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 relevance of new molecules reported in the literature and on the conference scene; Profiles offers commentary on promising lines of research, emerging molecular targets, novel technology, advances in synthetic and separation techniques and legislative issues.

journal_name

Drug Discov Today

journal_title

Drug discovery today

authors

Westwell AD

doi

10.1016/s1359-6446(01)02006-2

subject

Has Abstract

pub_date

2001-11-15 00:00:00

pages

1176-1177

issue

22

eissn

1359-6446

issn

1878-5832

pii

S1359-6446(01)02006-2

journal_volume

6

pub_type

杂志文章
  • Raising the bar in anticancer therapy: recent advances in, and perspectives on, telomerase inhibitors.

    abstract::Telomerase is a ribonucleic reverse transcriptase enzyme that uses an integral RNA component as a template to add tandem telomeric DNA repeats, TTAGGG, at the 3' end of the chromosomes. 85-90% of human tumors and their derived cell lines predominantly express high levels of telomerase, therefore contributing to cancer...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2019.05.015

    authors: Saraswati AP,Relitti N,Brindisi M,Gemma S,Zisterer D,Butini S,Campiani G

    更新日期:2019-07-01 00:00:00

  • Genomic microarrays in the spotlight.

    abstract::Microarray-based comparative genomic hybridization (array-CGH) has emerged as a revolutionary platform, enabling the high-resolution detection of DNA copy number aberrations. In this article we outline the use and limitations of genomic clones, cDNA clones and PCR products as targets for genomic microarray constructio...

    journal_title:Drug discovery today

    pub_type: 杂志文章

    doi:

    authors: Mantripragada KK,Buckley PG,de Ståhl TD,Dumanski JP

    更新日期:2004-12-15 00:00:00

  • Fsp3: A new parameter for drug-likeness.

    abstract::The drug-likeness of a compound is a key factor during the initial phases of drug discovery. It can be defined as the similarity between compounds and drugs. Here, we collate research related to the fraction of sp3 carbon atoms (Fsp3), including related high-throughput screening (HTS) cases, structural modifications b...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2020.07.017

    authors: Wei W,Cherukupalli S,Jing L,Liu X,Zhan P

    更新日期:2020-07-24 00:00:00

  • Advances in the computational development of DNA methyltransferase inhibitors.

    abstract::DNA methylation is an epigenetic change that results in the addition of a methyl group at the carbon-5 position of cytosine residues. The process is mediated by DNA methyltransferases (DNMTs), a family of enzymes for which inhibition is a promising strategy for the treatment of cancer and other diseases. Here, we revi...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2011.02.003

    authors: Medina-Franco JL,Caulfield T

    更新日期:2011-05-01 00:00:00

  • pH-dependent ileocolonic drug delivery, part I: in vitro and clinical evaluation of novel systems.

    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

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2020.06.011

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

    更新日期:2020-08-01 00:00:00

  • Optimizing the use of open-source software applications in drug discovery.

    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

    pub_type: 杂志文章,评审

    doi:10.1016/S1359-6446(05)03692-5

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

    更新日期:2006-02-01 00:00:00

  • Chemical ligands, genomics and drug discovery.

    abstract::The sequencing of the human genome and numerous pathogen genomes has resulted in an explosion of potential drug targets. These targets represent both an unprecedented opportunity and a technological challenge for the pharmaceutical industry. A new strategy is required to initiate small-molecule drug discovery with set...

    journal_title:Drug discovery today

    pub_type: 杂志文章

    doi:10.1016/s1359-6446(00)01468-9

    authors: Lenz GR,Nash HM,Jindal S

    更新日期:2000-04-01 00:00:00

  • Delivery of small molecules for bone regenerative engineering: preclinical studies and potential clinical applications.

    abstract::Stimulation of bone regeneration using growth factors is a promising approach for musculoskeletal regenerative engineering. However, common limitations with protein growth factors, such as high manufacturing costs, protein instability, contamination issues, and unwanted immunogenic responses of the host reduce potenti...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2014.01.012

    authors: Laurencin CT,Ashe KM,Henry N,Kan HM,Lo KW

    更新日期:2014-06-01 00:00:00

  • Fetal hypoxia and programming of matrix metalloproteinases.

    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

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2011.09.011

    authors: Tong W,Zhang L

    更新日期:2012-02-01 00:00:00

  • Mistletoe compound enters clinical trials.

    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

    pub_type: 杂志文章

    doi:10.1016/s1359-6446(02)02571-0

    authors: Habeck M

    更新日期:2003-01-15 00:00:00

  • Active targeting with particulate drug carriers in tumor therapy: fundamentals and recent progress.

    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

    pub_type: 杂志文章,评审

    doi:10.1016/S1359-6446(03)02988-X

    authors: Marcucci F,Lefoulon F

    更新日期:2004-03-01 00:00:00

  • Microarray patches: potentially useful delivery systems for long-acting nanosuspensions.

    abstract::Long-acting drug nanosuspension formulations are coming to the fore as controlled release strategies for several medical conditions and as a preventative measure against HIV infection. However, such delivery systems must, by necessity, be given by hypodermic injection, typically into muscle. This poses problems for pa...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2017.10.013

    authors: Donnelly RF,Larrañeta E

    更新日期:2018-05-01 00:00:00

  • Atomic force microscopy and drug discovery.

    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

    pub_type: 杂志文章,评审

    doi:10.1016/S1359-6446(03)02905-2

    authors: Edwardson JM,Henderson RM

    更新日期:2004-01-15 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

    doi:10.1016/s1359-6446(01)01925-0

    authors: Yuan Z,Trias J,White RJ

    更新日期:2001-09-15 00:00:00

  • Dimerization of chemokine receptors in living cells: key to receptor function and novel targets for therapy.

    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

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2008.04.004

    authors: Wang J,Norcross M

    更新日期:2008-07-01 00:00:00

  • Novel approaches to the pharmacotherapy of pulmonary arterial hypertension.

    abstract::Pulmonary arterial hypertension (PAH) has evolved from an untreatable condition to a disease for which several classes of drugs have now been approved, including various prostanoids, endothelin receptor antagonists and phosphodiesterase-5 inhibitors. Because the pathogenesis of pulmonary hypertension is increasingly u...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2008.12.003

    authors: Olsson KM,Hoeper MM

    更新日期:2009-03-01 00:00:00

  • Support vector machines approach for predicting druggable proteins: recent progress in its exploration and investigation of its usefulness.

    abstract::Identification and validation of viable targets is an important first step in drug discovery and new methods, and integrated approaches are continuously explored to improve the discovery rate and exploration of new drug targets. An in silico machine learning method, support vector machines, has been explored as a new ...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2007.02.015

    authors: Han LY,Zheng CJ,Xie B,Jia J,Ma XH,Zhu F,Lin HH,Chen X,Chen YZ

    更新日期:2007-04-01 00:00:00

  • Cancer cell senescence: a new frontier in drug development.

    abstract::Senescence forms a universal block to tumorigenesis which impacts on all hallmarks of cancer, making it an attractive target for drug discovery. Therefore a strategy must be devised to focus this broad potential into a manageable drug discovery programme. Several issues remain to be addressed including the lack of rob...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2012.01.019

    authors: Cairney CJ,Bilsland AE,Evans TR,Roffey J,Bennett DC,Narita M,Torrance CJ,Keith WN

    更新日期:2012-03-01 00:00:00

  • Novel antitussive strategies.

    abstract::Acute and chronic cough represent one of the most common symptoms of medical importance but effective pharmacotherapy is, to all intents and purposes, absent. Numerous initiatives targeting the recently discovered tussive pathways are in progress. Here, we review the current antitussive armamentarium and provide an up...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2012.11.004

    authors: Morjaria JB,Dickinson RS,Morice AH

    更新日期:2013-04-01 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

    doi:10.1016/j.drudis.2014.06.020

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

    更新日期:2014-10-01 00:00:00

  • Sharing lessons learnt across European cardiovascular research consortia.

    abstract::Research consortia in Europe often compete with each other for skills, human and technical resources and, eventually, recognition of the scientific impact of their work. In response to the same EU Horizon2020 call, we received funding for our research project proposals to identify and validate novel drug targets for c...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2020.01.009

    authors: de Jong L,Bobeldijk-Pastorova I,Erdmann J,Bijker-Schreurs M,Schunkert H,Kuivenhoven JA,van Gool AJ

    更新日期:2020-04-01 00:00:00

  • Impact of organ-on-a-chip technology on pharmaceutical R&D costs.

    abstract::Healthcare systems are faced with the challenge of providing innovative treatments, while shouldering high drug costs that pharmaceutical companies justify by the high costs of R&D. An emergent technology that could transform R&D efficiency is organ-on-a-chip. The technology bridges the gap between preclinical testing...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2019.06.003

    authors: Franzen N,van Harten WH,Retèl VP,Loskill P,van den Eijnden-van Raaij J,IJzerman M

    更新日期:2019-09-01 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

    doi:10.1016/j.drudis.2020.09.023

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

    更新日期:2020-12-01 00:00:00

  • Analysis of clinical trials of new drugs in China as of 2019.

    abstract::The research and development (R&D) of new drugs indicates scientific progress and economic development. However, little is known regarding ongoing or recent clinical trials in China. We analyzed data from clinical trials published before December 31, 2019, and found that the annual registration numbers are increasing ...

    journal_title:Drug discovery today

    pub_type: 杂志文章

    doi:10.1016/j.drudis.2020.09.030

    authors: Lin L,Chen Y,Yan L,Liu Y,Ni J,Yang H,Li H

    更新日期:2020-12-01 00:00:00

  • Translation of drug effects from experimental models of neuropathic pain and analgesia to humans.

    abstract::Neuropathic pain research remains a challenging undertaking owing to: (i) the lack of understanding about the underlying disease processes; and (ii) poor predictive validity of the current models of evoked pain used for the screening of novel compounds. Common consensus is that experimental models replicate symptoms (...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2012.02.010

    authors: Taneja A,Di Iorio VL,Danhof M,Della Pasqua O

    更新日期:2012-08-01 00:00:00

  • Towards a gold standard: regarding quality in public domain chemistry databases and approaches to improving the situation.

    abstract::In recent years there has been a dramatic increase in the number of freely accessible online databases serving the chemistry community. The internet provides chemistry data that can be used for data-mining, for computer models, and integration into systems to aid drug discovery. There is however a responsibility to en...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2012.02.013

    authors: Williams AJ,Ekins S,Tkachenko V

    更新日期:2012-07-01 00:00:00

  • Target 2035: probing the human proteome.

    abstract::Biomedical scientists tend to focus on only a small fraction of the proteins encoded by the human genome despite overwhelming genetic evidence that many understudied proteins are important for human disease. One of the best ways to interrogate the function of a protein and to determine its relevance as a drug target i...

    journal_title:Drug discovery today

    pub_type: 杂志文章

    doi:10.1016/j.drudis.2019.06.020

    authors: Carter AJ,Kraemer O,Zwick M,Mueller-Fahrnow A,Arrowsmith CH,Edwards AM

    更新日期:2019-11-01 00:00:00

  • Storage and transmission of microarray images.

    abstract::With the recent explosion of interest in microarray technology, massive amounts of microarray images are currently being produced. The storage and transmission of these types of data are becoming increasingly challenging. This article reviews the latest technologies that allow for the compression and storage of microa...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审

    doi:10.1016/S1359-6446(05)03647-0

    authors: Luo Y,Lonardi S

    更新日期:2005-12-01 00:00:00

  • In silico platform for xenobiotics ADME-T pharmacological properties modeling and prediction. Part II: The body in a Hilbertian space.

    abstract::We have broken old surviving dogmas and concepts used in computational chemistry and created an efficient in silico ADME-T pharmacological properties modeling and prediction toolbox for any xenobiotic. With the help of an innovative and pragmatic approach combining various in silico techniques, like molecular modeling...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2009.01.013

    authors: Jacob A,Pratuangdejkul J,Buffet S,Launay JM,Manivet P

    更新日期:2009-04-01 00:00:00

  • The microRNA landscape of cutaneous squamous cell carcinoma.

    abstract::Cutaneous squamous cell carcinoma (cSCC) is a keratinocyte-derived skin tumor. It is the second-most-common cancer affecting the Caucasian population and is responsible for >20% of all skin-cancer-related deaths. The estimated incidence of non-melanoma skin cancer in the USA is >1000000 cases per year, of which roughl...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2018.01.023

    authors: Konicke K,López-Luna A,Muñoz-Carrillo JL,Servín-González LS,Flores-de la Torre A,Olasz E,Lazarova Z

    更新日期:2018-04-01 00:00:00