Drug Discovery Today

article

The publishing and patenting strategies of successful university spinoffs in the biopharmaceutical industry

Zeynep Erden

Drug Discovery Today > 2017 > 22 > 1 > 5-9

Firms in the biopharmaceutical industry send signals to investors about the value of their knowledge by disclosing it in the form of patents and publications. In this way, they can gain reputation even before having products on the market. This paper compares the patenting and publishing activities of university spinoffs with other biopharmaceutical firms. The findings suggest that successful university...

article

Structural features of subtype-selective EP receptor modulators

Tijana Markovič, Žiga Jakopin, Marija Sollner Dolenc, Irena Mlinarič-Raščan

Drug Discovery Today > 2017 > 22 > 1 > 57-71

Prostaglandin E2 is a potent endogenous molecule that binds to four different G-protein-coupled receptors: EP1–4. Each of these receptors is a valuable drug target, with distinct tissue localisation and signalling pathways. We review the structural features of EP modulators required for subtype-selective activity, as well as the structural requirements for improved pharmacokinetic parameters. Novel...

article

The challenges of modulating the ‘rest and digest’ system: acetylcholine receptors as drug targets

Sonya VanPatten, Yousef Al-Abed

Drug Discovery Today > 2017 > 22 > 1 > 97-104

Acetylcholine, a major neurotransmitter of the parasympathetic and sympathetic nervous systems, was discovered in the early 1900s. Over the years, researchers have revealed much about its regulation, properties of its receptors and features of the downstream signaling that influence its terminal effects. The acetylcholine system, traditionally associated with neuromuscular communication, is now known...

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Predicting toxicities in humans by nonclinical safety testing: an update with particular reference to anticancer compounds

Varun Ahuja, Sanjay Bokan, Sharad Sharma

Drug Discovery Today > 2017 > 22 > 1 > 127-132

The sensitivity of the various preclinical models used to predict toxicity in humans varies. In this review, we analyze the various models used to predict safety in drug discovery and development with a view to understanding their translational value in humans. Twenty recently approved anticancer drugs were studied and the available nonclinical and clinical adverse effects information available from...

article

Cyclooxygenase-2 in glioblastoma multiforme

Jiange Qiu, Zhi Shi, Jianxiong Jiang

Drug Discovery Today > 2017 > 22 > 1 > 148-156

Glioblastoma multiforme (GBM) represents the most prevalent brain primary tumor, yet there is a lack of effective treatment. With current therapies, fewer than 5% of patients with GBM survive more than 5 years after diagnosis. Mounting evidence from epidemiological studies reveals that the regular use of nonsteroidal anti-inflammatory drugs (NSAIDs) is correlated with reduced incidence of GBM, suggesting...

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Contents page 1

Drug Discovery Today > 2017 > 22 > 1 > i

article

Recent advances in therapeutic recruitment of mammalian RNAi and bacterial CRISPR-Cas DNA interference pathways as emerging antiviral strategies

Wei-Xin Chin, Swee Kim Ang, Justin Jang Hann Chu

Drug Discovery Today > 2017 > 22 > 1 > 17-30

In invertebrate eukaryotes and prokaryotes, respectively, the RNAi and clustered regularly interspaced short palindromic repeats-CRISPR-associated (CRISPR-Cas) pathways are highly specific and efficient RNA and DNA interference systems, and are well characterised as potent antiviral systems. It has become possible to recruit or reconstitute these pathways in mammalian cells, where they can be directed...

article

Chasing the personalized medicine dream through biomarker validation in colorectal cancer

Harshali Patil, Shailaja Gada Saxena, Colin J. Barrow, Jagat R. Kanwar, more

Drug Discovery Today > 2017 > 22 > 1 > 111-119

Colorectal cancer (CRC) is a major health burden worldwide. The optimal approach to the diagnosis, management, and treatment of CRC involves multidisciplinary and integrated management practices. The field is rapidly changing because of recent advancements in delineating the molecular basis of tumorigenesis, introduction of targeted therapy, varied patient response to mainstay chemotherapeutics, biological...

article

Statin-associated myopathy and the quest for biomarkers: can we effectively predict statin-associated muscle symptoms?

Danina M. Muntean, Paul D. Thompson, Alberico L. Catapano, Mariusz Stasiolek, more

Drug Discovery Today > 2017 > 22 > 1 > 85-96

Over the past three decades, statins have become the cornerstone of prevention and treatment of atherosclerotic cardiovascular and metabolic diseases. Albeit generally well tolerated, these drugs can elicit a variety of muscle-associated symptoms that represent the most important reason for treatment discontinuation. Statin-associated myopathy has been systematically underestimated by randomized controlled...

article

Exploiting receptor tyrosine kinase co-activation for cancer therapy

Aik-Choon Tan, Simon Vyse, Paul H. Huang

Drug Discovery Today > 2017 > 22 > 1 > 72-84

Studies over the past decade have shown that many cancers have evolved receptor tyrosine kinase (RTK) co-activation as a mechanism to drive tumour progression and limit the lethal effects of therapy. This review summarises the general principles of RTK co-activation and discusses approaches to exploit this phenomenon in cancer therapy and drug discovery. Computational strategies to predict kinase...

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Targeting the endocannabinoid system: future therapeutic strategies

Oier Aizpurua-Olaizola, Izaskun Elezgarai, Irantzu Rico-Barrio, Iratxe Zarandona, more

Drug Discovery Today > 2017 > 22 > 1 > 105-110

The endocannabinoid system (ECS) is involved in many physiological regulation pathways in the human body, which makes this system the target of many drugs and therapies. In this review, we highlight the latest studies regarding the role of the ECS and the drugs that target it, with a particular focus on the basis for the discovery of new cannabinoid-based drugs. In addition, we propose some key steps,...

article

Macrophage polarization in response to epigenetic modifiers during infection and inflammation

Urmi Patel, Sheeja Rajasingh, Saheli Samanta, Thuy Cao, more

Drug Discovery Today > 2017 > 22 > 1 > 186-193

Macrophages are a heterogeneous population of phagocytic cells present in all tissues. Recently, several drugs that target the epigenetic machinery have emerged as attractive molecules for treating infection and inflammation by modulating macrophages. Treatment of lipopolysaccharide (LPS)-challenged macrophages with epigenetic modifiers leads to phenotype switching. This could provide stimulatory/destructive...

article

Defining drug response for stratified medicine

Mike Lonergan, Stephen J. Senn, Christine McNamee, Ann K. Daly, more

Drug Discovery Today > 2017 > 22 > 1 > 173-179

The premise for stratified medicine is that drug efficacy, drug safety, or both, vary between groups of patients, and biomarkers can be used to facilitate more targeted prescribing, with the aim of improving the benefit:risk ratio of treatment. However, many factors can contribute to the variability in response to drug treatment. Inadequate characterisation of the nature and degree of variability...

article

Recombinant high-density lipoproteins and their use in cardiovascular diseases

Yi-ni Cao, Lu Xu, Ying-chun Han, Yu-nan Wang, more

Drug Discovery Today > 2017 > 22 > 1 > 180-185

The unique anti-atherosclerosis abilities and other cardioprotective properties make high-density lipoprotein (HDL) a promising solution in treating cardiovascular diseases. A number of studies showed that HDL-based therapy was well tolerated and has great potential in the future. Among all these new agents, the most studied ones including recombinant HDL, recombinant human apolipoproteins, apolipoprotein...

article

Electrophysiological approaches to unravel the neurobiological basis of appetite and satiety: use of the multielectrode array as a screening strategy

Hamdy Shaban, Rory O’Connor, Saak V. Ovsepian, Timothy G. Dinan, more

Drug Discovery Today > 2017 > 22 > 1 > 31-42

Hypothalamic neural circuits are recognised as primary sites of the neuromodulator effect of homeostatic food intake, whereas changes in ventral tegmental area (VTA), hippocampus and amygdala have been implicated in the hedonic, cognitive and emotional aspects of eating. Here, we discuss synaptic transmission and plasticity within brain circuits governing appetite and food intake behaviour, focusing...

article

The many roles of molecular complexity in drug discovery

Oscar Méndez-Lucio, José L. Medina-Franco

Drug Discovery Today > 2017 > 22 > 1 > 120-126

Molecular complexity is becoming a crucial concept in drug discovery. It has been associated with target selectivity, success in progressing into clinical development and compound safety, among other factors. Multiple metrics have been developed to quantify molecular complexity and explore complexity–property relationships. However, there is no general agreement regarding how to measure this molecular...

article

Pharmaceutical and biomaterial engineering via electrohydrodynamic atomization technologies

Prina Mehta, Rita Haj-Ahmad, Manoochehr Rasekh, Muhammad S. Arshad, more

Drug Discovery Today > 2017 > 22 > 1 > 157-165

Complex micro- and nano-structures enable crucial developments in the healthcare remit (e.g., pharmaceutical and biomaterial sciences). In recent times, several technologies have been developed and explored to address key healthcare challenges (e.g., advanced chemotherapy, biomedical diagnostics and tissue regeneration). Electrohydrodynamic atomization (EHDA) technologies are rapidly emerging as promising...

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Contents page 2

Drug Discovery Today > 2017 > 22 > 1 > ii

article

In vivo fate of lipid-based nanoparticles

Jianping Qi, Jie Zhuang, Yi Lu, Xiaochun Dong, more

Drug Discovery Today > 2017 > 22 > 1 > 166-172

The in vivo fate of lipid-based nanoparticles (LBNs) is essentially determined by the properties of their lipid compositions. LBNs are rapidly degraded via lipolysis wherever lipases are abundant, especially in the gastrointestinal tract. LBNs that survive lipolysis can be translocated through the circulation to reach terminal organs or tissues. Lipid composition, particle size, and surface decoration,...

article

Am I or am I not proarrhythmic? Comparison of various classifications of drug TdP propensity

Barbara Wiśniowska, Sebastian Polak

Drug Discovery Today > 2017 > 22 > 1 > 10-16

This review aims to present and compare various Torsade de pointes propensity classification schemes of drugs that are publicly available from many scientific sources. We have also tracked and listed the compounds that were differently categorized. Additionally, we would like to draw attention to the need for establishing a general, standardized classification of a drug's proarrhythmic propensity...

INFONA - science communication portal

Drug Discovery Today

The publishing and patenting strategies of successful university spinoffs in the biopharmaceutical industry

Structural features of subtype-selective EP receptor modulators

The challenges of modulating the ‘rest and digest’ system: acetylcholine receptors as drug targets

Predicting toxicities in humans by nonclinical safety testing: an update with particular reference to anticancer compounds

Cyclooxygenase-2 in glioblastoma multiforme

Contents page 1

Recent advances in therapeutic recruitment of mammalian RNAi and bacterial CRISPR-Cas DNA interference pathways as emerging antiviral strategies

Chasing the personalized medicine dream through biomarker validation in colorectal cancer

Statin-associated myopathy and the quest for biomarkers: can we effectively predict statin-associated muscle symptoms?

Exploiting receptor tyrosine kinase co-activation for cancer therapy

Targeting the endocannabinoid system: future therapeutic strategies

Macrophage polarization in response to epigenetic modifiers during infection and inflammation

Defining drug response for stratified medicine

Recombinant high-density lipoproteins and their use in cardiovascular diseases

Electrophysiological approaches to unravel the neurobiological basis of appetite and satiety: use of the multielectrode array as a screening strategy

The many roles of molecular complexity in drug discovery

Pharmaceutical and biomaterial engineering via electrohydrodynamic atomization technologies

Contents page 2

In vivo fate of lipid-based nanoparticles

Am I or am I not proarrhythmic? Comparison of various classifications of drug TdP propensity

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