease, cardiovascular events and mortality. Strict blood pressure (BP) control in diabetics...

journal_title：Current medicinal chemistry

authors： Loutradis C,Papadopoulou E,Angeloudi E,Karagiannis A,Sarafidis P

更新日期：2020-01-01 00:00:00

abstract：:Infections with Mycobacterium tuberculosis, the causative agent of tuberculosis, are difficult to treat using currently available chemotherapeutics. Clinicians agree on the urgent need for novel drugs to treat tuberculosis. In this mini review, we summarize data that prompts the consideration of DNA repair-associated ...

journal_title：Current medicinal chemistry

authors： Minias A,Brzostek A,Dziadek J

更新日期：2019-01-01 00:00:00

abstract：:Tuberculosis (TB) which is caused by the resilient pathogen Mycobacterium tuberculosis (MTB) has re-emerged to become a leading public health problem in the world. The growing number of multi-drug resistant MTB strains and the more recently emerging problem with the extensively drug resistant strains of the pathogen a...

journal_title：Current medicinal chemistry

authors： Viganor L,Skerry C,McCann M,Devereux M

更新日期：2015-01-01 00:00:00

abstract：:Akuammiline alkaloids are a family of monoterpene indole alkaloids of renewed medicinal interest. These bases act as ligands for a heterogeneous group of molecular targets and, consequently, display a wide variety of pharmacological activities. For example, pseudoakuammigine (2) exhibits opioid activity in vivo, echit...

journal_title：Current medicinal chemistry

authors： Ramírez A,García-Rubio S

更新日期：2003-09-01 00:00:00

abstract：BACKGROUND:Nitric oxide (NO) plays important regulatory roles in a plethora of biological functions and thus holds tremendous potential to be exploited for clinical uses. However, the chemistries in the molecular design of nano-nitric oxide delivery systems is currently lacking. OBJECTIVE:The overarching aim of this r...

journal_title：Current medicinal chemistry

authors： Nguyen KT,Wu Z,Huang T,Tay CY

更新日期：2018-01-01 00:00:00

abstract：:Amyotrophic lateral sclerosis (ALS) is an age-related neurodegenerative disorder that is believed to have complex genetic and environmental influences in the pathogenesis, but etiologies are unidentified for most patients. Until the major causes are better defined, drug development is directed at downstream pathophysi...

journal_title：Current medicinal chemistry

authors： Blasco H,Mavel S,Corcia P,Gordon PH

更新日期：2014-01-01 00:00:00

abstract：: ...

journal_title：Current medicinal chemistry

authors： Poplawski T

更新日期：2019-01-01 00:00:00

abstract：BACKGROUND:A great effort has been made to develop efficacious antiviral drugs, but many viral infections are still lack of efficient antiviral therapies so far. The related exploration of natural products to fight viruses has been raised in recent years. Natural compounds with structural diversity and complexity offer...

journal_title：Current medicinal chemistry

authors： Wu YH,Zhang BY,Qiu LP,Guan RF,Ye ZH,Yu XP

更新日期：2017-01-01 00:00:00

abstract：:Protein C is a vitamin K-dependent anticoagulant serine protease zymogen in plasma which upon activation by the thrombin-thrombomodulin complex down-regulates the coagulation cascade by degrading cofactors Va and VIIIa by limited proteolysis. In addition to its anticoagulant function, activated protein C (APC) also bi...

journal_title：Current medicinal chemistry

authors： Rezaie AR

更新日期：2010-01-01 00:00:00

abstract：:The need for innovation in research is leading to an increased use of imaging biomarkers, which have shown to reduce timings and increase productivity, thus saving costs. PET and SPECT neurotransmission imaging has shown usefulness in the discovery and development of drugs for the central nervous system, providing uni...

journal_title：Current medicinal chemistry

authors： Catafau AM,Bullich S

更新日期：2013-01-01 00:00:00

abstract：:Studies on enzyme inhibition remain an important area of pharmaceutical research since these studies have led to the discoveries of drugs useful in a variety of physiological conditions. The enzyme inhibitors can interact with enzymes and block their activity towards natural substrates. Urease inhibitors have recently...

journal_title：Current medicinal chemistry

authors： Amtul Z,Rahman AU,Siddiqui RA,Choudhary MI

更新日期：2002-07-01 00:00:00

abstract：:Frontotemporal Lobar Degeneration (FTLD) is characterized by behavioral changes, executive dysfunctions, and language impairment, sustained by different neuropathological patterns. The collective efforts of clinical, pathological and genetic studies have recently opened new insights into the underpinnings of pathologi...

journal_title：Current medicinal chemistry

authors： Bigni B,Premi E,Pilotto A,Padovani A,Borroni B

更新日期：2012-01-01 00:00:00

abstract：:Obesity is a chronic disease characterized by the accumulation of excess adipose tissue associated with an increased risk of multiple morbidities and mortality. At the present time, only three drugs have been approved by the Food and Drug Administration (FDA) for the treatment of obesity. Agonists and antagonists of s...

journal_title：Current medicinal chemistry

authors： Rivera G,Bocanegra-García V,Galiano S,Cirauqui N,Ceras J,Pérez S,Aldana I,Monge A

更新日期：2008-01-01 00:00:00

abstract：:Over the past few decades, remarkable advances have been achieved in cancer therapy, including chemotherapeutic agents, their mode of application and more broader therapeutic strategies. Promising new therapeutic targets have emerged in the past ten years as a result of recent advances in our understanding of the path...

journal_title：Current medicinal chemistry

authors： Dobashi Y,Takehana T,Ooi A

更新日期：2003-12-01 00:00:00

abstract：:Matrix metalloproteinases (MMPs) are essential for the degradation and turnover of components of the extracellular matrix (ECM) and, when pathologically elevated, mediate connective tissue loss (including bone destruction) in various inflammatory and other diseases. Tetracyclines (TCs) are known inhibitors of mammalia...

journal_title：Current medicinal chemistry

authors： Zhang Y,Gu Y,Lee HM,Hambardjieva E,Vranková K,Golub LM,Johnson F

更新日期：2012-01-01 00:00:00

abstract：:Coumarins are of many different structures. They constitute an important class of pharmacological agents possessing a range of different physiological activities including anti-cancer, anti-oxidant, anti- inflammation, anti-HIV, anti-coagulant, anti-bacterial, analgesic and comparative immune-modulation. Recently, cou...

journal_title：Current medicinal chemistry

authors： Wu L,Wang X,Xu W,Farzaneh F,Xu R

更新日期：2009-01-01 00:00:00

abstract：:Mast cells are best known as central effector cells in IgE-mediated type I allergic diseases including asthma and hay fever. An increasing amount of evidence, however, has demonstrated that mast cells are sentinel cells playing a critical role in host defense against invading microbes. Mast cells are located immediate...

journal_title：Current medicinal chemistry

authors： Matsuguchi T

更新日期：2012-01-01 00:00:00

abstract：BACKGROUND:The large increase in epidemiological studies on night shift work is due to the important effects of night shift work on workers' health and psychophysical wellbeing. The short-term effects-insomnia, difficulties in managing work and private life, lower work performance, and more work and extra-work accident...

journal_title：Current medicinal chemistry

authors： Ferri GM,Cavone D,Intranuovo G,Macinagrossa L

更新日期：2019-01-01 00:00:00

abstract：:Gossypol, a disesquiterpene from cottonseed, exhibits multiple biological properties, including male antifertility activity and anticancer activity. Gossypol also inhibits the growth of numerous parasitic organisms and shows antiviral activity against a number of enveloped viruses, including the AIDS virus. Derivative...

journal_title：Current medicinal chemistry

authors： Vander Jagt DL,Deck LM,Royer RE

更新日期：2000-04-01 00:00:00

abstract：:Ornithine transcarbamylase (OTC; EC 2.1.3.3) is a one-carbon-unit transferring enzyme that synthesizes citrulline using ornithine and carbamoylphosphate as substrates. It is involved in the metabolic transformation of arginine and proline, and it participates in the urea cycle in vertebrates and in the formation of pu...

journal_title：Current medicinal chemistry

authors： Díaz-Muñoz M,Hernández-Muñoz R

更新日期：2010-01-01 00:00:00

abstract：:Current strategies in pharmaceutical research comprise two methodologically different but complementary approaches for lead finding purposes, namely the random screening of compound libraries and the structure-based effort, commonly termed rational drug design. The structure-based approach is aimed to exploit 3D struc...

journal_title：Current medicinal chemistry

authors： Müller G

更新日期：2000-09-01 00:00:00

abstract：:The concept of click chemistry represented by the formation of the 1,2,3-triazole core has found wide application in drug discovery, particularly in the early discovery phases and the lead optimization process. 1,2,3-Triazoles ha ve attracted considerable attention in recent years because of their wide range of biolog...

journal_title：Current medicinal chemistry

authors： Raic-Malic S,Mescic A

更新日期：2015-01-01 00:00:00

abstract：:Cellular interactions among platelets, leukocytes and endothelial cells are considered as a major cause of inflammation and atherosclerosis in many diseases. Via exposed surface receptors and released soluble substances, activated platelets play a crucial role in the initiation of inflammatory processes, resulting in ...

journal_title：Current medicinal chemistry

authors： Nagy B Jr,Miszti-Blasius K,Kerenyi A,Clemetson KJ,Kappelmayer J

更新日期：2012-01-01 00:00:00