Asthma: Alternative route to airway relaxation
Nature Reviews Drug Discovery 17, 241 (2018).
doi:10.1038/nrd.2018.37
Author: Sarah Crunkhorn
Promoting airway smooth muscle cell (ASMC) relaxation is an established therapeutic strategy for alleviating pulmonary resistance in asthma. However, current approaches, which involve the inhalation of β2-adrenoceptor agonists, do not adequately control symptoms in all patients and are associated with side effects. Writing (Source: Nature Reviews Drug Discovery)
Source: Nature Reviews Drug Discovery - March 16, 2018 Category: Drugs & Pharmacology Authors: Sarah Crunkhorn Tags: Research Highlight Source Type: research
Antibacterial drugs: Discovering antibiotics through soil metagenomics
Nature Reviews Drug Discovery 17, 240 (2018).
doi:10.1038/nrd.2018.36
Author: Katharine H. Wrighton
The identification of bacterial natural products with antimicrobial properties has been hampered by the fact that many bacteria cannot be cultured in the laboratory, and those that can do not produce all of their natural products in this setting. Hover et al. have devised a (Source: Nature Reviews Drug Discovery)
Source: Nature Reviews Drug Discovery - March 16, 2018 Category: Drugs & Pharmacology Authors: Katharine H. Wrighton Tags: Research Highlight Source Type: research
Cancer: Tipping the splicing balance to kill cancer cells
Nature Reviews Drug Discovery 17, 239 (2018).
doi:10.1038/nrd.2018.38
Author: Megan Cully
Mutations in genes encoding splicing factors are commonly found in samples from patients with several haematological cancers, as well as some solid tumours. A new paper in Nature Medicine describes a novel, orally available splicing modulator that preferentially kills cancer cells with mutations in (Source: Nature Reviews Drug Discovery)
Source: Nature Reviews Drug Discovery - March 16, 2018 Category: Drugs & Pharmacology Authors: Megan Cully Tags: Research Highlight Source Type: research
Vaccines take a shot at antimicrobial resistance
Nature Reviews Drug Discovery 17, 229 (2018).
doi:10.1038/nrd.2018.8
Author: Katie Kingwell
Economic and policy issues rein in industry enthusiasm for vaccines as an answer to drug-resistant bugs. (Source: Nature Reviews Drug Discovery)
Source: Nature Reviews Drug Discovery - March 9, 2018 Category: Drugs & Pharmacology Authors: Katie Kingwell Tags: News and Analysis Source Type: research
Tissue-agnostic cancer drug pipeline grows, despite doubts
Nature Reviews Drug Discovery 17, 227 (2018).
doi:10.1038/nrd.2018.6
Author: Ken Garber
The FDA could soon approve the first drug developed explicitly for a tissue-agnostic cancer indication, but biological complexity may limit this approach. (Source: Nature Reviews Drug Discovery)
Source: Nature Reviews Drug Discovery - March 9, 2018 Category: Drugs & Pharmacology Authors: Ken Garber Tags: News and Analysis Source Type: research
Cancer: Targeting the ubiquitin pathway
Nature Reviews Drug Discovery 17, 166 (2018).
doi:10.1038/nrd.2018.33
Author: Sarah Crunkhorn
Aberrations in the ubiquitin–proteasome system — which maintains cellular protein homeostasis — are implicated in tumour development and progression. Here, Hyer et al. report the identification of TAK-243, a first-in-class inhibitor of the ubiquitin-activating enzyme. In vitro, TAK-243 induced defective protein turnover and (Source: Nature Reviews Drug Discovery)
Source: Nature Reviews Drug Discovery - February 28, 2018 Category: Drugs & Pharmacology Authors: Sarah Crunkhorn Tags: Research Highlight Source Type: research
Alzheimer disease: Identification of blood-based biomarkers
Nature Reviews Drug Discovery 17, 166 (2018).
doi:10.1038/nrd.2018.32
Author: Sarah Crunkhorn
There is a significant need for a minimally invasive, cost-effective and reliable method to diagnose early-stage Alzheimer disease. Building on previous work, Nakamura et al. demonstrate the use of immunoprecipitation coupled with mass spectrometry to measure plasma amyloid-β (Aβ) biomarkers. Using two independent data (Source: Nature Reviews Drug Discovery)
Source: Nature Reviews Drug Discovery - February 28, 2018 Category: Drugs & Pharmacology Authors: Sarah Crunkhorn Tags: Research Highlight Source Type: research
Antibacterials: Synthetic peptides eradicate resistant infections
Nature Reviews Drug Discovery 17, 166 (2018).
doi:10.1038/nrd.2018.31
Author: Sarah Crunkhorn
Synthetic peptides based on naturally occurring antimicrobial peptides (AMPs) represent promising antibacterial agents. Now, de Breij and colleagues have synthesized novel peptides with improved antimicrobial and antibiofilm activities (SAAPs), based on a principle human AMP, LL-37. The most potent of these, SAAP-148, was effective against (Source: Nature Reviews Drug Discovery)
Source: Nature Reviews Drug Discovery - February 28, 2018 Category: Drugs & Pharmacology Authors: Sarah Crunkhorn Tags: Research Highlight Source Type: research
Cardiovascular disease: Inhalation therapy for heart failure
Nature Reviews Drug Discovery 17, 166 (2018).
doi:10.1038/nrd.2018.30
Author: Sarah Crunkhorn
Drug delivery via inhalation is commonly used for respiratory disorders, but its potential for therapeutically targeting the heart has not been explored. Here, Miragoli et al. demonstrate in mice that following inhalation, their previously reported small, biocompatible and biodegradable negatively charged calcium phosphate nanoparticles (Source: Nature Reviews Drug Discovery)
Source: Nature Reviews Drug Discovery - February 28, 2018 Category: Drugs & Pharmacology Authors: Sarah Crunkhorn Tags: Research Highlight Source Type: research
Immunotherapy: Direct shot
Nature Reviews Drug Discovery 17, 165 (2018).
doi:10.1038/nrd.2018.29
Author: Lucy Bird
Harnessing the immune system to fight tumours is providing real hope in treating patients with cancer. Yet several immunotherapy approaches are limited by the need for prior knowledge of tumour antigens or large doses of expensive antibodies. In a recent study published in Science Translational (Source: Nature Reviews Drug Discovery)
Source: Nature Reviews Drug Discovery - February 28, 2018 Category: Drugs & Pharmacology Authors: Lucy Bird Tags: Research Highlight Source Type: research
Fiona Marshall
Nature Reviews Drug Discovery 17, 158 (2018).
doi:10.1038/nrd.2018.25
Fiona Marshall co-founded Heptares in 2007 to apply structure-based drug design to G protein-coupled receptor (GPCR) targets, a large class of membrane-bound signalling receptors with diverse and critical roles across disease areas. Although around 35% of approved drugs act on GPCR targets, the research community had only solved the structure of a single GPCR at the time the company launched. Heptares has since determined more than 200 GPCR–ligand structures for 20 different GPCRs, advanced 4 drug candidates into the clinic, and partnered w...
Source: Nature Reviews Drug Discovery - February 28, 2018 Category: Drugs & Pharmacology Tags: News and Analysis Source Type: research
Alnylam prepares to land first RNAi drug approval
Nature Reviews Drug Discovery 17, 156 (2018).
doi:10.1038/nrd.2018.20
Author: Chris Morrison
With Alnylam's rare disease drug candidate patisiran nearing the regulatory finish line, the RNA interference community is now turning its attention to next-generation delivery technology to solidify the future of the emerging modality. (Source: Nature Reviews Drug Discovery)
Source: Nature Reviews Drug Discovery - February 28, 2018 Category: Drugs & Pharmacology Authors: Chris Morrison Tags: News and Analysis Source Type: research
Impact of target interactions on small-molecule drug disposition: an overlooked area
Nature Reviews Drug Discovery 17, 299 (2018).
doi:10.1038/nrd.2018.26
Authors: Robert A. B. van Waterschoot, Neil J. Parrott, Andrés Olivares-Morales, Thierry Lavé, Malcolm Rowland & Dennis A. Smith
The selection of an appropriate drug target, as well as a solid understanding of drug pharmacokinetics and pharmacodynamics, are crucial for successful drug discovery. Although it is generally accepted that the free (unbound) concentration of a drug is the driving force for its pharmacological (Source: Nature Reviews Drug Discovery)
Source: Nature Reviews Drug Discovery - February 23, 2018 Category: Drugs & Pharmacology Authors: Robert A. B. van Waterschoot Neil J. Parrott Andr é s Olivares-Morales Thierry Lav é Malcolm Rowland Dennis A. Smith Tags: Correspondence Source Type: research
Cancer: Reset your circadian clock
Nature Reviews Drug Discovery 17, 166 (2018).
doi:10.1038/nrd.2018.24
Author: M. Teresa Villanueva
The circadian clock controls several physiological functions, such as metabolism, cell proliferation and inflammation. Now, writing in Nature, Sulli et al. report that pharmacological targeting of the circadian clock components REV-ERBα (also known as NR1D1) and REV-ERBβ (also known as NR1D2), which are (Source: Nature Reviews Drug Discovery)
Source: Nature Reviews Drug Discovery - February 16, 2018 Category: Drugs & Pharmacology Authors: M. Teresa Villanueva Tags: Research Highlight Source Type: research
Cancer: New path to improving immunotherapy
Nature Reviews Drug Discovery 17, 164 (2018).
doi:10.1038/nrd.2018.22
Author: Sarah Crunkhorn
Cancer patients with high levels of circulating myeloid-derived suppressor cells (MDSCs) have been found to respond poorly to checkpoint blockade. Accordingly, there is significant interest in therapeutically targeting these immunosuppressive innate immune cells. Writing in Cell, lead author Masoud Tavazoie and colleagues now report (Source: Nature Reviews Drug Discovery)
Source: Nature Reviews Drug Discovery - February 16, 2018 Category: Drugs & Pharmacology Authors: Sarah Crunkhorn Tags: Research Highlight Source Type: research
