Supramolecular devices to improve the treatment of brain diseases.


:The blood-brain barrier (BBB) hinders the accumulation of active compounds in the central nervous system, thus decreasing their therapeutic effectiveness. To overcome this obstacle, interesting supramolecular nanodevices are herein considered. These systems have many advantages over the conventional formulations, such as having structures made up of biocompatible and biodegradable materials, the possibility of bypassing the BBB in a non-invasive manner (without structural modifications) and the possibility of being structurally modified to modulate the biopharmaceutical properties of the encapsulated compounds. Polymolecular (liposomes, niosomes, nanogels) and oligomolecular (cyclodextrins) devices have potential clinical applications in brain drug delivery, being capable of active targeting that can concentrate bioactives in the brain.


Drug Discov Today


Drug discovery today


Paolino D,Cosco D,Molinaro R,Celia C,Fresta M




Has Abstract


2011-04-01 00:00:00














  • Assessment of significant benefit for orphan medicinal products by European regulators may support subsequent relative effectiveness assessments by health technology assessment organizations.

    abstract::To maintain orphan drug status at the time of market authorization, orphan medicinal products (OMPs) need to be assessed for all criteria, including significant benefit, by the Committee for Orphan Medicinal Products (COMP) of the European Medicines Agency (EMA). Subsequently, health technology assessment (HTA) organi...

    journal_title:Drug discovery today

    pub_type: 杂志文章


    authors: Vreman RA,de Ruijter AS,Zawada A,Tafuri G,Stoyanova-Beninska V,O'Connor D,Naumann-Winter F,Wolter F,Mantel-Teeuwisse AK,Leufkens HGM,Sidiropoulos I,Larsson K,Goettsch WG

    更新日期:2020-07-01 00:00:00

  • Current status and future prospects of toxicogenomics in drug discovery.

    abstract::In drug discovery and development (DDD), the efficacy, safety and cost of new chemical entities are the main concerns of the pharmaceutical industry. Continuously updated and stricter recommendations imposed by regulatory authorities result in greater challenges being faced by the industry. Reliable high-throughput te...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审


    authors: Khan SR,Baghdasarian A,Fahlman RP,Michail K,Siraki AG

    更新日期:2014-05-01 00:00:00

  • Drug discovery: are productivity metrics inhibiting motivation and creativity?

    abstract::With a productivity gap in pharmaceutical research and development, and increased industrialization in both areas, an increased need for precise indicators of productivity has emerged. Measuring scientists' performance can impact the way the tasks are performed and the level of motivation of an individual. This is a c...

    journal_title:Drug discovery today

    pub_type: 杂志文章


    authors: Ullman F,Boutellier R

    更新日期:2008-11-01 00:00:00

  • Homologous recombination in human iPS and ES cells for use in gene correction therapy.

    abstract::The emergence of induced pluripotent stem (iPS) cell technology has shifted gene correction therapy toward reality. Crucial issues are ensuring the safety of using iPS cell technology in patients and discovering how best to transfer genetically manipulated iPS cells back into patients. One key issue that has hindered ...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审


    authors: Nakayama M

    更新日期:2010-03-01 00:00:00

  • Improved mouse models and advanced genetic and genomic technologies for the study of neutrophils.

    abstract::Mice have been excellent surrogates for studying neutrophil biology and, furthermore, murine models of human disease have provided fundamental insights into the roles of human neutrophils in innate immunity. The emergence of novel humanized mice and high-diversity mouse populations offers the research community innova...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审


    authors: Hosur V,Skelly DA,Francis C,Low BE,Kohar V,Burzenski LM,Amiji MM,Shultz LD,Wiles MV

    更新日期:2020-06-01 00:00:00

  • The multiple therapeutic applications of miRNAs for bone regenerative medicine.

    abstract::With the aging of the general population, there is an increasing need for bone defect repair, prompting the development of reliable alternatives to autologous bone grafting, without the usually associated major drawbacks (i.e., limited volume and severe postoperative pain). Given the crucial role that miRNAs appear to...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审


    authors: Scimeca JC,Verron E

    更新日期:2017-07-01 00:00:00

  • Epigenetic opportunities and challenges in cancer.

    abstract::Epigenetic covalent modifications of DNA and chromatin proteins strongly affect gene expression and cellular activity, and epigenetic misregulation occurs in several diseases, especially cancer. First-generation drugs targeting the relatively promiscuous DNA methylation and histone acetylation modifiers have had succe...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审


    authors: Best JD,Carey N

    更新日期:2010-01-01 00:00:00

  • Psoriasis: pathological mechanisms, current pharmacological therapies, and emerging drug delivery systems.

    abstract::Psoriasis is a chronic autoimmune skin disorder triggered by either genetic factors, environmental factors, life style, or a combination thereof. Clinical investigations have identified pathogenesis, such as T cell and cytokine-mediated, genetic disposition, antimicrobial peptides, lipocalin-2, galectin-3, vaspin, fra...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审


    authors: Rapalli VK,Waghule T,Gorantla S,Dubey SK,Saha RN,Singhvi G

    更新日期:2020-12-01 00:00:00

  • Pancreatic lipase inhibitors from natural sources: unexplored potential.

    abstract::The prevalence of obesity is increasing at an alarming rate, but, unfortunately, only a few medications are currently on the market. Obesity is primarily regarded as a disorder of lipid metabolism and the enzymes involved in this process could be selectively targeted to develop antiobesity drugs. Recently, newer appro...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审


    authors: Birari RB,Bhutani KK

    更新日期:2007-10-01 00:00:00

  • Current and future trends in the application of HPLC-MS to metabolite-identification studies.

    abstract::Metabolic determinations are an integral part of every drug-discovery and drug-development program. Recent emphasis has been to increase sample throughput while, at the same time, increase information content within assays. To this end, screening for potential drug-drug interactions, overall metabolic stability and me...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审


    authors: Castro-Perez JM

    更新日期:2007-03-01 00:00:00

  • Stem cells and cell lines from the human auditory organ: applications, hurdles and bottlenecks in the development of regenerative therapies for deafness.

    abstract::The development of any stem-cell-based therapy (and a potential one for deafness is no exception) relies on the generation of the necessary tools: 'cell drugs' that can be safely manufactured for their clinical application. An increasing body of work has focussed on the identification, in animal models, of potential s...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审


    authors: Rivolta MN

    更新日期:2010-04-01 00:00:00

  • Src and podoplanin forge a path to destruction.

    abstract::Cancer and arthritis present an enormous challenge to society. They share pathogenic pathways that involve extracellular matrix degradation, tissue invasion, and inflammation. Most cancer and arthritis treatments affect normal cell function to cause significant adverse effects in patients. Specific pathways that promo...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审


    authors: Krishnan H,Miller WT,Blanco FJ,Goldberg GS

    更新日期:2019-01-01 00:00:00

  • New ways to treat bacterial infections.

    abstract::There is an urgent need for fresh approaches to the treatment of bacterial infections because of the changing patterns of infectious disease and the emergence of bacterial strains resistant to current antibiotics. Modification of the cell phenotype to sensitize bacteria to components of the hosts' immune system or to ...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审


    authors: Taylor PW,Stapleton PD,Paul Luzio J

    更新日期:2002-11-01 00:00:00

  • Importance of target-mediated drug disposition for small molecules.

    abstract::Target concentration is typically not considered in drug discovery. However, if targets are expressed at relatively high concentrations and compounds have high affinity, such that most of the drug is bound to its target, in vitro screens can give unreliable information on compound affinity. In vivo, a similar situatio...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审


    authors: Smith DA,van Waterschoot RAB,Parrott NJ,Olivares-Morales A,Lavé T,Rowland M

    更新日期:2018-12-01 00:00:00

  • Deformylase as a novel antibacterial target.

    abstract::Bacterial genomics has revealed a plethora of previously unknown targets of potential use in the discovery of novel antibacterial drugs. However, so far little has emerged from this approach. Peptide deformylase is an interesting target that was discovered more than 30 years ago, but was not exploited until recently. ...

    journal_title:Drug discovery today

    pub_type: 杂志文章


    authors: Yuan Z,Trias J,White RJ

    更新日期:2001-09-15 00:00:00

  • Tuberculosis: from molecular pathogenesis to effective drug carrier design.

    abstract::In the past two decades, tuberculosis has gone from being a forgotten disease to a modern and recrudescent pathology. Tuberculosis is a curable infection and most of the negative therapeutic outcomes are related to poor patient compliance, which could be solved by new drug delivery approaches. By using such approaches...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审


    authors: Dube D,Agrawal GP,Vyas SP

    更新日期:2012-07-01 00:00:00

  • Advanced nanovehicles for cancer management.

    abstract::Over the past decade, together with the improvement of traditional cancer treatments, conveniently designed (with respect to their size, shape, main material, and coating) and specifically targeted nanovehicles have been developed. Nano-sized carriers can be functionalized to recognize key structures expressed in canc...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审


    authors: Saenz del Burgo L,Pedraz JL,Orive G

    更新日期:2014-10-01 00:00:00

  • Monitor: molecules and profiles.

    abstract::Monitor provides an insight into the latest developments in drug discovery through brief synopses of recent presentations and publications together with expert commentaries on the latest technologies. There are two sections: Molecules summarizes the chemistry and the pharmacological significance and biological relevan...

    journal_title:Drug discovery today

    pub_type: 杂志文章


    authors: Lloyd AW

    更新日期:2000-08-01 00:00:00

  • Modulating TNF-alpha signaling with natural products.

    abstract::Natural products have been, and continue to be, a major source of pharmacologically active substances from which drugs can be developed. Currently, tumor necrosis factor-alpha (TNF-alpha) inhibitors from natural origins are being advanced for the treatment of inflammatory disorders. Elevated TNF-alpha synthesis has be...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审


    authors: Paul AT,Gohil VM,Bhutani KK

    更新日期:2006-08-01 00:00:00

  • Updating molecular properties during early drug discovery.

    abstract::Current multiparameter optimization (MPO) strategies make use of few experimental physicochemical descriptors (i.e., solubility at physiological pH and lipophilicity in the octanol/water system). Here, we show how new trends in drug discovery (i.e., large and flexible molecules for 'difficult' targets) call for the in...

    journal_title:Drug discovery today

    pub_type: 杂志文章


    authors: Caron G,Ermondi G

    更新日期:2017-06-01 00:00:00

  • Discovery informatics: its evolving role in drug discovery.

    abstract::Drug discovery and development is a highly complex process requiring the generation of very large amounts of data and information. Currently this is a largely unmet informatics challenge. The current approaches to building information and knowledge from large amounts of data has been addressed in cases where the types...

    journal_title:Drug discovery today

    pub_type: 杂志文章


    authors: Claus BL,Underwood DJ

    更新日期:2002-09-15 00:00:00

  • Hybrid poly(lactic-co-glycolic acid) nanoparticles: design and delivery prospectives.

    abstract::Poly(lactic-co-glycolic acid) (PLGA), a US Food and Drug Administration (FDA)-approved copolymer, has been exploited widely in the design of nanoparticles because it is biodegradable, biocompatible, protects the drug molecules from degradation, and aids in producing sustained and targeted delivery. However, certain co...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审


    authors: Pandita D,Kumar S,Lather V

    更新日期:2015-01-01 00:00:00

  • Polymer-drug conjugates: recent advances and future perspectives.

    abstract::Polymer-drug conjugates (PDC) have exhibited clinical and commercial success in the field of drug delivery. A polymeric backbone, linker, targeting moiety, and drug constitute the building blocks of PDCs. Current attention is focusing on natural polymeric carriers, in particular the concept of graft copolymers, such a...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审


    authors: Thakor P,Bhavana V,Sharma R,Srivastava S,Singh SB,Mehra NK

    更新日期:2020-09-01 00:00:00

  • Nano-engineered delivery systems for cancer imaging and therapy: Recent advances, future direction and patent evaluation.

    abstract::Cancer is the second highest cause of death worldwide. Several therapeutic approaches, such as conventional chemotherapy, antibodies and small molecule inhibitors and nanotherapeutics have been employed in battling cancer. Amongst them, nanotheranostics is an example of successful personalized medicine bearing dual ro...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审


    authors: Nabil G,Bhise K,Sau S,Atef M,El-Banna HA,Iyer AK

    更新日期:2019-02-01 00:00:00

  • Docking optimization, variance and promiscuity for large-scale drug-like chemical space using high performance computing architectures.

    abstract::There is a continuing need to hasten and improve protein-ligand docking to facilitate the next generation of drug discovery. As the drug-like chemical space reaches into the billions of molecules, increasingly powerful computer systems are required to probe, as well as tackle, the software engineering challenges neede...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审


    authors: Trager RE,Giblock P,Soltani S,Upadhyay AA,Rekapalli B,Peterson YK

    更新日期:2016-10-01 00:00:00

  • How do we measure pathology in PAH (lung and RV) and what does it tell us about the disease.

    abstract::The current understanding of the pathology that underlies pulmonary vascular and right ventricular remodeling in pulmonary hypertension is discussed. Although recent studies underscored the importance of intima and media remodeling and, for the first time, the relevance of perivascular inflammation, much is needed to ...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审


    authors: Tuder RM

    更新日期:2014-08-01 00:00:00

  • Extending kinome coverage by analysis of kinase inhibitor broad profiling data.

    abstract::The explored kinome was extended with broad profiling using the DiscoveRx and Millipore assay panels. The analysis of the profiling of 3368 selected inhibitors on 456 kinases in the DiscoveRx format delivered several insights. First, the coverage depended on the threshold of the selectivity parameter. Second, the rela...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审


    authors: Jacoby E,Tresadern G,Bembenek S,Wroblowski B,Buyck C,Neefs JM,Rassokhin D,Poncelet A,Hunt J,van Vlijmen H

    更新日期:2015-06-01 00:00:00

  • Nuclear transport as a target for cell growth.

    abstract::The function of many key proteins and transcription factors involved in cell growth can be regulated by their cellular localization. Such proteins include the tumor suppressor p53 and the nuclear factor kappaB. Although the idea of trapping such proteins in either the nucleus or cytoplasm has been introduced as a pote...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审


    authors: Kau TR,Silver PA

    更新日期:2003-01-15 00:00:00

  • Graphene-based nanomaterials for drug and/or gene delivery, bioimaging, and tissue engineering.

    abstract::Here, we discuss the biomedical applications of graphene-based nanomaterials (GBNs). We examine graphene and its various derivatives, including graphene, graphene oxides (GOs), reduced graphene oxides (rGOs), graphene quantum dots (GQDs), and graphene composites, and discuss their unique properties related to their bi...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审


    authors: Zhao H,Ding R,Zhao X,Li Y,Qu L,Pei H,Yildirimer L,Wu Z,Zhang W

    更新日期:2017-09-01 00:00:00

  • Enabled clinical use of an HIV-1 attachment inhibitor through drug delivery.

    abstract::The clinical advancement of HIV-1 attachment inhibitors was hindered initially by poor bioavailability. Attempts to identify improved candidates revealed that solubility and dissolution-rate-limited absorption are barriers to achieving adequate antiviral plasma levels. This was mitigated by forming nanosized drugs or ...

    journal_title:Drug discovery today

    pub_type: 杂志文章


    authors: Timmins P,Brown J,Meanwell NA,Hanna GJ,Zhu L,Kadow JF

    更新日期:2014-09-01 00:00:00