Search Results - "Karatas, Hacer"
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High-Affinity, Small-Molecule Peptidomimetic Inhibitors of MLL1/WDR5 Protein–Protein Interaction
Published in Journal of the American Chemical Society (16-01-2013)“…Mixed lineage leukemia 1 (MLL1) is a histone H3 lysine 4 (H3K4) methyltransferase, and targeting the MLL1 enzymatic activity has been proposed as a novel…”
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Targeting MLL1 H3K4 Methyltransferase Activity in Mixed-Lineage Leukemia
Published in Molecular cell (23-01-2014)“…Here we report a comprehensive characterization of our recently developed inhibitor MM-401 that targets the MLL1 H3K4 methyltransferase activity. MM-401 is…”
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3
Synthesis and Anticancer Activity of Novel Indole Derivatives as Dual EGFR/SRC Kinase Inhibitors
Published in Current medicinal chemistry (01-01-2024)“…Recent studies showed that the cooperation between c-SRC and EGFR is responsible for more aggressive phenotype in diverse tumors, including glioblastomas and…”
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4
TEAD–YAP Interaction Inhibitors and MDM2 Binders from DNA‐Encoded Indole‐Focused Ugi Peptidomimetics
Published in Angewandte Chemie International Edition (09-11-2020)“…DNA‐encoded combinatorial synthesis provides efficient and dense coverage of chemical space around privileged molecular structures. The indole side chain of…”
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5
Discovery of a Highly Potent, Cell-Permeable Macrocyclic Peptidomimetic (MM-589) Targeting the WD Repeat Domain 5 Protein (WDR5)–Mixed Lineage Leukemia (MLL) Protein–Protein Interaction
Published in Journal of medicinal chemistry (22-06-2017)“…We report herein the design, synthesis, and evaluation of macrocyclic peptidomimetics that bind to WD repeat domain 5 (WDR5) and block the WDR5–mixed lineage…”
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Structure-Based Design of High-Affinity Macrocyclic Peptidomimetics to Block the Menin-Mixed Lineage Leukemia 1 (MLL1) Protein–Protein Interaction
Published in Journal of medicinal chemistry (14-02-2013)“…Menin is an essential oncogenic cofactor for mixed lineage leukemia 1 (MLL1)-mediated leukemogenesis through its direct interaction with MLL1. Targeting the…”
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7
A protein tertiary structure mimetic modulator of the Hippo signalling pathway
Published in Nature communications (27-10-2020)“…Transcription factors are key protein effectors in the regulation of gene transcription, and in many cases their activity is regulated via a complex network of…”
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An economical and practical procedure of favipiravir synthesis for the treatment of Covid-19
Published in Chemical papers (01-03-2023)“…Favipiravir is a wide-spectrum antiviral generic drug that has received large attention during the recent COVID-19 pandemic. While there are synthetic…”
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MLL1 and MLL1 fusion proteins have distinct functions in regulating leukemic transcription program
Published in Cell discovery (17-05-2016)“…Mixed lineage leukemia protein-1 (MLL1) has a critical role in human MLL1 rearranged leukemia ( MLLr ) and is a validated therapeutic target. However, its role…”
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Synthesis and Potent Antimicrobial Activity of Some Novel 4-(5, 6-Dichloro-1H-benzimidazol-2-yl)-N-substituted Benzamides
Published in Archiv der Pharmazie (Weinheim) (01-10-2004)“…A series of 4‐(5, 6‐dichloro‐1H‐benzimidazol‐2‐yl)‐N‐substituted benzamides were synthesized and evaluated for antibacterial and antifungal activities against…”
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11
In Vivo Molecular Bioluminescence Imaging: New Tools and Applications
Published in Trends in biotechnology (Regular ed.) (01-07-2017)“…in vivo bioluminescence imaging (BLi) is an optical molecular imaging technique used to visualize molecular and cellular processes in health and diseases and…”
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12
Chemical suppression of specific C-C chemokine signaling pathways enhances cardiac reprogramming
Published in The Journal of biological chemistry (07-06-2019)“…Reprogramming of fibroblasts into induced cardiomyocytes (iCMs) is a potentially promising strategy for regenerating a damaged heart. However, low…”
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13
Synthesis and Potent In vitro Activity of Novel 1H-Benzimidazoles as Anti-MRSA Agents
Published in Chemical biology & drug design (01-08-2012)“…A new class of 1H‐benzimidazolecarboxamidines was synthesized and evaluated for in vitro antibacterial and antifungal activities, including drug‐resistant…”
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14
Discovery of Covalent Inhibitors Targeting the Transcriptional Enhanced Associate Domain Central Pocket
Published in Journal of medicinal chemistry (22-10-2020)“…Transcriptional enhanced associate domain (TEAD) transcription factors together with coactivators and corepressors modulate the expression of genes that…”
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The cholesterol transfer protein GRAMD1A regulates autophagosome biogenesis
Published in Nature chemical biology (01-07-2019)“…Autophagy mediates the degradation of damaged proteins, organelles and pathogens, and plays a key role in health and disease. Thus, the identification of new…”
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Identification of Quinolinols as Activators of TEAD-Dependent Transcription
Published in ACS chemical biology (20-12-2019)“…The transcriptional co-regulators YAP (Yes-associated protein) and TAZ (transcriptional coactivator with PDZ-binding motif) are the vertebrate downstream…”
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Analysis of the Binding of Mixed Lineage Leukemia 1 (MLL1) and Histone 3 Peptides to WD Repeat Domain 5 (WDR5) for the Design of Inhibitors of the MLL1−WDR5 Interaction
Published in Journal of medicinal chemistry (22-07-2010)“…MLL1 is a histone 3 lysine 4 (H3K4) methyltransferase and a promising new cancer therapeutic target. The catalytic activity of MLL1 is regulated by the…”
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MLL1 Inhibition Reprograms Epiblast Stem Cells to Naive Pluripotency
Published in Cell stem cell (07-04-2016)“…The interconversion between naive and primed pluripotent states is accompanied by drastic epigenetic rearrangements. However, it is unclear whether intrinsic…”
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The Pseudo‐Natural Product Rhonin Targets RHOGDI
Published in Angewandte Chemie International Edition (25-04-2022)“…For the discovery of novel chemical matter generally endowed with bioactivity, strategies may be particularly efficient that combine previous insight about…”
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Real-Time Imaging and Quantification of Peptide Uptake in Vitro and in Vivo
Published in ACS chemical biology (18-10-2019)“…Peptides constitute an important class of drugs for the treatment of multiple metabolic, oncological, and neurodegenerative diseases, and several hundred novel…”
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