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Exploring the chemi...
Exploring the chemical space of orally bioavailable PROTACs
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- Apprato, Giulia (author)
- Univ Torino, Dept Mol Biotechnol & Hlth Sci, Piazza Nizza 44bis, I-10126 Turin, Italy.
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- Poongavanam, Vasanthanathan (author)
- Uppsala universitet,Organisk kemi
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- Jimenez, Diego Garcia (author)
- Univ Torino, Dept Mol Biotechnol & Hlth Sci, Piazza Nizza 44bis, I-10126 Turin, Italy.
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- Atilaw, Yoseph (author)
- Uppsala universitet,Organisk kemi
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- Erdélyi, Máté, 1975- (author)
- Uppsala universitet,Organisk kemi
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- Ermondi, Giuseppe (author)
- Univ Torino, Dept Mol Biotechnol & Hlth Sci, Piazza Nizza 44bis, I-10126 Turin, Italy.
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- Caron, Giulia (author)
- Univ Torino, Dept Mol Biotechnol & Hlth Sci, Piazza Nizza 44bis, I-10126 Turin, Italy.
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- Kihlberg, Jan (author)
- Uppsala universitet,Organisk kemi
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Univ Torino, Dept Mol Biotechnol & Hlth Sci, Piazza Nizza 44bis, I-10126 Turin, Italy Organisk kemi (creator_code:org_t)
- Elsevier, 2024
- 2024
- English.
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In: Drug Discovery Today. - : Elsevier. - 1359-6446 .- 1878-5832. ; 29:4
- Related links:
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https://uu.diva-port... (primary) (Raw object)
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Abstract
Subject headings
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- 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.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Farmaceutiska vetenskaper (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Pharmaceutical Sciences (hsv//eng)
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