Results 1 to 10 of about 92,461 (139)
Targeting the ubiquitin system by fragment-based drug discovery [PDF]
Frontiers in Molecular Biosciences, 2022 The ubiquitin system contains a wealth of potential drug targets for many diseases and conditions, including neurodegenerative, immune, metabolic and developmental diseases, as well as multiple cancers.
Cassandra Kennedy +2 more
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Implications of Fragment-Based Drug Discovery in Tuberculosis and HIV [PDF]
Pharmaceuticals, 2022 Tuberculosis (TB) remains a global health problem and the emergence of HIV has further worsened it. Long chemotherapy and the emergence of drug-resistance strains of Mycobacterium tuberculosis as well as HIV has aggravated the problem.
Mohan Krishna Mallakuntla +3 more
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Fragment-based drug discovery: A graphical review [PDF]
Current Research in Pharmacology and Drug DiscoveryThree decades after its introduction, fragment-based drug (or lead) discovery (FBDD or FBLD) has become a mature and powerful strategy for generating novel leads, offering distinct advantages for challenging or previously “undruggable” targets where ...
Dana F. AlKharboush +3 more
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Reactivity of Covalent Fragments and Their Role in Fragment Based Drug Discovery [PDF]
Pharmaceuticals, 2022 Fragment based drug discovery has long been used for the identification of new ligands and interest in targeted covalent inhibitors has continued to grow in recent years, with high profile drugs such as osimertinib and sotorasib gaining FDA approval.
Kirsten McAulay +2 more
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Application of Fragment-Based Drug Discovery to Versatile Targets [PDF]
Frontiers in Molecular Biosciences, 2020 Fragment-based drug discovery (FBDD) is a powerful method to develop potent small-molecule compounds starting from fragments binding weakly to targets. As FBDD exhibits several advantages over high-throughput screening campaigns, it becomes an attractive
Qingxin Li
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Fragment-Based Lead Discovery Strategies in Antimicrobial Drug Discovery
Antibiotics, 2023 Fragment-based lead discovery (FBLD) is a powerful application for developing ligands as modulators of disease targets. This approach strategy involves identification of interactions between low-molecular weight compounds (100–300 Da) and their putative ...
Monika I. Konaklieva, Balbina J. Plotkin
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Perspectives on Applications of 19F-NMR in Fragment-Based Drug Discovery [PDF]
MoleculesFragment-based drug discovery is a powerful approach in drug discovery, applicable to a wide range of targets. This method enables the discovery of potent compounds that can modulate target functions, starting from fragment compounds that bind weakly to ...
Qingxin Li, CongBao Kang
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Fragment‐based drug discovery—the importance of high‐quality molecule libraries [PDF]
Molecular Oncology, 2022 Fragment‐based drug discovery (FBDD) is now established as a complementary approach to high‐throughput screening (HTS). Contrary to HTS, where large libraries of drug‐like molecules are screened, FBDD screens involve smaller and less complex molecules ...
Marta Bon +3 more
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Native Mass Spectrometry in Fragment-Based Drug Discovery
Molecules, 2016 The advent of native mass spectrometry (MS) in 1990 led to the development of new mass spectrometry instrumentation and methodologies for the analysis of noncovalent protein–ligand complexes.
Liliana Pedro, Ronald J. Quinn
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Introduction to the themed collection on fragment-based drug discovery. [PDF]
RSC Med Chem, 2022 Guest editors David Rees, Anna Hirsch and Daniel Erlanson introduce the RSC Medicinal Chemistry themed collection on fragment-based drug discovery.
Rees DC, Hirsch AKH, Erlanson DA.
europepmc +3 more sources