SRC family kinases as potential therapeutic targets for malignancies and immunological disorders.

Abstract:

:The Src family consists of eight non-receptor protein tyrosine kinases characterised by a common structure. Based on their amino acid sequence, Src family kinases are grouped into two subfamilies, which are also characterised by different tissue specificity. Src kinases are involved in signal transduction pathways triggered by a wide variety of surface receptors, including receptor tyrosine kinases, integrins, G-protein-coupled receptors and antigen receptors. Several pieces of evidence implicate Src family kinases in cancer development, as a consequence of changes in protein expression and/or kinase activity, and have prompted the design of potent specific inhibitors, the most common of which are adenine mimetics, as tools of relevant clinical interest for the treatment of both solid tumours and leukaemias. In addition, the finding that some Src kinases expressed in haematopoietic cells play pivotal roles in lymphocyte maturation and activation has fostered the development of safe and effective inhibitors selective for specific Src family members, which are currently being tested in clinical trials as immunosuppressants for the treatment of immunological disorders. Here we shall review the recent literature on the involvement of Src family kinases in human neoplasias and immunological disorders and the goals reached in the search for selective pharmacological inhibitors.

journal_name

Curr Med Chem

authors

Benati D,Baldari CT

doi

10.2174/092986708784310404

subject

Has Abstract

pub_date

2008-01-01 00:00:00

pages

1154-65

issue

12

eissn

0929-8673

issn

1875-533X

journal_volume

15

pub_type

杂志文章,评审
  • NAChR α4β2 Subtype and their Relation with Nicotine Addiction, Cognition, Depression and Hyperactivity Disorder.

    abstract:BACKGROUND:Neuronal α4β2 nAChRs are receptors involved in the role of neurotransmitters regulation and release, and this ionic channel participates in biological process of memory, learning and attention. This work aims to review the structure and functioning of the α4β2 nAChR emphasizing its role in the treatment of a...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/0929867325666180410105135

    authors: Laikowski MM,Reisdorfer F,Moura S

    更新日期:2019-01-01 00:00:00

  • Design and Synthesis of Dopaminergic Agonists.

    abstract::The use of dopaminergic agonists is key in the treatment of Parkinson's disease and related central nervous system (CNS) neurodegenerative disorders. Despite there are a number of commercialized dopaminergic agonists that are currently being used successfully in the first stages of the disease, they often fail to prov...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/0929867323666160504103621

    authors: Matute MS,Matute R,Merino P

    更新日期:2016-01-01 00:00:00

  • Clinical impact of the detection of BRAF mutations in thyroid pathology: potential usefulness as diagnostic, prognostic and theragnostic applications.

    abstract::A BRAF somatic mutation at residue 600 of the BRAF protein (BRAFV600E) is highly prevalent in papillary thyroid carcinomas (PTC). This mutation occurs in approximately 44% (from 29% to 83%) of PTC depending on the different studies. BRAFV600E is almost always found in PTC with a papillary or a mixed follicular/papilla...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/092986710791111189

    authors: Lassalle S,Hofman V,Ilie M,Butori C,Bozec A,Santini J,Vielh P,Hofman P

    更新日期:2010-01-01 00:00:00

  • Role of apoptosis and apoptosis-related genes in cellular response and antitumor efficacy of anthracyclines.

    abstract::Cellular resistance to anthracyclines is a major limitation of their clinical use in the treatment of human tumors. Resistance to doxorubicin is described as a multifactorial phenomenon involving the overexpression of defense factors and alterations in drug-target interactions. Such changes do not account for all mani...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/0929867013373994

    authors: Perego P,Corna E,De Cesare M,Gatti L,Polizzi D,Pratesi G,Supino R,Zunino F

    更新日期:2001-01-01 00:00:00

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

    abstract::The new drug class of dipeptidyl peptidase-4 (DPP4) inhibitors has been widely accepted in the daily management of type 2 diabetes since its strategic advantages with regard to body weight, risk of hypoglycaemia, and beta cell survival. We have previously evaluated the theoretical implications of DPP4 inhibition given...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/092986711797535290

    authors: Matteucci E,Giampietro O

    更新日期:2011-01-01 00:00:00

  • The renaissance of polymyxins.

    abstract::Polymyxins are polypeptide antibiotics, with a primary effect of membrane damaging due to their selective binding to the lipopolysaccharide of Gram-negative bacteria. Their nephro- and neurotoxic side effects limited their use, however, in the last decade the emergence of multidrug-resistant Gram-negative bacteria led...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/09298673113209990185

    authors: Kadar B,Kocsis B,Nagy K,Szabo D

    更新日期:2013-01-01 00:00:00

  • Steroid receptor ligands for breast cancer targeting: an insight into their potential role as PET imaging agents.

    abstract::The design and development of radiolabelled steroid derivatives has been an important area of research due to their wellknown value in breast cancer targeting. The estrogen receptor (ER) and progesterone receptor (PR) are important biomarkers in the diagnosis, prognosis and follow-up of the therapeutic response of bre...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/092986713804806658

    authors: Oliveira MC,Neto C,Ribeiro Morais G,Thiemann T

    更新日期:2013-01-01 00:00:00

  • The efficacy of viral capsid inhibitors in human enterovirus infection and associated diseases.

    abstract::Enteroviruses are members of picornavirus family which causes diverse and severe diseases in humans and animals. Clinical manifestations of enterovirus infections include fever, hand, foot, and mouth disease, and herpangina. Enteroviruses also cause potentially severe and life-threatening infections such as meningitis...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/092986707780363032

    authors: Li C,Wang H,Shih SR,Chen TC,Li ML

    更新日期:2007-01-01 00:00:00

  • Interactions between calcium and cAMP signaling.

    abstract::The calcium ion is quite possibly the single most pervasive signaling molecule used by living organisms for the purpose of communicating internal and external states. It differs from other messengers in that it is neither created nor destroyed, but just moved around inside and outside the cell via transporters, pumps ...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/092986712804143286

    authors: Hofer AM

    更新日期:2012-01-01 00:00:00

  • Biopharmaceutics, pharmacokinetics and pharmacodynamics of antituberculosis drugs.

    abstract::Tuberculosis (TB) is the leading cause of mortality due to a single infectious agent. The currently used combination drug regimens produce cure rates that exceed 95%, given good patient adherence during the multiple months treatment period. However the recent surge in HIV infections and the synergy between HIV and TB ...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/092986708783955509

    authors: Budha NR,Lee RE,Meibohm B

    更新日期:2008-01-01 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

  • Effects and mechanism of organ protection by cardiotrophin-1.

    abstract::Cardiotrophin-1 (CT-1), a member of the interleukin (IL)-6 family, is reported to exhibit a plethora of pleiotropic effects in the heart such as cytoprotective, pro-proliferative and pro-fibrotic ones. An extensive research has been devoted on proliferative and profibrotic effects of CT-1 on the heart. Thus the presen...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/092986713804806702

    authors: García-Cenador MB,Lopez-Novoa JM,Díez J,García-Criado FJ

    更新日期:2013-01-01 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

  • DNA Damage Response as a Pharmacological Target for Cancer and Infectious Diseases.

    abstract:: ...

    journal_title:Current medicinal chemistry

    pub_type: 社论

    doi:10.2174/092986732608190516092613

    authors: Poplawski T

    更新日期:2019-01-01 00:00:00

  • Reprogramming cancer cells in endocrine-related tumors: open issues.

    abstract::Reprogramming technologies have been developed to revert somatic differentiated cells into pluripotent stem cells that can be differentiated into different lineages potentially useful in stem cell therapy. Reprogramming methods have been progressively refined to increase their efficiency, to obtain a cell population s...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/0929867321666131129125624

    authors: Tafani M,Perrone GA,Pucci B,Russo A,Bizzarri M,Mechanick JI,Carpi A,Russo MA

    更新日期:2014-01-01 00:00:00

  • Targeting airway inflammation: novel therapies for the treatment of asthma.

    abstract::It is now widely accepted that airway inflammation is the key factor underlying the pathogenesis of asthma. Inhaled corticosteroids remain the most important anti-inflammatory treatment for asthma. However, they are rather non-specific in their actions and their use raises concerns over side effects and compliance iss...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/092986706778521779

    authors: Walsh GM

    更新日期:2006-01-01 00:00:00

  • mTOR inhibitors (rapamycin and its derivatives) and nitrogen containing bisphosphonates: bi-functional compounds for the treatment of bone tumours.

    abstract::N-BP, rapamycin and its derivatives have been originally developed respectively as anti-resorptive and anti-fungal agents. In fact, in vitro and in vivo experiments demonstrated that these compounds are multi-functional molecules exerting their effects on tumour cell growth and bone remodelling. The major challenge in...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/092986707780831159

    authors: Ory B,Moriceau G,Redini F,Heymann D

    更新日期:2007-01-01 00:00:00

  • Xanthones as potential antioxidants.

    abstract::Xanthones (dibenzo-γ-pyrones) constitutes an important class of oxygenated heterocycles and occur as secondary metabolites in plants and microorganisms. They are known for various biological activities such as antioxidant, monoamine oxidase inhibitor, antihypertensive, hepatoprotective, antithrombotic, antifungal and ...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/09298673113209990144

    authors: Panda SS,Chand M,Sakhuja R,Jain SC

    更新日期:2013-01-01 00:00:00

  • Drug excipients.

    abstract::The therapeutical use of drugs involves the application of dosage forms, serving as carrier systems together with several excipients to deliver the active ingredient to the site of action. Drug delivery technology combines an understanding of medicinal chemistry and pharmacology with the skill of formulation, aiming t...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/092986706778201648

    authors: Kalász H,Antal I

    更新日期:2006-01-01 00:00:00

  • Resveratrol and ischemic preconditioning in the brain.

    abstract::Cardiovascular pathologies in the French are not prevalent despite high dietary saturated fat consumption. This is commonly referred to as the "French Paradox" attributing its anti-lipidemic effects to moderate consumption of red wine. Resveratrol, a phytoalexin found in red wine, is currently the focus of intense res...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/092986708784638861

    authors: Raval AP,Lin HW,Dave KR,Defazio RA,Della Morte D,Kim EJ,Perez-Pinzon MA

    更新日期:2008-01-01 00:00:00

  • Potential Relevance of Melatonin Against Some Infectious Agents: A Review and Assessment of Recent Research.

    abstract::Melatonin, a tryptophan-derived neurohormone found in animals, plants, and microbes, participates in various biological and physiological functions. Among other properties, numerous in vitro or in vivo studies have reported its therapeutic potential against many parasites, bacteria and viruses. In this concern, melato...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/0929867322666150827093730

    authors: Elmahallawy EK,Luque JO,Aloweidi AS,Gutiérrez-Fernández J,Sampedro-Martínez A,Rodriguez-Granger J,Kaki A,Agil A

    更新日期:2015-01-01 00:00:00

  • Endothelial Progenitor Cells as Mediators of the Crosstalk between Vascular Repair and Immunity: Lessons from Systemic Autoimmune Diseases.

    abstract::From the discovery of Endothelial Progenitor Cells (EPC), these bone marrowderived precursors have been placed as crucial mediators of the endothelial repair. Accordingly, altered levels and function of EPC have been found in different scenarios of CV risk. Despite the fact that EPC exhibit important characteristics w...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/0929867324666170428110311

    authors: Rodríguez-Carrio J,López P,Suárez A

    更新日期:2018-01-01 00:00:00

  • Receptor-operated regulation of ATP-sensitive K+ channels via membrane phospholipid metabolism.

    abstract::ATP-sensitive K(+) channels (K(ATP)channels) regulate insulin secretion by coupling intracellular metabolic changes to excitability of the plasma membrane in pancreatic beta-cells. The channels are closed when extracellular glucose levels are elevated due to enhanced feature. By contrast, cardiac-type K(ATP) channels,...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/0929867033368475

    authors: Kakei M

    更新日期:2003-02-01 00:00:00

  • High Resolution Nuclear Magnetic Resonance Spectroscopy on Biological Tissue and Metabolomics.

    abstract::High-resolution nuclear magnetic resonance (NMR) spectroscopy is a universal analytical tool. It can provide detailed information on chemical shifts, J coupling constants, multiplet patterns, and relative peak areas. It plays an important role in the fields of chemistry, biology, medicine, and pharmacy. A highly homog...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/0929867326666190312130155

    authors: Lin Y,Zeng Q,Lin L,Chen Z

    更新日期:2019-01-01 00:00:00

  • Is There A Role For Lifestyle Interventions In Obsessive-Compulsive And Related Disorders?

    abstract::Many of the currently available treatments for obsessive-compulsive and related disorders (OCRDs) such as pharmacotherapy augmentation strategies, partial hospitalization programs, deep brain stimulation, and neurosurgery are efficacious for individuals suffering from more severe forms of these conditions. Unfortunate...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/0929867325666180104150854

    authors: Fontenelle LF,Zeni-Graiff M,Quintas JN,Yücel M

    更新日期:2018-01-01 00:00:00

  • Structure Properties and Mechanisms of Action of Naturally Originated Phenolic Acids and Their Derivatives against Human Viral Infections.

    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

    pub_type: 杂志文章,评审

    doi:10.2174/0929867324666170815102917

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

    更新日期:2017-01-01 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

  • Antisense oligonucleotides: the state of the art.

    abstract::The use of antisense oligonucleotides as therapeutic agents has generated considerable enthusiasm in the research and medical community. Antisense oligonucleotides as therapeutic agents were proposed as far back as in the 1970s when the antisense strategy was initially developed. Nonetheless, it has taken almost a qua...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/0929867054864859

    authors: Aboul-Fadl T

    更新日期:2005-01-01 00:00:00

  • Intramolecular cyclisation of β-aryl-β-amino acids in the design of novel heterocyclic systems with therapeutic interest: an unfailing source of diversity.

    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

    pub_type: 杂志文章,评审

    doi:10.2174/092986710793361261

    authors: Rochais C,Rault S,Dallemagne P

    更新日期:2010-01-01 00:00:00

  • The role of antiangiogenetic agents in the treatment of breast cancer.

    abstract::Angiogenesis is known to be essential for the development and progression of cancer. Vascular endothelial growth factor (VEGF) is a critical mediator in tumor angiogenesis for many solid malignancies, including breast cancer. Increased levels of VEGF have been associated with poor clinical outcomes, including reduced ...

    journal_title:Current medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/092986711797636072

    authors: Bareschino MA,Schettino C,Colantuoni G,Rossi E,Rossi A,Maione P,Ciardiello F,Gridelli C

    更新日期:2011-01-01 00:00:00