Molecular hybridization: a useful tool in the design of new drug prototypes.

Abstract:

:Molecular hybridization is a new concept in drug design and development based on the combination of pharmacophoric moieties of different bioactive substances to produce a new hybrid compound with improved affinity and efficacy, when compared to the parent drugs. Additionally, this strategy can result in compounds presenting modified selectivity profile, different and/or dual modes of action and reduced undesired side effects. So, in this paper, we described several examples of different strategies for drug design, discovery and pharmacomodulation focused on new innovative hybrid compounds presenting analgesic, anti-inflammatory, platelet anti-aggregating, anti-infectious, anticancer, cardio- and neuroactive properties.

journal_name

Curr Med Chem

authors

Viegas-Junior C,Danuello A,da Silva Bolzani V,Barreiro EJ,Fraga CA

doi

10.2174/092986707781058805

subject

Has Abstract

pub_date

2007-01-01 00:00:00

pages

1829-52

issue

17

eissn

0929-8673

issn

1875-533X

journal_volume

14

pub_type

杂志文章,评审
  • L-type voltage-dependent calcium channels as therapeutic targets for neurodegenerative diseases.

    abstract::Ca(2+) is a highly versatile intracellular second messenger in the central nervous system, and regulates many complicated cellular processes, including excitation, plasticity and apoptosis. Influx of Ca(2+) from the extracellular fluid is required for sustained elevation of the cytosolic Ca(2+) concentration and full ...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/092986712803341430

    authors: Yagami T,Kohma H,Yamamoto Y

    更新日期:2012-01-01 00:00:00

  • Management of NSAID/aspirin-induced small intestinal damage by GI-sparing NSAIDs, anti-ulcer drugs and food constituents.

    abstract::Recent advances in endoscopic techniques such as capsule endoscopy have revealed that aspirin and other nonsteroidal antiinflammatory drugs (NSAIDs) often cause mucosal lesions not only in the upper gastrointestinal tract, but also in the small intestine in humans. Gastric and duodenal lesions caused by NSAIDs can be ...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/092986712803413980

    authors: Satoh H,Takeuchi K

    更新日期:2012-01-01 00:00:00

  • The glutamate hypothesis in ALS: pathophysiology and drug development.

    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

    pub_type: 杂志文章,评审

    doi:10.2174/0929867321666140916120118

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

    更新日期:2014-01-01 00:00:00

  • New drugs for HDL-C disorders: the beginning.

    abstract::For more than 20 years there has been increasing interest in the development of novel therapies to raise levels of high-density lipoprotein cholesterol (HDL-C). However, well publicized failures of recent clinical trials of agents that raise HDL-C levels have stimulated considerable controversy with regard to the pote...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/0929867321666140414104130

    authors: Duong M,Nicholls SJ

    更新日期:2014-01-01 00:00:00

  • Proteasome inhibition: a promising strategy for treating cancer, but what about neurotoxicity?

    abstract::The inhibition of protein degradation through the ubiquitin-proteasome pathway is a recently developed approach to cancer treatment which extends the range of cellular targets for chemotherapy. This therapeutic strategy is very interesting since the proteasomes carry out the regulated degradation of unnecessary or dam...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/092986708786848622

    authors: Gilardini A,Marmiroli P,Cavaletti G

    更新日期:2008-01-01 00:00:00

  • Managing the liabilities arising from structural alerts: a safe philosophy for medicinal chemists.

    abstract::Bioactivation of xenobiotics can, in certain circumstances, result in the formation of reactive electrophilic species. These reactive metabolites may covalently modify proteins and macromolecules and it has been suggested that protein modification is a key initial step in provoking idiosyncratic adverse drug reactions...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/092986711796391714

    authors: Edwards PJ,Sturino C

    更新日期:2011-01-01 00:00:00

  • Neuropeptide-derived antimicrobial peptides from invertebrates for biomedical applications.

    abstract::Since the beginning of the 20th century, important medicinal progress has led medical doctors to think that the end of devastating epidemics has arrived. In 1930, the discovery of sulfamides and penicillin opened a wide area of applications able to fight against bacterial infections. However, almost all antibiotics we...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/092986705774933470

    authors: Salzet M

    更新日期:2005-01-01 00:00:00

  • Impact of Natural Dietary Agents on Multiple Myeloma Prevention and Treatment: Molecular Insights and Potential for Clinical Translation.

    abstract::Chemoprevention is based on the use of non-toxic, pharmacologically active agents to prevent tumor progression. In this regard, natural dietary agents have been described by the most recent literature as promising tools for controlling onset and progression of malignancies. Extensive research has been so far performed...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/0929867325666180629153141

    authors: Raimondi L,De Luca A,Giavaresi G,Barone A,Tagliaferri P,Tassone P,Amodio N

    更新日期:2020-01-01 00:00:00

  • Boswellic acids: biological actions and molecular targets.

    abstract::Gum resin extracts of Boswellia species have been traditionally applied in folk medicine for centuries to treat various chronic inflammatory diseases, and experimental data from animal models and studies with human subjects confirmed the potential of B. spec extracts for the treatment of not only inflammation but also...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/092986706779010333

    authors: Poeckel D,Werz O

    更新日期:2006-01-01 00:00:00

  • The renin-angiotensin system: new insight into old therapies.

    abstract::Although the renin-angiotensin system (RAS) is already an old acquaintance, there are often exciting discoveries that improve our knowledge of it and open new therapeutic possibilities. Moreover, well-established drugs, such as angiotensin-converting enzyme inhibitors (ACEI), angiotensin receptor blockers (ARB), or be...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/0929867311320100008

    authors: Ramírez-Sánchez M,Prieto I,Wangensteen R,Banegas I,Segarra AB,Villarejo AB,Vives F,Cobo J,de Gasparo M

    更新日期:2013-01-01 00:00:00

  • Targeting DNA Repair Systems in Antitubercular Drug Development.

    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

    pub_type: 杂志文章,评审

    doi:10.2174/0929867325666180129093546

    authors: Minias A,Brzostek A,Dziadek J

    更新日期:2019-01-01 00:00:00

  • Thiol proteins, redox modulation and parenchymal lung disease.

    abstract::The lung is a unique organ in terms of its direct exposure to high levels of oxygen and reactive compounds. Several parenchymal lung diseases (e.g. emphysema associated with smoking and a number of fibrotic lung disorders) have been proposed to be due to the exposure of the lung to exogenous irritants leading to local...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/092986707779313345

    authors: Kinnula VL,Vuorinen K,Ilumets H,Rytilä P,Myllärniemi M

    更新日期:2007-01-01 00:00:00

  • Pyridine Based Antitumour Compounds Acting at the Colchicine Site.

    abstract::Antimitotics binding at the colchicine site of tubulin are important antitumour and vascular disrupting agents. Pyridines and azines are privileged scaffolds in medicinal chemistry and in recent years many colchicine site ligands (CSL) have incorporated them into their structures with the aim of improving their pharma...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/092986732311160420104823

    authors: Álvarez R,Aramburu L,Puebla P,Caballero E,González M,Vicente A,Medarde M,Peláez R

    更新日期:2016-01-01 00:00:00

  • The influence of a half-marathon race upon cardiac troponin T release in adolescent runners.

    abstract:OBJECTIVES:Post-exercise cardiac troponin T (cTnT) release has been widely reported in adult athletes but limited data is available for adolescents. The aim of this study was to determine the incidence and magnitude of cTnT appearance in a large group of adolescent runners, and to determine any association between cTnT...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/092986711796642625

    authors: Nie J,George KP,Tong TK,Gaze D,Tian Y,Lin H,Shi Q

    更新日期:2011-01-01 00:00:00

  • Receptor tyrosine kinase kit and gastrointestinal stromal tumours: an overview.

    abstract::Kit is a growth factor receptor of the type III tyrosine kinase family, whose gain-of-function mutations have been identified as driving causes of different kinds of tumours. It thus represents a viable drug target, and the development of Kit inhibitors has been shown to be a promising therapeutic concept. This review...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/092986711796150504

    authors: Sartini S,Dario B,Morelli M,Da Settimo F,La Motta C

    更新日期:2011-01-01 00:00:00

  • COVID-19 related coagulopathy: what is known up to now.

    abstract::Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) infection has been a global challenge. The complicated forms of the Coronavirus Disease 2019 (COVID-19) can evolve to multiple-organ failure, including several coagulopathies related to a sudden worsening of respiratory status. This article aimed to review s...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/0929867327666201005112231

    authors: Pena ALB,Oliveira RA,Severo RG,Simões E Silva AC

    更新日期:2020-10-05 00:00:00

  • Anti-galectin compounds as potential anti-cancer drugs.

    abstract::Galectins form a family of carbohydrate-binding proteins defined by their affinity for beta-galactosides containing glycoconjugates. The carbohydrate recognition domain (CRD) is responsible for the specificity of galectins for saccharides. This binding may result in modulated cell proliferation, cell death and cell mi...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/092986706779026219

    authors: Ingrassia L,Camby I,Lefranc F,Mathieu V,Nshimyumukiza P,Darro F,Kiss R

    更新日期:2006-01-01 00:00:00

  • Computational Approaches for the Design of Mosquito Repellent Chemicals.

    abstract:BACKGROUND:In view of many current mosquito-borne diseases there is a need for the design of novel repellents. OBJECTIVE:The objective of this article is to review the results of the researches carried out by the authors in the computer-assisted design of novel mosquito repellents. METHODS:Two methods in the computat...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/0929867325666181029165413

    authors: Basak SC,Bhattacharjee AK

    更新日期:2020-01-01 00:00:00

  • Non-antioxidant activities of vitamin E.

    abstract::Molecules in biological systems often can perform more than one function. In particular, many molecules have the ability to chemically scavenge free radicals and thus act in the test tube as antioxidant, but their main biological function is by acting as hormones, ligands for transcription factors, modulators of enzym...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/0929867043365332

    authors: Zingg JM,Azzi A

    更新日期:2004-05-01 00:00:00

  • Pharmacological implications of MMP-9 inhibition by ACE inhibitors.

    abstract::Matrix metalloproteinase-9 (MMP-9) plays an important role in the onset and prognosis of myocardial infarction. Targets of angiotensin converting enzyme (ACE) inhibitors might include not only ACE but also MMP-9, and ACE seems to be closely associated with complications of hypertension such as cardiovascular remodelin...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/092986709787846514

    authors: Yamamoto D,Takai S

    更新日期:2009-01-01 00:00:00

  • Recent Advances in Multi-target Drugs Targeting Protein Kinases and Histone Deacetylases in Cancer Therapy.

    abstract::Protein Kinase Inhibitors (PKIs) and Histone Deacetylase Inhibitors (HDACIs) are two important classes of anticancer agents and have provided a variety of small molecule drugs for the treatment of various types of human cancers. However, malignant tumors are of a multifactorial nature that can hardly be "cured" by tar...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/0929867327666200102115720

    authors: Ling Y,Liu J,Qian J,Meng C,Guo J,Gao W,Xiong B,Ling C,Zhang Y

    更新日期:2020-01-01 00:00:00

  • Torsadogenic cardiotoxicity of antipsychotic drugs: a structural feature, potentially involved in the interaction with cardiac HERG potassium channels.

    abstract::Many non-cardiovascular drugs of common clinical use cause, as an unwanted accessory property, the prolongation of the cardiac repolarisation process, due to the block of the HERG (Human Ether-a-go-go Related Gene) potassium channel, responsible for the repolarising I(Kr) current. This delayed cardiac repolarisation p...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/0929867043364351

    authors: Testai L,Bianucci AM,Massarelli I,Breschi MC,Martinotti E,Calderone V

    更新日期:2004-10-01 00:00:00

  • Transglutaminase-catalyzed reactions responsible for the pathogenesis of celiac disease and neurodegenerative diseases: from basic biochemistry to clinic.

    abstract::Transglutaminases (TGases) are enzymes which catalyze the cross linking of a glutaminyl residue of a protein/peptide substrate to a lysyl residue of a protein/peptide co-substrate with the formation of an N-gamma-(epsilon-L-glutamyl)-L-lysine [GGEL] cross link (isopeptidic bond) and the concomitant release of ammonia....

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/092986706777585068

    authors: Martin A,Romito G,Pepe I,De Vivo G,Merola MR,Limatola A,Gentile V

    更新日期:2006-01-01 00:00:00

  • Dietary Polyphenols and Mitochondrial Function: Role in Health and Disease.

    abstract::Mitochondria are cytoplasmic double-membraned organelles that are involved in a myriad of key cellular regulatory processes. The loss of mitochondrial function is related to the pathogenesis of several human diseases. Over the last decades, an increasing number of studies have shown that dietary polyphenols can regula...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/0929867324666170529101810

    authors: Teixeira J,Chavarria D,Borges F,Wojtczak L,Wieckowski MR,Karkucinska-Wieckowska A,Oliveira PJ

    更新日期:2019-01-01 00:00:00

  • Curcumin: a dietary phytochemical for targeting the phenotype and function of dendritic cells.

    abstract::Dendritic cells (DCs) are the most powerful antigen-presenting cells which link the innate and adaptive immune responses. Depending on the context DCs initiate the immune responses or contribute to immune tolerance. Any disturbance in their phenotypes and functions may initiate inflammatory or autoimmune diseases. Hen...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/0929867327666200515101228

    authors: Rahimi K,Hassanzadeh K,Khanbabaei H,Haftcheshmeh SM,Ahmadi A,Izadpanah E,Mohammadi A,Sahebkar A

    更新日期:2020-05-14 00:00:00

  • Comparison of Clinical Outcomes Between Genders Following Antihypertensive Therapy: A Meta-Analysis.

    abstract:BACKGROUND:Numerous studies have reported sex and gender differences in the prevalence and treatment of cardiovascular diseases. However, sex differences in the therapy of hypertension have not been completely examined. OBJECTIVE:To estimate the gender-specific dissimilarity in outcomes among patients following antihy...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,meta分析

    doi:10.2174/0929867323666161213160440

    authors: Giorgini P,Sahebkar A,Stamerra CA,Raparelli V,Petrarca M,Grassi D,Ferri C,Di Giosia P

    更新日期:2017-01-01 00:00:00

  • NGS of microRNAs involved in cardioprotection induced by sevoflurane compared to propofol in myocardial revascularization surgery: The ACDHUVV-16 Clinical Trial.

    abstract:BACKGROUND:Numerous studies have demonstrated that halogenated agents elicit myocardial conditioning effects when adminis-tered perioperatively in cardiac surgery. Recent evidence has been published of the benefits of maintaining exposure to halogenated agents during the early postoperative period. The enzymatic mechan...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/0929867327999201001202607

    authors: Guerrero Orriach JL,Escalona Belmonte JJ,Ramirez Aliaga M,Ramirez Fernandez A,Rodriguez Capitan MJ,Quesada Muñoz G,Raigón Ponferrada A,Alcaide Torres J,Santiago-Fernandez C,Matute Gonzalez E,Rubio Navarro M,Bautista R,Gómez Maldo

    更新日期:2020-10-01 00:00:00

  • Metal-based antimicrobial protease inhibitors.

    abstract::Limitations associated with the production cost, metabolic instability, side-effects, resistance and poor pharmacokinetics of organic protease inhibitors (PIs), which form an essential component of the front line HAART treatment for HIV, have fuelled efforts into finding novel, transition metal-based alternatives. Som...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/0929867311320250008

    authors: Kellett A,Prisecaru A,Slator C,Molphy Z,McCann M

    更新日期:2013-01-01 00:00:00

  • A possible target of antioxidative therapy for diabetic vascular complications-vascular NAD(P)H oxidase.

    abstract::A growing body of evidence has shown that oxidative stress may be involved in the development of vascular complications associated with diabetes. However, the molecular mechanism for increased reactive oxygen species (ROS) production in diabetes remains uncertain. Among various possible mechanisms, attention have incr...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/0929867033457133

    authors: Inoguchi T,Tsubouchi H,Etoh T,Kakimoto M,Sonta T,Utsumi H,Sumimoto H,Yu HY,Sonoda N,Inuo M,Sato N,Sekiguchi N,Kobayashi K,Nawata H

    更新日期:2003-09-01 00:00:00

  • Progress in COX-2 inhibitors: a journey so far.

    abstract::The non-steroidal anti-inflammatory drugs (NSAIDs) are diverse group of compounds used for the treatment of inflammation, since the introduction of acetylsalicylic acid in 1899. Traditional (first generation) NSAIDs exert antiinflammatory, analgesic, and antipyretic effects through the blockade of prostaglandin synthe...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/092986710790979980

    authors: Chakraborti AK,Garg SK,Kumar R,Motiwala HF,Jadhavar PS

    更新日期:2010-01-01 00:00:00