Showing papers in "Drug Discovery Today in 2012"

TL;DR: This review presents a classification scheme for cell-penetrating peptides based on their physical-chemical properties and origin, and provides a general framework for understanding and discovering new CPPs.

TL;DR: The design and development of nanoparticles, self-assemblies, nanogels, liposomes and complex fabrication for sustained and efficient curcumin delivery and the anticancer applications and clinical benefits of nanocurcumin formulations are focused on.

TL;DR: A key finding was that an integrated understanding of the fundamental pharmacokinetic/pharmacodynamic principles of exposure at the site of action, target binding and expression of functional pharmacological activity all determine the likelihood of candidate survival in Phase II trials and improve the chance of progression to Phase III.

TL;DR: The sustained, controlled and targeted delivery of chemotherapeutic drugs in a combination approach enhanced therapeutic anticancer effects with reduced drug-associated side effects is summarized.

TL;DR: An emerging 'symbiotic model of innovation', that addresses underlying issues in drug failure and attempts to narrow gaps in current drug discovery processes, is discussed to boost productivity.

TL;DR: A large number of compounds with low solubility have been developed in the past few years for use in drug discovery and drug development, and these include polymethine-like compounds, which have shown promise in the treatment of cancer.

TL;DR: This review focuses on the basic theranostic approach, the different materials used in theranostics, the Branostic applications and future directions based on recent developments in these areas.

TL;DR: An overview of key enabling technologies is provided and the wealth of recent work regarding on-chip tissue models is highlighted, to discuss the current challenges and future directions of organ-on-chip development.

TL;DR: The challenges and how the Open PHACTS project is hoping to address these challenges technically and socially are laid out.

TL;DR: Four major categories of scaffold hopping are classified, namely heterocycle replacements, ring opening or closure, peptidomimetics and topology-based hopping, which are used by medicinal chemists to discover equipotent compounds with novel backbones that have improved properties.

TL;DR: The potential of the semi-synthetic BA derivative obeticholic acid (OCA), a first-in-class FXR agonist, as a safe and effective drug to address this significant unmet medical need of NASH.

TL;DR: Although liposomal anticancer drugs have grown to maturity in several indications and are now in widespread further development programmes using their theoretical advantages to fulfil the high expectations, further studies are warranted--including the development of novelliposomal formulations.

TL;DR: This short review highlights novel uses of silica-based nanoparticles (NPs) in the biomedical sector, focusing on novel techniques based on silica NPs for the most important biomedical applications.

TL;DR: It is suggested that structure-based ADMET profiling will probably join the mainstream during the coming years following current trends in the field and results suggested that.

TL;DR: Connectivity Map provides a data-driven and systematic approach for discovering associations among genes, chemicals and biological conditions such as diseases in order to identify and suggest new indications for existing drugs and elucidating mode of actions for novel chemicals.

TL;DR: In this article, the authors summarize preclinical and clinical human studies that demonstrate that A(3)AR agonists induce specific anti-inflammatory and anticancer effects through a molecular mechanism that entails modulation of the Wnt and the NF-κB signal transduction pathways.

TL;DR: An overview of the compared quantitative importance of biotransformation reactions in the metabolism of drugs and other xenobiotics is offered, based on a meta-analysis of current research interests, and the relative significance the enzyme (super)families or categories catalysing these reactions are assessed.

TL;DR: Molecular determinants, which crucially contribute to immunocytokine performance in vivo, are discussed in the article, as well as recent trends for the combined use of this novel class of biopharmaceuticals with other therapeutic agents.

TL;DR: Genetic inactivation of ATR and Chk1 abrogates cell cycle arrest and enhances cytotoxicity following exposure to DNA-damaging agents, and might also cause 'synthetic lethality' in tumour cells defective in defined DNA repair pathways.

TL;DR: This work presents the largest and newest information on plasma protein binding for 222 drugs, of which 50% show 90-100% binding, a range that could be considered as a favorable element for future lead selection.

TL;DR: A review of recent developments in targeting metabolic pathways in cancer aims to illustrate why it is believed that targeting metabolism in cancer presents such a promising therapeutic rationale.

TL;DR: The basic principles of kinetics and thermodynamics of target-drug binding within the context of drug discovery are introduced and the best practices in the triage and chemical optimization towards clinical candidates with maximal in vivo efficacy devoid of adverse events are discussed.

TL;DR: This review describes common type I and type II RIPs, their diverse biological functions, mechanism of cell entry, stability in plasma and antigenicity, and a discussion of promising applications for RIPs in biomedicine.

TL;DR: Many advantages such as safety, biodegradability, widespread availability and low cost justify the continuing development of promising insulin delivery system based on CS.

TL;DR: It is shown that the revenue-generating potential of orphan drugs is as great as for non-orphan drugs, even though patient populations for rare diseases are significantly smaller, and suggested that orphan drugs have greater profitability when considered in the full context of developmental drivers.

TL;DR: Methods for assessing protein-ligand structure quality and a new set of identification criteria are presented here and resulted in Iridium, a highly trustworthy protein- ligand structure database to be used for development and validation of structure-based design tools for drug discovery.

TL;DR: Modifications of STD pulse programs using (13)C and (15)N nuclei are now used to overcome the signal overlapping that occurs with more complex structures.

TL;DR: The chemoinformatic profile of natural products in the Traditional Chinese Medicine database and a large collection assembled from 30 small-molecule combinatorial libraries with emphasis on assessing molecular complexity are discussed.

TL;DR: The challenges of developing reliable prediction models for P-gp inhibitors or substrates, as well as the strategies to surmount these challenges, are reviewed.

TL;DR: A brief description of the roles and potential therapeutic modulation of adipokines, such as leptin, resistin, adiponectin, apelin, visfatin, FABP-4, tumor necrosis factor-α, interleukin-6 and plasminogen activator inhibitor-1 (PAI-1) are presented.