abstract：:There is currently a marketed drug for nearly every nuclear receptor for which the natural ligand has been identified. However, because of the complexity of signal transduction by this class of ligand-regulated transcription factors, few of these drugs have been optimized for pharmaceutical effectiveness. Over the pas...

journal_title：Drug discovery today

authors： Pearce KH,Iannone MA,Simmons CA,Gray JG

更新日期：2004-09-01 00:00:00

abstract：:Transdermal drug delivery offers an attractive alternative to the conventional drug delivery methods of oral administration and injection. However, the stratum corneum acts as a barrier that limits the penetration of substances through the skin. Application of ultrasound to the skin increases its permeability (sonopho...

journal_title：Drug discovery today

authors： Lavon I,Kost J

更新日期：2004-08-01 00:00:00

abstract：:For many years, there has been spirited debate as to the relative importance of environmental and genetic factors in the pathogenesis of cancer. Current efforts to annotate the human genome for germ-line genetic variants should establish the foundation for dissecting the contribution of genetics to the risk for cancer...

journal_title：Drug discovery today

authors： Savage SA,Chanock SJ

更新日期：2004-07-15 00:00:00

abstract：:Peptide-based drugs are now viable alternatives to biopharmaceuticals, such as antibodies. Most of the past limitations of peptides have been removed by new technologies, so that peptides now face similar hurdles to antibodies. Phage-display technology provides novel peptides that bind protein targets with high affini...

journal_title：Drug discovery today

authors： Ladner RC,Sato AK,Gorzelany J,de Souza M

更新日期：2004-06-15 00:00:00

abstract：:Compelling new evidence supports the idea that regulatory T cells play a major role in our immune system. Several subsets of these regulators have been identified recently. Differences in the phenotypical and functional characteristics of these subsets have immunological implications. From our growing knowledge of the...

journal_title：Drug discovery today

authors： Sutmuller RP,Offringa R,Melief CJ

更新日期：2004-04-01 00:00:00

abstract：:Drug therapy for the treatment of tumors is often limited by a narrow therapeutic index. One approach that overcomes this limitation is the active targeting of tumors with particulate drug carriers. The derivatization of particulate drug carriers with a ligand leads to the selective targeting of the particulate to sel...

journal_title：Drug discovery today

authors： Marcucci F,Lefoulon F

更新日期：2004-03-01 00:00:00

abstract：:Many of the drug candidates that fail in clinical trials are withdrawn because of unforeseen effects of human metabolism, such as toxicity and unfavorable pharmacokinetic profiles. Early pre-clinical elimination of such compounds is important but not yet possible. An ideal system would enable researchers to make a con...

journal_title：Drug discovery today

authors： Bugrim A,Nikolskaya T,Nikolsky Y

更新日期：2004-02-01 00:00:00

abstract：:The completion of the human genome sequencing project has provided a flood of new information that is likely to change the way scientists approach the study of complex biological systems. A major challenge lies in translating this information into new and better ways to treat human disease. The multidisciplinary scien...

journal_title：Drug discovery today

authors： Jeffery DA,Bogyo M

更新日期：2004-01-15 00:00:00

abstract：:Atomic force microscopy is being used ever more widely in biological imaging, because of its unique ability to provide structural information at the single molecule level and under near-physiological conditions. Detailed topographic images of potential drug targets, such as proteins and DNA, have been produced, and th...

journal_title：Drug discovery today

authors： Edwardson JM,Henderson RM

更新日期：2004-01-15 00:00:00

abstract：:The cachexia syndrome, characterized by a marked weight loss, anorexia, asthenia and anaemia, is invariably associated with the growth of a tumour and leads to a malnutrition status caused by the induction of anorexia or decreased food intake. In addition, the competition for nutrients between the tumour and the host ...

journal_title：Drug discovery today

authors： Argilés JM,Moore-Carrasco R,Busquets S,López-Soriano FJ

更新日期：2003-09-15 00:00:00

abstract：:The focus of high-throughput drug discovery has progressed through the genome and the transcriptome and is now moving towards more difficult problems in assessing the proteome, glycome and metabolome. Microarrays are currently the major tool in the assessment of gene expression via cDNA or RNA analysis; however, they ...

journal_title：Drug discovery today

authors： Howbrook DN,van der Valk AM,O'Shaughnessy MC,Sarker DK,Baker SC,Lloyd AW

更新日期：2003-07-15 00:00:00

abstract：:In the past five years therapeutic monoclonal antibodies have established themselves as perhaps the most important and rapidly expanding class of therapeutic drugs. More than 25% of pharmacological agents that are currently under development are based on antibodies and the total income generated from them in 2002 exce...

journal_title：Drug discovery today

authors： Glennie MJ,van de Winkel JG

更新日期：2003-06-01 00:00:00

abstract：:Genomics and gene expression data require interpretation at the protein level to validate the biological or pathological findings. To match with the efficiency and capacity of DNA microarray application, methods and approaches of protein analysis in multiplex and high-throughput manner are required for effectively dis...

journal_title：Drug discovery today

authors： Zhang WW

更新日期：2003-04-15 00:00:00

abstract：:The proces of piecemeal microautophagy of the nucleus describes the way in which autophagy occurs in the nucleus, a realm of the cell once considered to be off limits for autophagy. ...

journal_title：Drug discovery today

authors： Sutherland S

更新日期：2003-03-15 00:00:00

abstract：:The potential of peptide and protein anticancer agents has yet to be realized owing to the many unresolved problems concerning their delivery to the site of a tumor and into tumor cells. However, our understanding of the mechanisms underlying the biological fate and biodistribution of protein and peptide drugs has adv...

journal_title：Drug discovery today

authors： Torchilin VP,Lukyanov AN

更新日期：2003-03-15 00:00:00

abstract：:Sudden cardiac death, secondary to ventricular fibrillation (VF), remains the leading cause of death in the USA. Recent experimental and theoretical studies suggest that VF could be caused by spiral wave re-entry. The initiation and subsequent break-up of spiral waves has been linked to electrical alternans, a phenome...

journal_title：Drug discovery today

authors： Gilmour RF Jr

更新日期：2003-02-15 00:00:00

abstract：:Highlights of the 9th (Biennial) International Congress on TNF-Related Cytokines (30 October-2 November 2002; The Manchester Grand Hyatt, San Diego, CA, USA. ...

journal_title：Drug discovery today

authors： Steed PM,Hubert RS

更新日期：2003-02-01 00:00:00

abstract：:A drug has entered clinical trials that contains a recombinant version of the main extract from mistletoe, adn holds promise for cancer patients. ...

journal_title：Drug discovery today

authors： Habeck M

更新日期：2003-01-15 00:00:00

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

authors： Kau TR,Silver PA

更新日期：2003-01-15 00:00:00

abstract：:Treatment of neurodegenerative diseases, such as Alzheimer's disease, multiple sclerosis, Parkinson's disease and amyotrophic lateral sclerosis (ALS), represents a major challenge for the pharmaceutical industry. These disorders have common and unique molecular pathological characteristics that result in serious reduc...

journal_title：Drug discovery today

authors： Mathisen PM

更新日期：2003-01-01 00:00:00

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

authors： Taylor PW,Stapleton PD,Paul Luzio J

更新日期：2002-11-01 00:00:00

abstract：:To enable the list of genes and proteins contained within genomic databases to be useful for drug discovery, we need to understand how the genome maps into the phenome. An essential, but not explicitly listed ingredient of the genome is the regulatory interactions between genes and proteins that form a genome-wide net...

journal_title：Drug discovery today

authors： Huang S

更新日期：2002-10-15 00:00:00

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

authors： Claus BL,Underwood DJ

更新日期：2002-09-15 00:00:00

abstract：:Identifying the right target for drug development is a critical bottleneck in the pharmaceutical and biotech industries. The genomics revolution has shifted the problem from a scarcity of targets to a surplus of putative drug targets. As the validity of a target cannot be simply inferred from correlative data, the key...

journal_title：Drug discovery today

authors： Ilag LL,Ng JH,Beste G,Henning SW

更新日期：2002-09-15 00:00:00

abstract：:To successfully research and develop an animal pharmaceutical dosage form, a diverse array of issues covering basic medicine, pharmacology and technology must be addressed. Societal concerns regarding animal and public health, as well as the rapidly changing farming and economic environments, provide additional challe...

journal_title：Drug discovery today

authors： Rathbone MJ,Martinez MN

更新日期：2002-08-01 00:00:00

abstract：:Functional proteomics approaches aim to characterize comprehensively the function of gene products, and provide a first-level understanding of cellular mechanisms. Here, we review recent techniques for the construction and prediction of large-scale protein-interaction networks, with a particular emphasis on computatio...

journal_title：Drug discovery today

authors： Schächter V

更新日期：2002-06-01 00:00:00

abstract：:Although many existing methods are used to study the functions of ion channels and to screen lead compounds for important ion-channel targets, new technologies are being developed for improved performance. It is important to identify the advantages and disadvantages of each technology. In this review, we segment the i...

journal_title：Drug discovery today

authors： Xu J,Wang X,Ensign B,Li M,Wu L,Guia A,Xu J

更新日期：2001-12-15 00:00:00

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

authors： Westwell AD

更新日期：2001-11-15 00:00:00

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

authors： Yuan Z,Trias J,White RJ

更新日期：2001-09-15 00:00:00

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

authors： Barlocco D

更新日期：2001-08-15 00:00:00

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

authors： Barlocco D,Langston S,Tranter D

更新日期：2001-08-01 00:00:00

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

authors： Langston S,Barlocco D

更新日期：2001-07-01 00:00:00

abstract：:The transition from slow, manual, low-throughput screening to industrialized robotic ultra-high throughput screening (uHTS) in the past few years has made it possible to screen hundreds of thousands of chemical entities against a biological target in a short time-frame. The need to minimize the cost of screening has b...

journal_title：Drug discovery today

authors： Wölcke J,Ullmann D

更新日期：2001-06-01 00:00:00

abstract：:The Discussion Forum provides a medium for airing your views on any issues related to the pharmaceutical industry and obtaining feedback and discussion on these views from others in the field. You can discuss issues that get you hot under the collar, practical problems at the bench, recently published literature, or j...

journal_title：Drug discovery today

authors： Ray BJ

更新日期：2001-06-01 00:00:00

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

authors： Barrett D,Barlocco D,Tranter D

更新日期：2001-03-01 00:00:00

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

authors： Westwell A

更新日期：2001-02-01 00:00:00

abstract：:Effective direct inhibition of adhesion receptors by small molecules has been hampered by extended receptor-ligand interfaces as well as the entropic penalties often associated with inhibition of cell adhesion. Therefore, alternative strategies have targeted enzymes that are centrally involved in the biosynthesis of r...

journal_title：Drug discovery today

authors： Hemmerich S

更新日期：2001-01-01 00:00:00

abstract：:The successful cloning and subsequent clinical application of recombinant cytokines and/or growth factors has generated a number of important therapeutics. In contrast to the G-protein-coupled receptors, identification of small-molecule agonists of the cytokine and/or growth factor receptor family has proved difficult...

journal_title：Drug discovery today

authors： Miller SG

更新日期：2000-12-01 00:00:00

abstract：:'Many professional scientists over the years have expressed their thoughts and ideas in poetry.' ...

journal_title：Drug discovery today

authors： Rowe RC

更新日期：2000-10-01 00:00:00

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

authors： Edwards P

更新日期：2000-10-01 00:00:00