abstract：:Intravitreal injection is one of the major administration routes for the treatment of posterior ocular diseases. Intravitreal therapeutics usually suffer from unsatisfactory efficacy owing to fast clearance from the vitreous humour and insufficient distribution into the retina. Engineered nanoparticles have been appli...

journal_title：Drug discovery today

authors： Huang X,Chau Y

更新日期：2019-08-01 00:00:00

abstract：:A reduction in intraocular pressure (IOP) is the only recognized therapy for glaucoma. Hence, drugs exhibiting ocular hypotensive effects are important targets for antiglaucomatous drug development. IOP is determined by the equilibrium of aqueous humor production and outflow through either the trabecular meshwork or t...

journal_title：Drug discovery today

authors： Garhöfer G,Schmetterer L

更新日期：2019-08-01 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：: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

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

abstract：:The eventual candidate drug (CD) is often already synthesized during early drug discovery but not nominated until much later. To facilitate the rapid identification of a potential CD, a thoroughly worked-out CD target profile (CDTP) with criteria acceptable for the disease target product profile (TPP) is required at t...

journal_title：Drug discovery today

authors： Bergström F,Lindmark B

更新日期：2019-06-01 00:00:00

abstract：:Thermodynamic profiles of ligand binding, particularly enthalpically favored binding signatures, have been suggested as a criterion to support the decision-making process around which compounds to select for further optimization in drug development. The concept was enthusiastically taken up, but turned out to be too s...

journal_title：Drug discovery today

authors： Klebe G

更新日期：2019-04-01 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：:Outnumbering our own cells over ten times, gut microbes can even be considered an additional organ. Several studies have explored the association between microbiomes and antitumor drug response. It has been reported that the presence of specific bacteria might modulate cancer progression and the efficacy of anticancer...

journal_title：Drug discovery today

authors： Chen B,Du G,Guo J,Zhang Y

更新日期：2019-04-01 00:00:00

abstract：:The pregnane X receptor (PXR) and the constitutive androstane receptor (CAR) are ligand-activated nuclear receptors (NRs) that are notorious for their role in drug metabolism, causing unintended drug-drug interactions and decreasing drug efficacy. They control the xenobiotic detoxification system by regulating the exp...

journal_title：Drug discovery today

authors： Chai SC,Lin W,Li Y,Chen T

更新日期：2019-03-01 00:00:00

abstract：:Rare-disease drug development is both scientifically and commercially challenging. This case study highlights Agilis Biotherapeutics (Agilis), a small private biotechnology company that has developed the most clinically advanced adeno-associated virus (AAV) gene therapy for the brain. In an international collaboration...

journal_title：Drug discovery today

authors： Das S,Huang S,Lo AW

更新日期：2019-03-01 00:00:00

abstract：:Following multiple warnings from governments and health organisations, there has been renewed investment, led by the public sector, in the discovery of novel antimicrobials to meet the challenge of rising levels of drug-resistant infection, particularly in the case of resistance to antibiotics. Initiatives have also b...

journal_title：Drug discovery today

authors： Dougan G,Dowson C,Overington J,Next Generation Antibiotic Discovery Symposium Participants.

更新日期：2019-02-01 00:00:00

abstract：:Neurodegenerative diseases (NDs), including Alzheimer's disease (AD) and Parkinson's disease (PD), threaten the health of an ever-growing number of older people worldwide; so far, there are no effective cures. Significant efforts have been devoted to developing new drugs for NDs in recent years, and some small molecul...

journal_title：Drug discovery today

authors： Wang ZY,Sreenivasmurthy SG,Song JX,Liu JY,Li M

更新日期：2019-02-01 00:00:00

abstract：:Cancer is the second highest cause of death worldwide. Several therapeutic approaches, such as conventional chemotherapy, antibodies and small molecule inhibitors and nanotherapeutics have been employed in battling cancer. Amongst them, nanotheranostics is an example of successful personalized medicine bearing dual ro...

journal_title：Drug discovery today

authors： Nabil G,Bhise K,Sau S,Atef M,El-Banna HA,Iyer AK

更新日期：2019-02-01 00:00:00

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

authors： Pavithra PS,Mehta A,Verma RS

更新日期：2019-02-01 00:00:00

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

authors： Heilker R,Lessel U,Bischoff D

更新日期：2019-02-01 00:00:00

abstract：:Nonalcoholic steatohepatitis (NASH) is emerging as a major public health issue for the 21st century and is associated with significant liver-related morbidity and mortality. At present, there are no approved drug therapies for NASH. Consequently, NASH has become the focus of significant public and private research and...

journal_title：Drug discovery today

authors： Black D,Brockbank S,Cruwys S,Goldenstein K,Hein P,Humphries B

更新日期：2019-02-01 00:00:00

abstract：:Inhibition of vascular endothelial growth factor (VEGF) or its corresponding receptor (VEGFR) has been validated as an efficacious antiangiogenetic approach for cancer treatment. More recently, neuropilins (NRPs), the essential coreceptors for VEGF, have also been shown to have a significant role in VEGF signaling. Gi...

journal_title：Drug discovery today

authors： Peng K,Bai Y,Zhu Q,Hu B,Xu Y

更新日期：2019-02-01 00:00:00

abstract：:Carcinomas overexpressing EGFR family receptors are of high clinical importance, because the receptors have prognostic value and are used as molecular targets for anticancer therapy. Insufficient drug efficacy necessitates further in-depth research of the receptor biology and improvement in preclinical stages of drug ...

journal_title：Drug discovery today

authors： Sokolova EA,Vodeneev VA,Deyev SM,Balalaeva IV

更新日期：2019-01-01 00:00:00

abstract：:Cancer and arthritis present an enormous challenge to society. They share pathogenic pathways that involve extracellular matrix degradation, tissue invasion, and inflammation. Most cancer and arthritis treatments affect normal cell function to cause significant adverse effects in patients. Specific pathways that promo...

journal_title：Drug discovery today

authors： Krishnan H,Miller WT,Blanco FJ,Goldberg GS

更新日期：2019-01-01 00:00:00

abstract：:Drug-induced rhabdomyolysis (DIR) is an idiosyncratic and fatal adverse drug reaction (ADR) characterized in severe muscle injuries accompanied by multiple-organ failure. Limited knowledge regarding the pathophysiology of rhabdomyolysis is the main obstacle to developing early biomarkers and prevention strategies. Giv...

journal_title：Drug discovery today

authors： Wen Z,Liang Y,Hao Y,Delavan B,Huang R,Mikailov M,Tong W,Li M,Liu Z

更新日期：2019-01-01 00:00:00

abstract：:3D bioprinting has emerged as the intersection between chemistry, biology and technology. Through its integration of cells, biocompatible materials and robotic-controlled dispensing systems, the process enables the production of structures that are biomimetic and functional, thus revolutionizing the concept of tissue ...

journal_title：Drug discovery today

authors： Parak A,Pradeep P,du Toit LC,Kumar P,Choonara YE,Pillay V

更新日期：2019-01-01 00:00:00

abstract：:Target concentration is typically not considered in drug discovery. However, if targets are expressed at relatively high concentrations and compounds have high affinity, such that most of the drug is bound to its target, in vitro screens can give unreliable information on compound affinity. In vivo, a similar situatio...

journal_title：Drug discovery today

authors： Smith DA,van Waterschoot RAB,Parrott NJ,Olivares-Morales A,Lavé T,Rowland M

更新日期：2018-12-01 00:00:00

abstract：:Regenerative medicine involves the study of cells, signaling cues and biomatrices to restore normal function of tissues and organs. To develop the matrices for use in tissue engineering there are three main groups of biomaterials: (i) naturally derived materials; (ii) synthetic polymers; and (iii) decellularized organ...

journal_title：Drug discovery today

authors： Steffens D,Braghirolli DI,Maurmann N,Pranke P

更新日期：2018-08-01 00:00:00

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

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

更新日期：2018-07-01 00:00:00

abstract：:Increasing evidence indicates that extracellular vesicles (EVs) are key players in undesirable cell-cell communication in cancer. However, the release of EVs is not unique to cancer cells; normal cells release EVs to perform physiological roles. Thus, selective inhibition of EV release from cancer cells is desirable. ...

journal_title：Drug discovery today

authors： Lowry MC,O'Driscoll L

更新日期：2018-06-01 00:00:00

abstract：:New therapies based on the use of biomolecules [e.g., proteins, peptides, and non-coding (nc)RNAs] have emerged during the past few years. Given their instability, adverse effects, and limited ability to cross cell membranes, delivery systems are required to fully reveal their biological potential. Sophisticated nanof...

journal_title：Drug discovery today

authors： Lino MM,Ferreira L

更新日期：2018-05-01 00:00:00

abstract：:A quantitative analysis has cast doubt over the limited advantages provided by particles for nose-to-brain (NTB) drug delivery. Thus, it is imperative to identify the role of nanovehicles in NTB drug delivery. If nanocarriers are used merely as an option to improve various properties of the drugs or the formulations, ...

journal_title：Drug discovery today

authors： Feng Y,He H,Li F,Lu Y,Qi J,Wu W

更新日期：2018-05-01 00:00:00

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

authors： Donnelly RF,Larrañeta E

更新日期：2018-05-01 00:00:00

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

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

abstract：:Epidermal growth factor (EGFR) tyrosine kinase inhibitors (TKIs), such as gefitinib and erlotinib, show excellent clinical efficacy for patients with non-small cell lung cancer (NSCLC) with EGFR mutations, including Exon 19 deletion and single-point substitution, and L858R of exon 21. The reason for the reduction in e...

journal_title：Drug discovery today

authors： Singh M,Jadhav HR

更新日期：2018-03-01 00:00:00

abstract：:The development of tissue-engineering (TE) solutions for osteochondral (OC) regeneration has been slowed by technical hurdles related to the recapitulation of their complex and hierarchical architecture. OC defects refer to damage of both the articular cartilage and the underlying subchondral bone. To repair an OC tis...

journal_title：Drug discovery today

authors： Carvalho MR,Reis RL,Oliveira JM

更新日期：2018-03-01 00:00:00

abstract：:Dysfunction of the endocannabinoid system (ECS) has been identified in metabolic disease. Cannabinoid receptor 1 (CB1) is abundantly expressed in the brain but also expressed in the periphery. Cannabinoid receptor 2 (CB2) is more abundant in the periphery, including the immune cells. In obesity, global antagonism of o...

journal_title：Drug discovery today

authors： Shrestha N,Cuffe JSM,Hutchinson DS,Headrick JP,Perkins AV,McAinch AJ,Hryciw DH

更新日期：2018-03-01 00:00:00

abstract：:It is widely accepted that placental ischemia is central in the evolution of hypertension in pregnancy. Many studies and reviews have targeted placental ischemia to explain mechanisms for initiating pregnancy hypertension. The placenta is rich in blood vessels, which are the basis for developing placental ischemia. Ho...

journal_title：Drug discovery today

authors： Gao Q,Tang J,Li N,Liu B,Zhang M,Sun M,Xu Z

更新日期：2018-02-01 00:00:00

abstract：:Depending on the timing of market entry, radical innovations can be distinguished from incremental innovations. Whereas a radical innovation typically is the first available derivative of a drug class, incremental innovations are launched later and show a certain benefit compared with the radical innovation. Here, we ...

journal_title：Drug discovery today

authors： Alt S,Helmstädter A

更新日期：2018-02-01 00:00:00

abstract：:Indacaterol/glycopyrronium (IND/GLY) 110/50mcg was the first once-daily, long-acting β2-agonist (LABA)/long-acting muscarinic antagonist (LAMA) fixed-dose combination (FDC) approved in Europe for the treatment of chronic obstructive pulmonary disease (COPD). Development of IND/GLY was driven by the need to improve the...

journal_title：Drug discovery today

authors： Banerji D,Fogel R,Patalano F

更新日期：2018-01-01 00:00:00

abstract：:Identifying new indications for existing drugs creates new therapeutic options while bypassing much of the costs and time involved with bringing a new drug to market. The rediscovery of a generic drug, however, is a challenging pursuit because there is no formal regulatory approach and a lack of economic interest by p...

journal_title：Drug discovery today

authors： Simsek M,Meijer B,van Bodegraven AA,de Boer NKH,Mulder CJJ

更新日期：2018-01-01 00:00:00

abstract：:Advanced chemotherapy fails to treat liver cancer but recent progress in understanding epigenetic modifications have witnessed promising clinical outcomes. Epigenetic alteration is the alteration of epigenomes (surrounding histone proteins) without changing the DNA sequence. Such epigenetic mechanisms include histone ...

journal_title：Drug discovery today

authors： Zeidler R,de Freitas Soares BL,Bader A,Giri S

更新日期：2017-11-01 00:00:00

abstract：:An overview of drugs approved by FDA in 2016 reveals dramatic disruptions in long-term trends. The number of new molecular entities (NMEs) dropped, reflecting the lowest rate of small-molecule approvals observed in almost five decades. In addition, the pace of industry consolidation slowed substantially. The impact of...

journal_title：Drug discovery today

authors： Griesenauer RH,Kinch MS

更新日期：2017-11-01 00:00:00

abstract：:The tumor vasculature transports oxygen, nutrients and drugs for crucial roles in tumor therapy. Antivascular therapy directly targets existing tumor vessels to reduce blood perfusion and then inhibit tumor growth. Vascular disrupting agents and ultrasound-stimulated microbubble destruction use chemical toxicity and p...

journal_title：Drug discovery today

authors： Ho YJ,Wang TC,Fan CH,Yeh CK

更新日期：2017-10-01 00:00:00

abstract：:Here, we discuss the biomedical applications of graphene-based nanomaterials (GBNs). We examine graphene and its various derivatives, including graphene, graphene oxides (GOs), reduced graphene oxides (rGOs), graphene quantum dots (GQDs), and graphene composites, and discuss their unique properties related to their bi...

journal_title：Drug discovery today

authors： Zhao H,Ding R,Zhao X,Li Y,Qu L,Pei H,Yildirimer L,Wu Z,Zhang W

更新日期：2017-09-01 00:00:00