Developing polyphenolic acetates as radiation countermeasure agents: current status and future perspectives.

Abstract:

:Total-body exposure to ionizing radiation (TBI) results in life-threatening acute radiation syndrome (ARS), which encompasses hematopoietic and gastrointestinal (GI) injuries and results in dose-dependent morbidity and mortality. Management of ARS warrants the deployment of effective medical countermeasure agents (MCM) that protect against and/or mitigate lethal radiation injury. The polyphenolic acetate (PA) 7,8-diacetoxy-4-methylthiocoumarin (DAMTC) has been identified as a potential MCM against ARS by virtue of it mitigating the lethal effects of TBI in C57BL/6 mice. Herein, we describe current evidence, including mechanistic aspects, for the use of PAs as MCMs against ARS and provide perspectives for their further development as approved drugs for the mitigation of ARS.

journal_name

Drug Discov Today

journal_title

Drug discovery today

authors

Venkateswaran K,Shrivastava A,Prasad AK,Parmar VS,Dwarakanath BS

doi

10.1016/j.drudis.2020.02.004

subject

Has Abstract

pub_date

2020-04-01 00:00:00

pages

781-786

issue

4

eissn

1359-6446

issn

1878-5832

pii

S1359-6446(20)30072-6

journal_volume

25

pub_type

杂志文章,评审
  • The multiple therapeutic applications of miRNAs for bone regenerative medicine.

    abstract::With the aging of the general population, there is an increasing need for bone defect repair, prompting the development of reliable alternatives to autologous bone grafting, without the usually associated major drawbacks (i.e., limited volume and severe postoperative pain). Given the crucial role that miRNAs appear to...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2017.04.007

    authors: Scimeca JC,Verron E

    更新日期:2017-07-01 00:00:00

  • Where is the hope for drug discovery? Let history tell the future.

    abstract::For drug discovery, historical experience is always of significance. Through examining the history of traditional medicines, we find that these medicines have more implications for drug discovery than just providing new chemical entities. The history of traditional medicines indicates that they depended more on the co...

    journal_title:Drug discovery today

    pub_type: 历史文章,杂志文章

    doi:10.1016/j.drudis.2008.07.002

    authors: Kong DX,Li XJ,Zhang HY

    更新日期:2009-02-01 00:00:00

  • The role of the 14-3-3 protein family in health, disease, and drug development.

    abstract::14-3-3 proteins regulate intracellular signaling pathways, such as signal transduction, protein trafficking, cell cycle, and apoptosis. In addition to the ubiquitous roles of 14-3-3 isoforms, unique tissue-specific functions are also described for each isoform. Owing to their role in regulating cell cycle, protein tra...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2015.09.012

    authors: Aghazadeh Y,Papadopoulos V

    更新日期:2016-02-01 00:00:00

  • FDA-approved drug labeling for the study of drug-induced liver injury.

    abstract::Drug-induced liver injury (DILI) is a leading cause of drugs failing during clinical trials and being withdrawn from the market. Comparative analysis of drugs based on their DILI potential is an effective approach to discover key DILI mechanisms and risk factors. However, assessing the DILI potential of a drug is a ch...

    journal_title:Drug discovery today

    pub_type: 杂志文章

    doi:10.1016/j.drudis.2011.05.007

    authors: Chen M,Vijay V,Shi Q,Liu Z,Fang H,Tong W

    更新日期:2011-08-01 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

  • The neuroprotective role of the brain opioid system in stroke injury.

    abstract::Novel neuroprotective therapies are desperately needed to improve neuronal recovery after ischemic stroke and extend the therapeutic window or offset some of the adverse effects of tissue-type plasminogen activator (tPA). These advances could provide a more effective and safe therapeutic regimen for patients with isch...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2018.02.011

    authors: Vaidya B,Sifat AE,Karamyan VT,Abbruscato TJ

    更新日期:2018-07-01 00:00:00

  • Essential oils: from prevention to treatment of skin cancer.

    abstract::The increasing incidence of cutaneous malignancies signifies the need for multiple treatment options. Several available reviews have emphasized the potential role of various botanical extracts and naturally occurring compounds as anti-skin-cancer agents. Few studies relate to the role of chemoprevention and therapeuti...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2018.11.020

    authors: Pavithra PS,Mehta A,Verma RS

    更新日期:2019-02-01 00:00:00

  • The druggable genome: an update.

    abstract::Annotating the druggable genome estimates the potential maximum size of the playing field for current small-molecule drug design but It does not consider biologicals or future breakthroughs in medicinal chemistry or biology. ...

    journal_title:Drug discovery today

    pub_type: 杂志文章

    doi:10.1016/S1359-6446(05)03666-4

    authors: Russ AP,Lampel S

    更新日期:2005-12-01 00:00:00

  • Organoid-on-a-chip and body-on-a-chip systems for drug screening and disease modeling.

    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

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2016.07.003

    authors: Skardal A,Shupe T,Atala A

    更新日期:2016-09-01 00:00:00

  • The role of fragment-based and computational methods in polypharmacology.

    abstract::Polypharmacology-based strategies are gaining increased attention as a novel approach to obtaining potentially innovative medicines for multifactorial diseases. However, some within the pharmaceutical community have resisted these strategies because they can be resource-hungry in the early stages of the drug discovery...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2011.08.002

    authors: Bottegoni G,Favia AD,Recanatini M,Cavalli A

    更新日期:2012-01-01 00:00:00

  • Is the European regulatory framework sufficient to assure the safety of citizens using health products containing nanomaterials?

    abstract::The growing application of nanomaterials in healthcare products (i.e., cosmetics, medical devices, and medicinal products) has encouraged the upgrade of the regulatory framework within the European Community to better control their use and manage the risk of negative effects on human health and environment. Unfortunat...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2017.01.016

    authors: Musazzi UM,Marini V,Casiraghi A,Minghetti P

    更新日期:2017-06-01 00:00:00

  • Polymer-drug conjugates: recent advances and future perspectives.

    abstract::Polymer-drug conjugates (PDC) have exhibited clinical and commercial success in the field of drug delivery. A polymeric backbone, linker, targeting moiety, and drug constitute the building blocks of PDCs. Current attention is focusing on natural polymeric carriers, in particular the concept of graft copolymers, such a...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2020.06.028

    authors: Thakor P,Bhavana V,Sharma R,Srivastava S,Singh SB,Mehra NK

    更新日期:2020-09-01 00:00:00

  • Methods to identify and optimize small molecules interacting with RNA (SMIRNAs).

    abstract::RNAs, particularly noncoding RNAs (ncRNAs), are becoming increasingly important therapeutic targets, because they are causative and antagonists of human disease. Indeed, aberrant RNA structural elements and expression deregulate biological processes. In this review, we describe methodologies to discover and optimize s...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2019.06.019

    authors: Ursu A,Vézina-Dawod S,Disney MD

    更新日期:2019-10-01 00:00:00

  • Therapeutic potential for novel ultra long-acting β2-agonists in the management of COPD: biological and pharmacological aspects.

    abstract::Chronic obstructive pulmonary disease (COPD) is characterised by progressive airflow limitation. In moderate-to-severe COPD, long-acting bronchodilators are the basis of therapy. Inhaled long-acting β(2)-agonists (LABAs) are used for the treatment of COPD. LABAs have been in use since the 1990s enabling persistent bro...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2011.11.002

    authors: Malerba M,Radaeli A,Morjaria JB

    更新日期:2012-05-01 00:00:00

  • Learning from the past for TB drug discovery in the future.

    abstract::Tuberculosis drug discovery has shifted in recent years from a primarily target-based approach to one that uses phenotypic high-throughput screens. As examples of this, through our EU-funded FP7 collaborations, New Medicines for Tuberculosis was target-based and our more-recent More Medicines for Tuberculosis project ...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2016.09.025

    authors: Mikušová K,Ekins S

    更新日期:2017-03-01 00:00:00

  • Delivery of epidrugs.

    abstract::Inhibitors of epigenetic targets have entered clinical trials with some success, in particular for combined therapies. Like many other chemotherapeutics these new classes of molecules have dose-limiting toxicities and highly active metabolism in vivo resulting in lower efficacy than expected. This review presents drug...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2014.03.017

    authors: el Bahhaj F,Dekker FJ,Martinet N,Bertrand P

    更新日期:2014-09-01 00:00:00

  • New tools for functional genomic analysis.

    abstract::For the past decade, the development of genomic technology has revolutionized modern biological research and drug discovery. Functional genomic analyses enable biologists to perform analysis of genetic events on a global scale and they have been widely used in gene discovery, biomarker determination, disease classific...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2009.05.005

    authors: Chen X,Jorgenson E,Cheung ST

    更新日期:2009-08-01 00:00:00

  • Current and future trends in the application of HPLC-MS to metabolite-identification studies.

    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

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2007.01.007

    authors: Castro-Perez JM

    更新日期:2007-03-01 00:00:00

  • Revival of the regulatory T cell: new targets for drug development.

    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

    pub_type: 杂志文章,评审

    doi:10.1016/S1359-6446(03)03021-6

    authors: Sutmuller RP,Offringa R,Melief CJ

    更新日期:2004-04-01 00:00:00

  • Pharmaceutical patents: reconciling the human right to health with the incentive to invent.

    abstract::In developed countries that protect core aspects of the fundamental human right to the highest attainable standard of health, how does that right intersect with intellectual property rights? Here, the human rights implication of providing access to all cancer drugs recommended by experts in a developed country is cons...

    journal_title:Drug discovery today

    pub_type: 杂志文章

    doi:10.1016/j.drudis.2020.04.009

    authors: Khachigian LM

    更新日期:2020-07-01 00:00:00

  • The power of combining phenotypic and target-focused drug discovery.

    abstract::A fierce dispute has arisen between the supporters of phenotypic and target-focused screening regarding which path grants the higher probability of successful drug development. A chance to reconcile these two approaches lies in successful target deconvolution (TD) after phenotypic screens. But, despite the panoply of ...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2018.10.009

    authors: Heilker R,Lessel U,Bischoff D

    更新日期:2019-02-01 00:00:00

  • Targeting Rabs as a novel therapeutic strategy for cancer therapy.

    abstract::Rab GTPases constitute the largest family of small GTPases. Rabs regulate not only membrane trafficking but also cell signaling, growth and survival, and development. Increasingly, Rabs and their effectors are shown to be overexpressed or subject to loss-of-function mutations in a variety of disease settings, includin...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2017.03.012

    authors: Qin X,Wang J,Wang X,Liu F,Jiang B,Zhang Y

    更新日期:2017-08-01 00:00:00

  • 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 relevan...

    journal_title:Drug discovery today

    pub_type: 杂志文章

    doi:10.1016/s1359-6446(01)01910-9

    authors: Barlocco D

    更新日期:2001-08-15 00:00:00

  • Value your compound management team!

    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

    pub_type: 杂志文章

    doi:10.1016/s1359-6446(01)01816-5

    authors: Ray BJ

    更新日期:2001-06-01 00:00:00

  • Compound high-quality criteria: a new vision to guide the development of drugs, current situation.

    abstract::For several decades, the pharmaceutical industry has suffered due to major issues such as reductions of the number of FDA approved drugs and biologics. Several analyses have been highlighted that the 'druglikeness' is one of the strategies to improve succeed rates of screening such as, for instance, high-throughput sc...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2016.01.005

    authors: Mignani S,Huber S,Tomás H,Rodrigues J,Majoral JP

    更新日期:2016-04-01 00:00:00

  • The targeted delivery of cancer drugs across the blood-brain barrier: chemical modifications of drugs or drug-nanoparticles?

    abstract::One of the most challenging problems, if not the most challenging, in drug development is not to develop drugs to treat diseases of the central nervous system (CNS), but to manage to distribute them to the CNS across the blood-brain barrier (BBB) using transvascular routes following intravenous administration. The dev...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2008.09.005

    authors: Juillerat-Jeanneret L

    更新日期:2008-12-01 00:00:00

  • Hybrid poly(lactic-co-glycolic acid) nanoparticles: design and delivery prospectives.

    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

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2014.09.018

    authors: Pandita D,Kumar S,Lather V

    更新日期:2015-01-01 00:00:00

  • Diagnostic challenges for multiplexed protein microarrays.

    abstract::Multiplexed protein analysis using planar microarrays or microbeads is growing in popularity for simultaneous assays of antibodies, cytokines, allergens, drugs and hormones. However, this new assay format presents several new operational issues for the clinical laboratory, such as the quality control of protein-microa...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2006.09.010

    authors: Master SR,Bierl C,Kricka LJ

    更新日期:2006-11-01 00:00:00

  • PCSK9 and diabetes: is there a link?

    abstract::Diabetes mellitus (DM) is associated with an increased risk of cardiovascular disease (CVD). Inhibitors of proprotein convertase subtilisin/kexin type 9 (PCSK9) have emerged as effective low-density lipoprotein cholesterol-lowering compounds. Although the results of available epidemiological, preclinical, and clinical...

    journal_title:Drug discovery today

    pub_type: 杂志文章,评审

    doi:10.1016/j.drudis.2017.01.006

    authors: Momtazi AA,Banach M,Pirro M,Stein EA,Sahebkar A

    更新日期:2017-06-01 00:00:00

  • 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 relevan...

    journal_title:Drug discovery today

    pub_type: 杂志文章

    doi:10.1016/s1359-6446(01)01877-3

    authors: Barlocco D,Langston S,Tranter D

    更新日期:2001-08-01 00:00:00