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Designing the ideal opioid

Brigitte L. Kieffer
2016 Nature  
PZM21 reduced pain responses mediated by the central nervous DRUG DISCOVERY Designing the ideal opioid The development of a drug that mimics the pain-relieving activity of opioid compounds, but has  ...  drug discovery 9 .  ... 
doi:10.1038/nature19424 pmid:27533037 fatcat:qhuunuh7rjhgflullhochsbxyq

Drug Discovery and Development [chapter]

Benjamin E. Blass
2015 Basic Principles of Drug Discovery and Development  
doi:10.1016/b978-0-12-411508-8.00001-3 fatcat:wibaxowuuvg57aj7n5j2g6tdxi

Drug metabolism in drug discovery and development

Zhoupeng Zhang, Wei Tang
2018 Acta Pharmaceutica Sinica B  
Drug metabolism as a discipline plays an important role in drug discovery and development and the effects of drug metabolism on pharmacokinetics (PK), pharmacodynamics (PD), and safety should be carefully  ...  This communication provides an overview of common strategies in the area of drug metabolism for improving PK/PD and safety profiles of drug candidates; these include, but are not limited to, collaboration  ...  Acknowledgements The authors would like to thank Charles Thompson, Mark Cancilla and Christine Fandozzi for critical reading of the manuscript and invaluable suggestions.  ... 
doi:10.1016/j.apsb.2018.04.003 pmid:30245961 pmcid:PMC6146880 fatcat:krvfntehnzebvhkbheradu4qq4

The Process of Drug Discovery [chapter]

Terry P. Kenakin
2009 A Pharmacology Primer  
-André Gide The real voyage of discovery consists not in seeking new landscapes but in having new eyes.  ...  One doesn't discover new lands without consenting to lose sight of the shore for a very long time.  ...  Another approach to the discovery of drugs is "rational design."  ... 
doi:10.1016/b978-0-12-374585-9.00008-6 fatcat:wfbool2wfbdungor7n2qbr7ng4

Applications of Machine Learning in Drug Discovery I: Target Discovery and Small Molecule Drug Design [chapter]

John W. Cassidy
2020 Artificial Intelligence in Oncology Drug Discovery and Development  
In this first part of our analysis of the application of ML to the drug discovery and development process, we discuss recent advances in the use of computational techniques in drug target discovery and  ...  In this chapter, we will provide a basic primer to ML before discussing methods for, and examples of, the use of ML-based techniques in target identification and structure-based drug design.  ...  of uses of ML in the drug discovery process to the clinical arena.  ... 
doi:10.5772/intechopen.93159 fatcat:z5xuzsnga5ggfnp5sofk6hyodi

Natural Products Drug Discovery [chapter]

Giovanni Appendino, Gabriele Fontana, Federica Pollastro
2010 Comprehensive Natural Products II  
where ligands are designed ex novo or assembled by fragments and where emphasis is apparently placed on design rather than on discovery.  ...  the costs of drug discovery or fill pharma pipelines with new drugs anytime soon. '' 194 Natural Products Drug Discovery Natural Products Drug Discovery Natural Products Drug Discovery  ... 
doi:10.1016/b978-008045382-8.00064-2 fatcat:7fo4jl5uhrhqnpagit3awfj4fq

Current challenges in peptide-based drug discovery

Laszlo Otvos, John D. Wade
2014 Frontiers in Chemistry  
design.  ...  and Davis, 2005) , and more recently to simultaneous intestinal drug absorption and blood-brain barrier penetration of endomorphine-1, an opioid tetrapeptide (Varamini et al., 2012) .  ...  Conflict of Interest Statement: The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest  ... 
doi:10.3389/fchem.2014.00062 pmid:25152873 pmcid:PMC4126357 fatcat:cyghkkhmbra7nfnjr2vk6ulhlq

The 6th Drug Discovery for Neurodegeneration Conference: An Intensive Course on Translating Research into Drugs

Laura K Chico, Daniel Martin Watterson
2012 Expert Opinion on Drug Discovery  
Small molecule drug discovery remains a chemo-centric paradigm with structural design and synthesis at the core of this process.  ...  However, chemical tool compounds designed for in vivo use can be useful starting points for the later stage drug discovery lead compound attainment.  ... 
doi:10.1517/17460441.2012.733692 pmid:23092534 fatcat:iqa2udp2jvgzdbdabmzslogqje

Mitigating risk in academic preclinical drug discovery

Jayme L. Dahlin, James Inglese, Michael A. Walters
2015 Nature reviews. Drug discovery  
In this article, we discuss strategies to mitigate risks in several key aspects of preclinical drug discovery at academic drug discovery centres, including organization, target selection, assay design,  ...  | The number of academic drug discovery centres has grown considerably in recent years, providing new opportunities to couple the curiosity-driven research culture in academia with rigorous preclinical  ...  Nelson for critical reading of the manuscript and the many other important contributions in the drug discovery community that, regrettably, could not be cited owing to space constraints.  ... 
doi:10.1038/nrd4578 pmid:25829283 pmcid:PMC6002840 fatcat:sfx4kibn55fedhckaemxvphl3u

Novel 1,2,4-Oxadiazole Derivatives in Drug Discovery

Karol Biernacki, Mateusz Daśko, Olga Ciupak, Konrad Kubiński, Janusz Rachon, Sebastian Demkowicz
2020 Pharmaceuticals  
After a century since the1,2,4-oxadiazole have been discovered, the uncommon potential attracted medicinal chemists'attention, leading to the discovery of a few presently accessible drugs containing 1,2,4  ...  novel drug development.  ...  This work is a continuation of the considerable research in the discovery of a potent drug for primary insomnia treatment.  ... 
doi:10.3390/ph13060111 pmid:32485996 pmcid:PMC7345688 fatcat:clytlhhbdfeafn62622zgn6lpe

Developing selectively nonselective drugs for treating CNS disorders

John A. Gray, Bryan L. Roth
2006 Drug Discovery Today : Therapeutic Strategies  
As an example of designed conjugated ligands, opioid ligands have been conjugated to form homodimeric ligands with increased potency at opioid receptors due to enhanced interaction with dimerized receptors  ...  approach is not ideal for developing drugs for complex CNS disorders [1] .  ... 
doi:10.1016/j.ddstr.2006.11.009 fatcat:4owagoolqfgzdls4krzdjunoya

Significance of the human genome sequence to drug discovery

O Grenet
2001 The Pharmacogenomics Journal  
Significance of the human genome sequence to drug discovery O Grenet NOVARTIS Pharma AG, Preclinical Safety, Basel, Switzerland Towards the end of their research and development efforts, pharmaceutical  ...  Such genomewide expression profiling at the mRNA level may designate new genes involved in a pathway, potential drug targets or expression markers that can be used in a predictive or diagnostic manner.  ... 
doi:10.1038/sj.tpj.6500010 fatcat:dssiyap4zfaynaq67hdk7b257m

Quantitative metrics for drug–target ligandability

Sinisa Vukovic, David J. Huggins
2018 Drug Discovery Today  
The metric is evaluated for a standard set of well-studied drug targets -some traditionally considered to be ligandable and some regarded as difficult.  ...  the human body.  ...  A continuous metric, such as the best-known affinity [13] , is more natural and more useful to inform decision making in drug design.  ... 
doi:10.1016/j.drudis.2018.02.015 pmid:29522887 fatcat:spjkacd4lbfhnine6kv3vtyggu

Artificial Intelligence in Drug Discovery: Applications and Techniques [article]

Jianyuan Deng, Zhibo Yang, Iwao Ojima, Dimitris Samaras, Fusheng Wang
2021 arXiv   pre-print
Artificial intelligence (AI) has been transforming the practice of drug discovery in the past decade.  ...  Various AI techniques have been used in a wide range of applications, such as virtual screening and drug design.  ...  The neural networks templates are from Visuals by ( Supporting Information Available AI Drug Discovery  ... 
arXiv:2106.05386v4 fatcat:w2at5y5jyffrxiejsupmwiimhq

Computational Biology and Drug Discovery: From Single-Target to Network Drugs

Alberto Ambesi-Impiombato, Diego Bernardo
2006 Current Bioinformatics  
Computational biology and bioinformatics have the potential not only to speed up the drug discovery process, thus reducing the costs, but also to change the way drugs are designed.  ...  The drug discovery process is complex, time consuming and expensive, and includes preclinical and clinical phases.  ...  Computational biology and bioinformatics have the potential not only of speeding up the drug discovery process thus reducing the costs, but also of changing the way drugs are designed.  ... 
doi:10.2174/157489306775330598 fatcat:d4xf6wdms5cwhd3long3jie2ba
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