Structural and functional analyses of minimal phosphopeptides targeting the polo-box domain of polo-like kinase 1 [PDF]
, 2009 Polo-like kinase-1 (Plk1) has a pivotal role in cell proliferation and is considered a potential target for anticancer therapy. The noncatalytic polo-box domain (PBD) of Plk1 forms a phosphoepitope binding module for protein-protein interaction. Here, we
A Hanisch +45 more
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Atomically Precise Clusterzymes: A Programmable Optoelectronic Platform for Neuroscience. [PDF]
Adv Sci (Weinh)Atomically precise clusterzymes, engineered via atomic and ligand design, serve as programmable platforms for neuroscience applications. They demonstrate tailored biocatalysis for neuroinflammation, tunable optical properties for deep‐tissue bioimaging and 3D visualization, and enhanced charge transfer for brain–computer interfaces.
Sun S +6 more
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Transcriptomic-metabolomic reprogramming in EGFR-mutant NSCLC early adaptive drug escape linking TGFβ2-bioenergetics-mitochondrial priming. [PDF]
, 2016 The impact of EGFR-mutant NSCLC precision therapy is limited by acquired resistance despite initial excellent response. Classic studies of EGFR-mutant clinical resistance to precision therapy were based on tumor rebiopsies late during clinical tumor ...
Bagai, Rakesh +14 more
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Characterization of the transport of lysine-containing dipeptides by PepT1orthologs expressed in Xenopus laevis oocytes. [PDF]
, 2013 During digestion, dietary proteins cleaved in di and tri-peptides are translocated from the intestinal lumen into the enterocytes via PepT1 (SLC15A1) using an inwardly directed proton electrochemical gradient.
Bossi E. +6 more
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Фармакокинетика и Фармакодинамика, 2020 At the Zakusov Institute of Pharmacology designed and synthesized dimeric dipeptide mimetics of the 1st (GK-6) and 4th (GK-2) nerve growth factor loops, 1st (GSB-214), 2nd (GTS-201) and 4th (GSB -106, GSB-106Ac) brain-derived neurotrophic factor loops ...
A. G. Mezhlumyan +5 more
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Synthesis of potential β-turn bicyclic dipeptide mimetics
J. Chem. Soc., Chem. Commun., 1993 The syntheses of four diastereoisomeric bicyclic lactams, intended for analysis as β-turn-inducing mimetics, are described; the crystal structure of one derivative has been reported.
Baldwin, J +3 more
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PTPN22 regulates NLRP3-mediated IL1B secretion in an autophagy-dependent manner [PDF]
, 2017 A variant within the gene locus encoding PTPN22 (protein tyrosine phosphatase, non-receptor type 22) emerged as an important risk factor for auto-inflammatory disorders, including rheumatoid arthritis, systemic lupus erythematosus and type 1 diabetes ...
Chan, Andrew C +7 more
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Фармакокинетика и Фармакодинамика, 2020 . The study of allergenic properties and immunotoxic effects of the ready-to-use drug form of GSB-106 was carried out. The study of allergenic properties and immunotoxicity of GSB-106 was performed on male albino guinea pigs weighing 250-300 g and on ...
L. P. Kovalenko +4 more
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Targeting SxIP-EB1 interaction: An integrated approach to the discovery of small molecule modulators of dynamic binding sites [PDF]
, 2017 End binding protein 1 (EB1) is a key element in the complex network of protein-protein interactions at microtubule (MT) growing ends, which has a fundamental role in MT polymerisation. EB1 is an important protein target as it is involved in regulating MT
Almeida, TB +3 more
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Dipeptide mimetic of the bdnf loop 4 possesses analgetic activity
Доклады Академии наук, 2019 Previously, we synthesized a dimeric dipeptide mimetic of the brain-derived neurotrophic factor (BDNF) loop 4, GSB-106, which, similarly to BDNF, activated TrkB, PI3K/AKT, and MAPK/ERK. When administered systemically, it exhibited neuroprotective, antidepressant, and antidiabetic activities and stimulated neurogenesis and synaptogenesis. In this study,
T A, Gudasheva +4 more
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