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Showing results 1 to 6 of 6
  • OER000002767.pdf.jpg
  • Journal article

  • Compound interaction screen on a photoactivatable cellulose membrane (CISCM) identifies drug targets

    • Authors : Melder, Teresa (2023)

  • Identifying the protein targets of drugs is an important but tedious process. Existing proteomic approaches enable unbiased target identification but lack the throughput needed to screen larger compound libraries. Here, we present a compound interaction screen on a photoactivatable cellulose membrane (CISCM) that enables target identification of several drugs in parallel. To this end, we use diazirine-based undirected photoaffinity labeling (PAL) to immobilize compounds...
  • OER000002354.pdf.jpg
  • Journal Article

  • Drug repurposing approach for potential Pfmrk inhibitors as antimalarial agents: an In-silico analysis

    • Authors : Sahu, Abhishek (2023)

  • Malaria is a major global health issue due to the emergence of resistance to most of the available antimalarial drugs. There is an urgent need to discover new antimalarials to tackle the resistance issue. A CDK- like protein, Pfmrk from Plasmodium falciparum, plays a crucial role in regulating cell proliferation and shares 36.28% homology with humans CDK (hCDK7). Pfmrk complex with Pfcyc-1 and stimulates kinase activity. Also, Pfcyc-1 from P.&#...
  • OER000002364.pdf.jpg
  • Journal Article

  • Drug repurposing approach for potential Pfmrk inhibitors as antimalarial agents: an In-silico analysis

    • Authors : McBride, John M. (2023)

  • Alteration of one or few amino acid residues can affect structure [1–3] and function [4] of a protein and, in extreme cases, be the difference between health and disease [5, 6]. Understanding structural consequences of point mutations is important for drug design [7, 8] and could also accelerate optimization of enzymatic function via directed evolution [9, 10]. In these and other applications, theoretical models [11] could...
  • OER000002752.pdf.jpg
  • Journal article

  • Prediction Of The Impact Of Genetic Variability On Drug Sensitivity For Clinically Relevant EGFR Mutations

    • Authors : Suriñach, Aristarc (2023)

  • Mutations in the kinase domain of the Epidermal Growth Factor Receptor (EGFR) can be drivers of cancer and also trigger drug resistance in patients under chemotherapy treatment based on kinase inhibitors use. A priori knowledge of the impact of EGFR variants on drug sensitivity would help to optimize chemotherapy and to design new drugs effective against resistant variants. To this end, we have explored a variety of in silico methods, from...
  • OER000002690-2.pdf.jpg
  • Journal article

  • Smart-design of universally decorated nano-particles for drug delivery applications driven by active transport

    • Authors : Halbi, Gal (2023)

  • Targeting the cell nucleus remains a challenge for drug delivery. Here we present a universal platform for smart design of nano-particles (NPs) decoration that allows recruitment of multiple dynein motors to drive their active motion towards the nucleus. The uniqueness of our approach is based on using: (i) a spacer polymer, commonly Biotin-Polyethylene-glycol-thiol (B-PEG-SH), whose grafting density and molecular weight can be tuned thereby allowing NP trans...
  • OER000002673.pdf.jpg
  • Journal article

  • System-wide profiling by proteome integral solubility alteration assay of drug residence times for target characterization

    • Authors : Sabatier, Pierre (2023)

  • Most drugs used in the clinic and drug candidates target multiple proteins, and thus detailed characterization of their efficacy targets is required. While current methods rely on quantitative measurements at thermodynamic equilibrium, kinetic parameters such as the residence time of a drug on its target provide a better proxy for efficacy in vivo. Here, we present Residence Time Proteome Integral Solubility Alteration (ResT-PISA) assay which provides monitor...