| 1. |
- Apprato, Giulia, et al.
(författare)
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Exploring the chemical space of orally bioavailable PROTACs
- 2024
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Ingår i: Drug Discovery Today. - : Elsevier. - 1359-6446 .- 1878-5832. ; 29:4
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Forskningsöversikt (refereegranskat)abstract
- A principal challenge in the discovery of proteolysis targeting chimeras (PROTACs) as oral medications is their bioavailability. To facilitate drug design, it is therefore essential to identify the chemical space where orally bioavailable PROTACs are more likely to be situated. To this aim, we extracted structure-bioavailability insights from published data using traditional 2D descriptors, thereby shedding light on their potential and limitations as drug design tools. Subsequently, we describe cuttingedge experimental, computational and hybrid design strategies based on 3D descriptors, which show promise for enhancing the probability of discovering PROTACs with high oral bioavailability.
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| 2. |
- Arvidsson, Per I., et al.
(författare)
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Open for collaboration : an academic platform for drug discovery and development at SciLifeLab
- 2016
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Ingår i: Drug Discovery Today. - : Elsevier BV. - 1359-6446 .- 1878-5832. ; 21:10, s. 1690-1698
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Forskningsöversikt (refereegranskat)abstract
- The Science for Life Laboratory Drug Discovery and Development (SciLifeLab DDD) platform reaches out to Swedish academia with an industry-standard infrastructure for academic drug discovery, supported by earmarked funds from the Swedish government. In this review, we describe the build-up and operation of the platform, and reflect on our first two years of operation, with the ambition to share learnings and best practice with academic drug discovery centers globally. We also discuss how the Swedish Teacher Exemption Law, an internationally unique aspect of the innovation system, has shaped the operation. Furthermore, we address how this investment in infrastructure and expertise can be utilized to facilitate international collaboration between academia and industry in the best interest of those ultimately benefiting the most from translational pharmaceutical research - the patients.
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| 3. |
- Bersani, Francesco S, et al.
(författare)
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Telomerase activation as a possible mechanism of action for psychopharmacological interventions.
- 2015
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Ingår i: Drug Discovery Today. - : Elsevier BV. - 1878-5832 .- 1359-6446. ; 20:11, s. 1305-1309
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Forskningsöversikt (refereegranskat)abstract
- Originally studied in relation to aging and cancer research, telomerase is now also investigated in relation to psychiatric disorders and treatments. Based on emerging clinical and preclinical data, we hypothesise that telomerase activation could represent a novel element mediating the mechanism of action of certain psychopharmacological interventions (e.g. antidepressants, lithium and antipsychotics). The modulation of intracellular Wnt/β-catenin or PI3K/Akt signalling pathways, the interaction with BDNF and 5-HT, and the antioxidant properties could represent possible mechanisms by which the different types of psychiatric medications could modulate telomerase activity. The potential of telomerase in promoting cellular survival and/or function in the brain and in the periphery could, in turn, represent a neurobiological substrate through which the enzyme can mediate the therapeutic effect of such interventions.
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| 4. |
- Bignami, Francesca, et al.
(författare)
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Potential effects of increased openness in pharma : the original knowledge behind new drugs
- 2019
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Ingår i: Drug Discovery Today. - : Elsevier BV. - 1359-6446 .- 1878-5832.
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Tidskriftsartikel (refereegranskat)abstract
- This study seeks to determine potential changes in the degree of openness in pharmaceutical R&D by investigating where the knowledge behind new molecular entities (NMEs) comes from in terms of type of organization, geography and time. We find that the organizations granted NMEs increasingly rely on external knowledge sources but that these are increasingly shared among NME grantees. Universities are the most important indirect knowledge contributor and their relative importance has increased with time. NME grantees are increasingly relying on knowledge from different countries and the age of the knowledge sources confirms that recent NMEs are mostly follow-on drugs. This work provides evidence of the increasing openness of pharma to new knowledge sources as a means to improving the drug discovery and development process.
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| 5. |
- Bohlin, Lars, et al.
(författare)
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Podophyllotoxin derivatives : drug discovery and development
- 1996
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Ingår i: Drug Discovery Today. - : Elsevier. - 1359-6446 .- 1878-5832. ; 1:8, s. 343-351
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Forskningsöversikt (refereegranskat)abstract
- The exploration and exploitation of podophyllin formulations provide an example of how a plant extract with established ethnomedical use, but also causing toxicity, can provide a basis for new drug discovery and development. Applications and potential applications include the treatment of venereal warts, psoriasis, rheumatoid arthritis, malaria and Alzheimer's disease. This review addresses the history and pharmacological action of these natural products and outlines the preclinical development and clinical trials of drugs in the pipeline and with marketing approval.
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| 6. |
- Borrebaeck, Carl, et al.
(författare)
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Progress in miniaturisation of proteon arrays - a step closer to high-density nanoarrays
- 2007
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Ingår i: Drug Discovery Today. - : Elsevier BV. - 1878-5832 .- 1359-6446. ; 12:19-20, s. 813-819
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Forskningsöversikt (refereegranskat)abstract
- Protein microarrays is a technology with great promise for high-throughput proteomics. Designing high-performance protein microarrays for global proteome analysis has, however, turned out to be challenging. To this end, major efforts are under way to design novel array formats capable of harboring the tremendous range of probes required to target complex proteomes composed of more than 10 000 analytes. By adopting nanotechnology, the first generation of miniaturized nanoarrays has recently emerged, which opens up new avenues for global proteome analysis and disease proteomics. This review describes the progress and key issues in designing miniaturized protein arrays.
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| 7. |
- Bosma, M
(författare)
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Lipid homeostasis in exercise
- 2014
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Ingår i: Drug discovery today. - : Elsevier BV. - 1878-5832 .- 1359-6446. ; 19:7, s. 1019-1023
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Tidskriftsartikel (refereegranskat)
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| 8. |
- Bostrom, PA
(författare)
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All organ exercise for metabolic health
- 2014
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Ingår i: Drug discovery today. - : Elsevier BV. - 1878-5832 .- 1359-6446. ; 19:7, s. 997-998
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Tidskriftsartikel (övrigt vetenskapligt/konstnärligt)
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| 9. |
- Bruhn, Jan G., et al.
(författare)
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Molecular Pharmacognosy : an explanatory model
- 1997
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Ingår i: Drug Discovery Today. - : Elsevier. - 1359-6446 .- 1878-5832. ; 2:6, s. 243-246
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Forskningsöversikt (refereegranskat)abstract
- Increased interest in the study of natural products as potential drugs and rapidly changing research strategies are driving us to reassess the role of pharmacognosy in the wider context of pharmaceutical research. The authors propose a new definition and an explanatory model of modern pharmacognosy that can be used as a theoretical foundation for future development of this classical branch of the life sciences.
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| 10. |
- Cheung, Herman H., et al.
(författare)
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Monitor – Biology
- 2004
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Ingår i: Drug Discovery Today. - 1878-5832. ; 9:14, s. 621-622
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Tidskriftsartikel (refereegranskat)abstract
- The hottest developments in the fields of cancer research, neuroscience, genomics and proteomics, anti-virals and more, with a pick of the key research papers in these areas.
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