Fragment‐based drug discovery—the importance of high‐quality molecule libraries
Sign Up to like & getrecommendations! Published in 2022 at "Molecular Oncology"
DOI: 10.1002/1878-0261.13277
Abstract: 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 which,… read more here.
Keywords: fragment based; drug discovery; based drug; discovery importance ... See more keywords
A 3D Osteosarcoma Model with Bone‐Mimicking Cues Reveals a Critical Role of Bone Mineral and Informs Drug Discovery
Sign Up to like & getrecommendations! Published in 2022 at "Advanced Healthcare Materials"
DOI: 10.1002/adhm.202200768
Abstract: Osteosarcoma (OS) is an aggressive bone cancer for which survival has not improved over three decades. While biomaterials have been widely used to engineer 3D soft‐tissue tumor models, the potential of engineering 3D biomaterials‐based OS… read more here.
Keywords: drug discovery; role; bone; model ... See more keywords
Drug re‐engineering and repurposing: A significant and rapid approach to tuberculosis drug discovery
Sign Up to like & getrecommendations! Published in 2022 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202200214
Abstract: The prevalence of tuberculosis (TB) remains the leading cause of death from a single infectious agent, ranking it above all other contagious diseases. The problem to tackle this disease seems to become even worse due… read more here.
Keywords: drug discovery; tuberculosis; classes compounds; drug development ... See more keywords
PROTACs: An Emerging Targeting Technique for Protein Degradation in Drug Discovery
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DOI: 10.1002/bies.201700247
Abstract: Proteolysis‐targeting chimeric molecules (PROTACs) represent an emerging technique that is receiving much attention for therapeutic intervention. The mechanism is based on the inhibition of protein function by hijacking a ubiquitin E3 ligase for protein degradation.… read more here.
Keywords: protein; technique; degradation; protein degradation ... See more keywords
Breaking the Fourth Wall: Modulating Quaternary Associations for Protein Regulation and Drug Discovery
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DOI: 10.1002/cbic.201800716
Abstract: Protein–protein interactions (PPIs) are an effective means to orchestrate intricate biological processes required to sustain life. Approximately 650 000 PPIs underlie the human interactome; thus underscoring its complexity and the manifold signaling outputs altered in response… read more here.
Keywords: ppi; fourth wall; drug; drug discovery ... See more keywords
Six Laws of Open Source Drug Discovery
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DOI: 10.1002/cmdc.201900565
Abstract: Six to swear by! Society needs effective and affordable medicines. We currently have at our disposal essentially one system to discover and develop drugs, and there are many areas where this system struggles to deliver,… read more here.
Keywords: drug discovery; open source; six laws;
Drug Discovery and Development on Pma1, Where Are We Now? A Critical Review from 1995 to 2022
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DOI: 10.1002/cmdc.202200356
Abstract: Plasma membrane H+‐ATPase (Pma1) is an enzyme uniquely found in plants and fungi. The enzyme controls the nutrient uptake of plants and fungi via an electrochemical gradient processes, which is essential for their survival. Inhibiting… read more here.
Keywords: review; drug discovery; 1995 2022; discovery development ... See more keywords
Fluorinated Cycloalkyl Building Blocks for Drug Discovery
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DOI: 10.1002/cmdc.202200365
Abstract: The review covers various aspects of fluorinated cycloalkyl (C3−C7) building blocks for drug discovery, including their synthesis, key physicochemical properties, and biological and medicinal applications of their derivatives. The discussed synthetic methods include classical nucleophilic… read more here.
Keywords: drug discovery; cycloalkyl building; blocks drug; building blocks ... See more keywords
New and Emerging Research on Solute Carrier and ATP Binding Cassette Transporters in Drug Discovery and Development: Outlook From the International Transporter Consortium
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DOI: 10.1002/cpt.2627
Abstract: Enabled by a plethora of new technologies, research in membrane transporters has exploded in the past decade. The goal of this state‐of‐the‐art article is to describe recent advances in research on membrane transporters that are… read more here.
Keywords: discovery development; drug discovery; transporter; membrane transporters ... See more keywords
Direct and indirect approaches to identify drug modes of action
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DOI: 10.1002/iub.1697
Abstract: Phenotypic assays are becoming increasingly more common among drug discovery practices, expanding drug target diversity as lead compounds identified through such screens are not limited to known targets. While increasing diversity is beneficial to the… read more here.
Keywords: drug; modes action; drug discovery; action ... See more keywords
A comprehensive overview of CRISPR/Cas 9 technology and application thereof in drug discovery
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Cellular Biochemistry"
DOI: 10.1002/jcb.30329
Abstract: Clustered Regularly Interspaced Short Palindromic Repeat (CRISPR)‐Cas technology possesses revolutionary potential to positively affect various domains of drug discovery. It has initiated a rise in the area of genetic engineering and its advantages range from… read more here.
Keywords: drug discovery; technology; crispr; crispr cas ... See more keywords