Molecular diversity and its analysis.

abstract：:Described in this article are strategies implemented to increase the throughput of in vivo rodent pharmacokinetic (PK) studies using the snapshot PK study design and automated methods for compound submission, sample processing, data analysis and reporting. Applying snapshot PK studies to categorize the oral exposure o...

journal_title：Drug discovery today

authors： Liu B,Chang J,Gordon WP,Isbell J,Zhou Y,Tuntland T

更新日期：2008-04-01 00:00:00

abstract：:Denosumab (Dmab) was the first monoclonal antibody (mAb) approved for the treatment of osteoporosis. It blocks the receptor activator for nuclear factor κB ligand (RANKL) and acts as a potent antiresorptive agent. In contrast to classic antiresorptive agents, Dmab treatment leads to a progressive increase in bone mass...

journal_title：Drug discovery today

authors： Wang L,Huang B,Chen X,Su J

更新日期：2020-09-09 00:00:00

abstract：:The recent increase in pharmaceutical companies' efforts toward the treatment of obesity reflects recognition of the related health risks, the growth of knowledge about mechanisms that control energy balance, and the potential market for new compounds. The current patent literature gives a picture of the targets that ...

journal_title：Drug discovery today

authors： Jandacek RJ,Woods SC

更新日期：2004-10-15 00:00:00

abstract：:Manipulation of the human immune system is becoming more of a therapeutic focus as a treatment option or complement. Prominent examples are the increasing use of monoclonal antibodies in combating malignant tumours, and the numerous adoptive immunotherapy trials underway. One important aspect of any use of the human i...

journal_title：Drug discovery today

authors： Gustafsson K,Anderson J,Fisher JPH,Yan M

更新日期：2014-06-01 00:00:00

abstract：:Drug discovery is a time consuming and costly process. Recently, a trend towards the use of in silico computational chemistry and molecular modeling for computer-aided drug design has gained significant momentum. This review investigates the application of free and/or open-source software in the drug discovery process...

journal_title：Drug discovery today

authors： Geldenhuys WJ,Gaasch KE,Watson M,Allen DD,Van der Schyf CJ

更新日期：2006-02-01 00:00:00

abstract：:Cocaine is a major drug of abuse whose devastating effects have captured the attention of health officials and policy makers. Based upon the alarming health and crime-related costs associated with the use of this powerful reinforcing drug, immediate therapies are needed for the treatment of cocaine addiction. In this ...

journal_title：Drug discovery today

authors： Smith MP,Hoepping A,Johnson KM,Trzcinska M,Kozikowski AP

更新日期：1999-07-01 00:00:00

abstract：:Understanding skin metabolism is important when considering drug discovery and safety assessment. This review compares xenobiotic skin metabolism in ex vivo skin to reconstructed human skin and reconstructed human epidermis models, concentrating on phase I and phase II enzymes. Reports on phase I enzymes are more abun...

journal_title：Drug discovery today

authors： Kazem S,Linssen EC,Gibbs S

更新日期：2019-09-01 00:00:00

abstract：:Analyzers for in-vitro diagnostic (IVD) testing facilitate the determination of medical information from biological samples. To reach a high quality, the detection reagents have to be dispensed with a high degree of precision and accuracy. A technology change from conventional pipetting systems to contact-free dispens...

journal_title：Drug discovery today

authors： Losleben N,Spinke J,Adler S,Oranth N,Zengerle R

更新日期：2013-11-01 00:00:00

abstract：:Chemokine receptors control and mediate a diverse array of physiological and pathogenic processes. Many seven transmembrane (TM) G-protein-coupled receptors (GPCRs), including chemokine receptors, exist as homo- or heterodimers. Growing evidence indicates that the dimeric form is the basic functional structure of thes...

journal_title：Drug discovery today

authors： Wang J,Norcross M

更新日期：2008-07-01 00:00:00

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

authors： Castro-Perez JM

更新日期：2007-03-01 00:00:00

abstract：:This review provides an update on the promises and pitfalls when using in vitro bioassays to evaluate beneficial and adverse health effects of botanicals and botanical preparations. Important issues addressed in the paper are: (i) the type of assays and biological effects available; (ii) false-positives, false-negativ...

journal_title：Drug discovery today

authors： Prinsloo G,Papadi G,Hiben MG,de Haan L,Louisse J,Beekmann K,Vervoort J,Rietjens IMCM

更新日期：2017-08-01 00:00:00

abstract：:Drug delivery systems are undergoing technology changes to enhance patient comfort and compliance. Electronic drug delivery (E-drug delivery) systems are being developed to regulate drug dose delivery by easy monitoring of doses, especially in chronic and age-related diseases. E-drug delivery can monitor the correct d...

journal_title：Drug discovery today

authors： Yadav KS,Kapse-Mistry S,Peters GJ,Mayur YC

更新日期：2019-04-01 00:00:00

abstract：:Fetal hypoxia adversely affects the brain and heart development, yet the mechanisms responsible remain elusive. Recent studies indicate an important role of the extracellular matrix in fetal development and tissue remodeling. The matrix metalloproteinases (MMPs) and their endogenous inhibitors, tissue inhibitors of me...

journal_title：Drug discovery today

authors： Tong W,Zhang L

更新日期：2012-02-01 00:00:00

abstract：:Model-based drug discovery (MBDDx) aims to build and continuously improve the quantitative understanding of the relation between drug exposure (target engagement) efficacy and safety, to support target validation; to define compound property criteria for lead optimization and safety margins; to set the starting dose; ...

journal_title：Drug discovery today

authors： Visser SA,Aurell M,Jones RD,Schuck VJ,Egnell AC,Peters SA,Brynne L,Yates JW,Jansson-Löfmark R,Tan B,Cooke M,Barry ST,Hughes A,Bredberg U

更新日期：2013-08-01 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：:In recent years, advances in tissue engineering and microfabrication technologies have enabled rapid growth in the areas of in vitro organoid development as well as organoid-on-a-chip platforms. These 3D model systems often are able to mimic human physiology more accurately than traditional 2D cultures and animal mode...

journal_title：Drug discovery today

authors： Skardal A,Shupe T,Atala A

更新日期：2016-09-01 00:00:00

abstract：:After the pH dependency of novel pH-dependent ileocolonic drug delivery systems is confirmed in vitro, their performance should be evaluated in human volunteers. ...

journal_title：Drug discovery today

authors： Broesder A,Woerdenbag HJ,Prins GH,Nguyen DN,Frijlink HW,Hinrichs WLJ

更新日期：2020-08-01 00:00:00

abstract：:Since the Life Science Identifier (LSID) data identification and access standard made its official debut in late 2004, several organizations have begun to use LSIDs to simplify the methods used to uniquely name, reference and retrieve distributed data objects and concepts. In this review, the authors build on introduc...

journal_title：Drug discovery today

authors： Martin S,Hohman MM,Liefeld T

更新日期：2005-11-15 00:00:00

abstract：:In recent years, there have been significant developments made in the way new drugs are being discovered and developed. Such changes are driven by new technologies that have expanded the opportunities to prepare and screen large libraries of compounds in a rapid time frame by the use of high-throughput synthesis and s...

journal_title：Drug discovery today

authors： Potoski J

更新日期：2005-01-15 00:00:00

abstract：:Huntington's disease (HD) is a progressive and fatal neurodegenerative disease, and the most common inherited CAG repeat disorder. A polyglutamine expansion in the N-terminus of the huntingtin protein (HTT) leads to protein misfolding and downstream pathogenic processes culminating in widespread functional impairment ...

journal_title：Drug discovery today

authors： Appl T,Kaltenbach L,Lo DC,Terstappen GC

更新日期：2012-11-01 00:00:00

abstract：:As the field of ocular drug delivery grows so does the potential for novel drug discovery or reformulation in lesser-known diseases of the eye. In particular, rare corneal diseases are an interesting area of research because drug delivery is limited to the outermost tissue of the eye. This review will highlight the op...

journal_title：Drug discovery today

authors： Jimenez J,Sakthivel M,Nischal KK,Fedorchak MV

更新日期：2019-08-01 00:00:00

abstract：:Medical oncologists are increasingly using anti-angiogenic drugs, but identifying the best-suited drug and the optimal dosage and schedule for treatment of patients remain challenging issues. Circulating endothelial cells (CECs) and circulating endothelial progenitors (CEPs) are modulated in a variety of diseases incl...

journal_title：Drug discovery today

authors： Bertolini F,Mancuso P,Shaked Y,Kerbel RS

更新日期：2007-10-01 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：: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：: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

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

更新日期：2014-09-01 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 US Food and Drug Administration (FDA) Expanded Access (EA) Program, which allows for compassionate uses of unapproved therapeutics and diagnostics outside of clinical trials, has gained significant traction during the Coronavirus 2019 (COVID-19) pandemic. While development of vaccines has been the major focus, unc...

journal_title：Drug discovery today

authors： Rizk JG,Forthal DN,Kalantar-Zadeh K,Mehra MR,Lavie CJ,Rizk Y,Pfeiffer JP,Lewin JC

更新日期：2020-11-27 00:00:00

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

authors： Pandita D,Kumar S,Lather V

更新日期：2015-01-01 00:00:00

abstract：:The concept of drug-likeness helps to optimise pharmacokinetic and pharmaceutical properties, for example, solubility, chemical stability, bioavailability and distribution profile. A number of molecular descriptors have emerged as reasonably informative and predictive, for example, the Rule-of-Five. Here, we review so...

journal_title：Drug discovery today

authors： Vistoli G,Pedretti A,Testa B

更新日期：2008-04-01 00:00:00

abstract：:The endocannabinoid system is implicated in, and regulates, several physiological processes, ranging from food intake and energy balance to pain and inflammation. 2-Arachidonoylglycerol (2-AG) is a full agonist at the cannabinoid receptors which classically mediate its effects. The activity of this bioactive lipid is ...

journal_title：Drug discovery today

authors： Alhouayek M,Masquelier J,Muccioli GG

更新日期：2014-03-01 00:00:00