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Allosteric adenosine receptor modulator alleviates pain Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-09-24
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A novel single-agent antibiotic Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-09-23
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Emerging therapeutic opportunities for integrin inhibitors Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-09-17 R. J. Slack, S. J. F. Macdonald, J. A. Roper, R. G. Jenkins, R. J. D. Hatley
Integrins are cell adhesion and signalling proteins crucial to a wide range of biological functions. Effective marketed treatments have successfully targeted integrins αIIbβ3, α4β7/α4β1 and αLβ2 for cardiovascular diseases, inflammatory bowel disease/multiple sclerosis and dry eye disease, respectively. Yet, clinical development of others, notably within the RGD-binding subfamily of αv integrins, including
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Advances in TRP channel drug discovery: from target validation to clinical studies Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-09-15 Ari-Pekka Koivisto, Maria G. Belvisi, Rachelle Gaudet, Arpad Szallasi
Transient receptor potential (TRP) channels are multifunctional signalling molecules with many roles in sensory perception and cellular physiology. Therefore, it is not surprising that TRP channels have been implicated in numerous diseases, including hereditary disorders caused by defects in genes encoding TRP channels (TRP channelopathies). Most TRP channels are located at the cell surface, which
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What does AlphaFold mean for drug discovery? Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-09-14
AlphaFold and RoseTTAFold have delivered a revolutionary advance for protein structure predictions, but the implications for drug discovery are more incremental. For now.
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Upcoming market catalysts in Q4 2021 Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-09-13
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The Nobel Prize-winning path from oxygen sensing research to new drugs Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-09-10
William Kaelin, a professor at the Dana-Farber Cancer Institute, discusses how his research into the mechanisms of oxygen sensing paved the way for two new drugs, and how to improve the calibre of preclinical research.
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PIKfyve: a lipid kinase target for COVID-19, cancer and neurodegenerative disorders Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-09-09
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Pfizer buys Trillium and its CD47 candidates for US$2.3 billion Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-09-06
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Monoclonal antibodies show promise in phase I malaria trial Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-09-06
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FDA releases proposed terms of PDUFA VII agreement Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-09-06
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Pfizer’s COVID-19 vaccine secures first full FDA approval Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-09-06
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Putting a PIN in pancreatic cancer Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-09-03
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Overcoming ICB resistance in lung cancer Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-09-02
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Nonhormonal target for endometriosis Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-09-02
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Prime editing rescues mice from genetic disorders Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-09-02
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Crossing the blood–brain barrier Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-09-02
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Promoting APRIL interaction to control atherosclerosis Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-09-02
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Evolution of the market for mRNA technology Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-09-02
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Author Correction: Trends in kinase drug discovery: targets, indications and inhibitor design. Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-09-02 Misty M Attwood,Doriano Fabbro,Aleksandr V Sokolov,Stefan Knapp,Helgi B Schiöth
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Tres Cantos Open Lab: celebrating a decade of innovation in collaboration to combat endemic infectious diseases Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-09-01 Felix Calderón, Lluis Ballell, David Barros, Graeme Bilbe, Nicholas Cammack, Raquel Gabarró, Audra Halsey, Penny M. Heaton, Gagandeep Kang, Valerie Mizrahi, Mike E. Strange, Pauline M. Williams, Elizabeth A. Winzeler, Alan H. Fairlamb
Tres Cantos Open Lab is a collaborative initiative that integrates teams from academia and GlaxoSmithKline to enable rapid testing of innovative therapeutic hypotheses for endemic infectious diseases. Here, we provide an overview of the key scientific achievements in its first decade.
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Author Correction: PI3K inhibitors are finally coming of age. Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-09-01 Bart Vanhaesebroeck,Matthew W D Perry,Jennifer R Brown,Fabrice André,Klaus Okkenhaug
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Hitting SEND on mRNA delivery Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-08-27
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mRNA vaccines for infectious diseases: principles, delivery and clinical translation Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-08-25 Namit Chaudhary, Drew Weissman, Kathryn A. Whitehead
Over the past several decades, messenger RNA (mRNA) vaccines have progressed from a scepticism-inducing idea to clinical reality. In 2020, the COVID-19 pandemic catalysed the most rapid vaccine development in history, with mRNA vaccines at the forefront of those efforts. Although it is now clear that mRNA vaccines can rapidly and safely protect patients from infectious disease, additional research
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Noncoding RNA mimic treats metabolic disorder Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-08-25 Crunkhorn, Sarah
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Atopic dermatitis: an expanding therapeutic pipeline for a complex disease Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-08-20 Bieber, Thomas
Atopic dermatitis (AD) is a common chronic inflammatory skin disease with a complex pathophysiology that underlies a wide spectrum of clinical phenotypes. AD remains challenging to treat owing to the limited response to available therapies. However, recent advances in understanding of disease mechanisms have led to the discovery of novel potential therapeutic targets and drug candidates. In addition
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What’s next for an immuno-oncology powerhouse? Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-08-13 Mullard, Asher
Dean Li, the recently appointed President of Merck Research Laboratories, discusses his immuno-oncology ambitions, emerging antiviral opportunities and the changing pace of technological cycle times.
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Engineering islets from stem cells for advanced therapies of diabetes Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-08-10 Siehler, Johanna, Blöchinger, Anna Karolina, Meier, Matthias, Lickert, Heiko
Diabetes mellitus is a metabolic disorder that affects more than 460 million people worldwide. Type 1 diabetes (T1D) is caused by autoimmune destruction of β-cells, whereas type 2 diabetes (T2D) is caused by a hostile metabolic environment that leads to β-cell exhaustion and dysfunction. Currently, first-line medications treat the symptomatic insulin resistance and hyperglycaemia, but do not prevent
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FDA approves first all-oral sleeping sickness drug Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-08-06 Mullard, Asher
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FDA approves AstraZeneca’s anifrolumab for lupus Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-08-06 Mullard, Asher
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Failure of Seres’s phase II ulcerative colitis programme renews microbiome concerns Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-08-06 Mullard, Asher
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T cell-regulating therapies for autoimmune diseases take FDA rejection in stride Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-08-06 Cully, Megan
Despite a regulatory setback for Provention Bio’s diabetes prevention candidate teplizumab, hopes remain high for T cell-regulating therapies in autoimmune indications including multiple sclerosis, systemic lupus erythematosus and coeliac disease.
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Antibiotics switch to anticancer target Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-08-05 Kingwell, Katie
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Trends in kinase drug discovery: targets, indications and inhibitor design Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-08-05 Attwood, Misty M., Fabbro, Doriano, Sokolov, Aleksandr V., Knapp, Stefan, Schiöth, Helgi B.
The FDA approval of imatinib in 2001 was a breakthrough in molecularly targeted cancer therapy and heralded the emergence of kinase inhibitors as a key drug class in the oncology area and beyond. Twenty years on, this article analyses the landscape of approved and investigational therapies that target kinases and trends within it, including the most popular targets of kinase inhibitors and their expanding
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UPR activator eliminates breast tumours Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-08-03 Crunkhorn, Sarah
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Preventing hearing loss in neurofibromatosis Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-08-03 Crunkhorn, Sarah
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Switch system fine tunes protein translation Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-08-03 Crunkhorn, Sarah
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Understanding NMDA-mediated ketamine activity Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-08-03 Crunkhorn, Sarah
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Kinase inhibitor combination combats liver cancer Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-08-03 Crunkhorn, Sarah
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Therapeutic genome editing: regulatory horizons Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-07-29 Hines, Philip A., Agricola, Eleonora, Llinares Garcia, Jordi, O’Dwyer, Laurence , Herold, Ralf
An increasing number of genome-editing technologies are being developed. Here, we highlight some of the key issues for future therapies using these technologies from a regulatory perspective.
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Targeting viruses in their phase Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-07-27 Strzyz, Paulina
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Broadly neutralizing anti-coronavirus antibodies Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-07-27 Megan Cully
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Immune-related toxicities of checkpoint inhibitors: mechanisms and mitigation strategies Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-07-27 Ryan J. Sullivan, Jeffrey S. Weber
The immune-related adverse events associated with treatment with immune checkpoint inhibitors result in significant morbidity for patients as well as considerable cost to the health-care system, and can limit the use of these beneficial drugs. Understanding the mechanisms of these side effects and how they can be separated from the antitumour effects of immune checkpoint inhibitors, as well as identifying
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The PROTACtable genome Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-07-20 Melanie Schneider, Chris J. Radoux, Andrew Hercules, David Ochoa, Ian Dunham, Lykourgos-Panagiotis Zalmas, Gerhard Hessler, Sven Ruf, Veerabahu Shanmugasundaram, Michael M. Hann, Pam J. Thomas, Markus A. Queisser, Andrew B. Benowitz, Kris Brown, Andrew R. Leach
Proteolysis-targeting chimeras (PROTACs) are an emerging drug modality that may offer new opportunities to circumvent some of the limitations associated with traditional small-molecule therapeutics. By analogy with the concept of the ‘druggable genome’, the question arises as to which potential drug targets might PROTAC-mediated protein degradation be most applicable. Here, we present a systematic
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FDA new drug approvals in Q2 2021 Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-07-15 Lisa Urquhart
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Small activating RNAs lead the charge to turn up gene expression Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-07-15 Katie Kingwell
As small activating RNAs gear up to enter phase II testing, other noncoding RNAs that upregulate gene expression are also progressing towards the clinic. But it’s early days for a complex field.
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The glomerular filtration barrier: a structural target for novel kidney therapies Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-07-14 Ilse S. Daehn, Jeremy S. Duffield
Loss of normal kidney function affects more than 10% of the population and contributes to morbidity and mortality. Kidney diseases are currently treated with immunosuppressive agents, antihypertensives and diuretics with partial but limited success. Most kidney disease is characterized by breakdown of the glomerular filtration barrier (GFB). Specialized podocyte cells maintain the GFB, and structure–function
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Can a platform of platform companies open up more opportunities? Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-07-14 Asher Mullard
Luisa Salter-Cid, the Chief Scientific Officer of Pioneering Medicines, will build a portfolio of programmes by tapping technologies on offer at dozens of companies founded by venture capital firm Flagship.
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eEF2K: an atypical kinase target for cancer Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-07-13 Louisa Temme, Christopher R. M. Asquith
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Ligand binding at the protein–lipid interface: strategic considerations for drug design Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-07-13 Jian Payandeh, Matthew Volgraf
Many drug targets are embedded within the phospholipid bilayer of cellular membranes, including G protein-coupled receptors, ion channels, transporters and membrane-bound enzymes. Increasing evidence from biophysical and structural studies suggests that many small-molecule drugs commonly associate with these targets at binding sites at the protein–phospholipid interface. Without a direct path from
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A shared target for stroke subtypes Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-07-08 M. Teresa Villanueva
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Alzheimer antibody rush begins, as efficacy concerns remain Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-07-08 Asher Mullard
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Docking downstream to treat myasthenia Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-07-08 Katie Kingwell
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Immuno-oncology target TIGIT attracts a new contender Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-07-08 Asher Mullard
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Sensitizing glioblastoma to radiotherapy Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-07-07 Sarah Crunkhorn
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Live malaria vaccine shows promise Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-07-07
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Yeast probiotics treat IBD Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-07-07 Sarah Crunkhorn
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Reactivating PTEN promotes antitumour immunity Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-07-07 Sarah Crunkhorn
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Implications of sex-related differences in central nervous system disorders for drug research and development Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-07-05 Florence Butlen-Ducuing, Ewa Balkowiec-Iskra, Christina Dalla, David A. Slattery, Maria Teresa Ferretti, Nikolaos Kokras, Pavel Balabanov, Corinne De Vries, Simona Mellino, Antonella Santuccione Chadha
Research on sex differences in central nervous system disorders has developed substantially in recent years. Here, we discuss selected examples and the implications for drug development.
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Targeting oxidative stress in disease: promise and limitations of antioxidant therapy Nat. Rev. Drug. Disc. (IF 84.694) Pub Date : 2021-06-30 Henry Jay Forman, Hongqiao Zhang
Oxidative stress is a component of many diseases, including atherosclerosis, chronic obstructive pulmonary disease, Alzheimer disease and cancer. Although numerous small molecules evaluated as antioxidants have exhibited therapeutic potential in preclinical studies, clinical trial results have been disappointing. A greater understanding of the mechanisms through which antioxidants act and where and
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