New inhibitors of bacterial hyaluronidase - synthesis and structure-activity relationships [PDF]
, 2006 Potent and selective inhibitors of hyaluronidases are not reported in the literature so far. Such compounds are required as pharmacological tools to investigate the physiological and pathophysiological role of the enzymes and their preferred substrate ...
Braun, Stephan
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Reconstructing enzyme evolution by protein engineering
FEBS Letters, EarlyView.Natural enzyme evolution can be retraced by protein engineering methods such as directed evolution, rational design, and ancestral sequence reconstruction. These approaches reveal how enzymes emerged from ligand‐binding scaffolds, developed varying substrate preferences, formed oligomeric complexes, adapted to environmental changes, and evolved novel ...
Lukas Drexler +2 more
wiley +1 more source
Methyl 9-(1-methyl-1H-indol-3-yl)-9-oxononanoate
Molbank, 2023 Methyl 9-(1-methyl-1H-indol-3-yl)-9-oxononanoate was synthesized using Friedel–Crafts acylation between N-methyl indole and methyl 9-chloro-9-oxononanoate.
Gabriele Micheletti, Carla Boga
doaj +1 more source
One-Pot Approach for the Synthesis of Bis-indole-1,4-disubstituted-1,2,3-triazoles [PDF]
, 2018 A new strategy for the synthesis of bis-indoletriazoles was developed using a sequential one-pot four-step procedure via I2 and H2SO4–SiO2 catalyzed Friedel–Crafts reactions of indole with aldehyde followed by N-alkylation with propargyl bromide ...
Teerapich Kasemsuk (5867480) +3 more
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Organocatalytic Discrimination of Non-Directing Aryl and Heteroaryl Groups: Enantioselective Synthesis of Bioactive Indole-Containing Triarylmethanes [PDF]
, 2021 Despite the enormous developments of asymmetric catalysis, the basis for asymmetric induction is largely limited to spatial interaction between substrate and catalyst.
Meng , Duan +9 more
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Loss of IGF‐1R impairs DNA‐PKcs recruitment to chromatin leading to defective end‐joining
Molecular Oncology, EarlyView.IGF‐1R promotes radioresistance by facilitating DNA‐PKcs recruitment to chromatin, enabling non‐homologous end‐joining (NHEJ) repair of double‐strand breaks. Inhibition or loss of IGF‐1R disrupts this recruitment to damage sites, driving compensatory reliance on microhomology‐mediated end‐joining (MMEJ) repair.
Matthew O. Ellis +3 more
wiley +1 more source
Target-Based Anticancer Indole Derivatives for the Development of Anti-Glioblastoma Agents
Molecules, 2023 Glioblastoma (GBM) is the most aggressive and frequent primary brain tumor, with a poor prognosis and the highest mortality rate. Currently, GBM therapy consists of surgical resection of the tumor, radiotherapy, and adjuvant chemotherapy with ...
Silvia Salerno +5 more
doaj +1 more source
Molecular Oncology, EarlyView.The novel styrylquinazolinone‐based molecule W1B effectively suppresses glioblastoma by inhibiting IGF1R and EGFR. In high‐glucose microenvironments driving tumor resistance, W1B acts synergistically with the EGFR inhibitor dacomitinib. This combination safely blocks compensatory survival signaling in zebrafish xenograft models. Showcasing promising in
Patryk Rurka +9 more
wiley +1 more source
Animals, 2023 Chronic inflammatory enteropathy (CIE) and low-grade intestinal T-cell lymphoma (LGITL) are common chronic enteropathies (CE) in cats. Enteric microbiota dysbiosis is implicated in the pathogenesis of CE; however, the mechanisms of host–microbiome ...
Patrick C. Barko +6 more
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Supplementary Fig. S3 from Interruption of RNA processing machinery by a small compound, 1-[(4-chlorophenyl)methyl]-1H-indole-3-carboxaldehyde (oncrasin-1) [PDF]
, 2009 Supplementary Fig. S3 from Interruption of RNA processing machinery by a small compound, 1-[(4-chlorophenyl)methyl]-1H-indole-3-carboxaldehyde (oncrasin ...
Jinsong Liu (6516) +6 more
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