Showing papers in "Drug Discovery Today in 2007"

TL;DR: In this review, it is intended to discuss the recent advances related on the area of solid dispersions.

TL;DR: Brain drug development programs of the future need to be re-configured so that drugs are formulated to enable transport into the brain via endogenous BBB transporters.

TL;DR: The biological rationale for combination therapeutics is discussed, some existing combination drugs are reviewed, and a systematic approach to identify interactions between molecular pathways that could be leveraged for therapeutic benefit is presented.

TL;DR: Various extracts and secondary metabolites from plants and microbial origin with PL inhibitory activity that can be focused for drug development programs are reviewed.

TL;DR: New developments suggest that it is feasible to acquire PTP1B-based, small-molecule therapeutics with the requisite potency and selectivity and that future efforts will probably transform the potent and selective P TP1B inhibitors into orally available drugs with desirable physicochemical properties and in vivo efficacies.

TL;DR: These findings demonstrate the importance of growth control in the pathology of major diseases and overall human health, and underscore the therapeutic potential of the mTOR pathway.

TL;DR: It is found that there is often little overlap in the similarity relationships detected by different approaches, which rationalizes the need to develop alternative similarity methods.

TL;DR: Although recent radioprotective agents have lower efficacy, they have lower toxicity, more favourable administration routes and improved pharmacokinetics compared to the older thiol compounds.

TL;DR: In animal models, HIF-1 overexpression is associated with increased tumor growth, vascularization, and metastasis, whereas Hif-1 loss-of-function has the opposite effect, thus validating HIF -1 as a target.

TL;DR: Assays for mitochondrial function, cell models that better report mitochondrial impairment, and new animal models that more faithfully reflect clinical manifestations of mitochondrial dysfunction are discussed in the context of how such data can reduce late stage attrition of drug candidates and can yield safer drugs in the future.

TL;DR: Evidence now suggests that miRNAs represent a new species of regulator, controlling the levels of potentially large numbers of proteins, many of which might be important drug targets.

TL;DR: Objectively validating the improved applicability and performance of QM over classical-based models in DD will be the focus of research in the coming years along with research on the conformational sampling problem as it relates to protein-ligand complexes.

TL;DR: An overview of the investigations on the feasibility and application of terpenes as sorption promoters for improved delivery of drugs through skin is presented.

TL;DR: Mechanistic studies with currently available SARMs will help to define the contributions of differential tissue distribution, tissue-specific expression of 5alpha-reductase, ligand-specific regulation of gene expression and AR interactions with tissue- specific coactivators to their observed tissue selectivity, and lead to even greater expansion of selective anabolic therapies.

TL;DR: This review describes recent developments of hollow and porous inorganic nanomaterials in nanomedicine, especially for drug/gene delivery and potential safety concerns about the use of inorganic nanoparticles and nanotubes in biomedical applications could be alleviated with proper surface treatment.

TL;DR: A fragment-based approach to multi-target drug discovery could lead to a new generation of compounds with improved physicochemical and pharmacokinetic properties.

TL;DR: 11beta-HSD1 inhibition is an emerging pleiotropic therapeutic target and resists cognitive decline with ageing, and this is seen in humans with a prototypic inhibitor.

TL;DR: In this review, what is known and what is not known about the interactions between therapeutic antibodies and the immune system are discussed, with the goal being progress toward clear target profiles for effector engineering efforts.

TL;DR: Evidence supporting a key role for SREBPs in NAFLD is presented and it is suggested that further studies are urgently needed to evaluate modulation of SREBP activity as a potential new treatment forNAFLD.

TL;DR: Their mode of action, involving interaction with fungus-specific sphingolipids, and heterologous expression, required for cost-effective production, are major assets for development of plant and insect defensins as antifungal leads.

TL;DR: Gleevec is a notable example from a new class of allosteric inhibitors that alter protein kinase conformation to block productive ATP binding, promising exciting therapeutic opportunities by exploiting new mechanisms of action and may allow greater specificity in protein kinases inhibition with fewer off-target side effects.

TL;DR: Computational contributions to epitope mapping and reverse vaccinology are discussed, two techniques central to the new discipline of immunomics, and methods to improve the efficiency of vaccination are discussed.

TL;DR: A brief summary and an assessment of most of the approaches to computational systems biology, including systems of differential equations, Petri nets, cellular automata simulators, agent-based models and pi calculus are provided.

TL;DR: The emerging in vitro approaches for assessing taste characteristics of taste masked drug and drug products will result in a decreased reliance on human panel tests, as discussed here.

TL;DR: Preclinical and clinical data indicate that rapamycin is a promising drug for age-related diseases and seems to have anti-tumor, bone-sparing and calorie-restriction-mimicking 'side-effects'.

TL;DR: It is proposed that drug-herb and herb-CYP interaction studies should be incorporated into drug development and used to identify drug interactions with herbs.

TL;DR: This work has shown that binding is not driven by the favourable entropic loss of solvent water from the binding pocket, but rather by favourable dispersion interactions arising from suboptimal hydration of the protein-binding pocket, and can anticipate particularly dramatic gains in binding affinity using shape complementarity to optimise solute-solute dispersive interactions.

TL;DR: An overview of the physiological effects of ghrelin and of its pathological and potential therapeutic roles is provided and it is suggested that gh Relin might be involved in the pathogenesis of many diseases and be a therapeutic target in these diseases.

TL;DR: A roadmap is now available to guide fragment-to-lead evolution when structural information is available and the next challenge is to apply FBDD to targets for which high-resolutionStructural information is not available.

TL;DR: The metabolism and immunological relevance of sialic acids are described and how their properties have been exploited by the pharmaceutical industry to enhance the therapeutic properties of proteins such as asparaginase and darbepoetin alpha are outlined.