Barbara Czakó

Multidisciplinary management of acute cholecystitis during the COVID-19 pandemic

Illés Tóth, Szabolcs Ábrahám, Zain A. Karamya, Ria Benkő et autres

The coronavirus disease 2019 pandemic had a major impact on most medical services. Our aim was to assess the outcome of acute cholecystitis during the nationwide lockdown period. All patients admitted to our emergency department for AC were analysed. Patient characteristics, performance …

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A novel molecular class that recruits HDAC/MECP2 complexes to PU.1 motifs reduces neuroinflammation

William T. Ralvenius, Alison E. Mungenast, Hannah Woolf, M M Huston et autres

Pervasive neuroinflammation occurs in many neurodegenerative diseases, including Alzheimer's disease (AD). SPI1/PU.1 is a transcription factor located at a genome-wide significant AD-risk locus and its reduced expression is associated with delayed onset of AD. We analyzed single-cell transcriptomic datasets from microglia of …

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Abstract 3097: Prodrugs of a 1-hydroxy-2-oxopiperidin-3-yl phosphonate enolase inhibitor for the treatment of ENO1-deleted cancers

Victoria C. Yan, Cong-Dat Pham, Elliot Ballato, Kristine L. Yang et autres

Abstract Cancers harboring homozygous deletion of the glycolytic enzyme enolase 1 (ENO1) are selectively vulnerable to inhibition of the paralogous isoform, enolase 2 (ENO2). We previously identified and characterized a competitive, small molecule phosphonate inhibitor of ENO2, 1-hydroxy-2-oxopiperidin-3-yl phosphonate (HEX), and its …

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Data from Allosteric SHP2 Inhibitor, IACS-13909, Overcomes EGFR-Dependent and EGFR-Independent Resistance Mechanisms toward Osimertinib

Yuting Sun, Brooke A. Meyers, Barbara Czakó, Paul G. Leonard et autres

Abstract Src homology 2 domain-containing phosphatase (SHP2) is a phosphatase that mediates signaling downstream of multiple receptor tyrosine kinases (RTK) and is required for full activation of the MAPK pathway. SHP2 inhibition has demonstrated tumor growth inhibition in RTK-activated cancers in preclinical …

Data from Allosteric SHP2 Inhibitor, IACS-13909, Overcomes EGFR-Dependent and EGFR-Independent Resistance Mechanisms toward Osimertinib

Yuting Sun, Brooke A. Meyers, Barbara Czakó, Paul G. Leonard et autres

Abstract Src homology 2 domain-containing phosphatase (SHP2) is a phosphatase that mediates signaling downstream of multiple receptor tyrosine kinases (RTK) and is required for full activation of the MAPK pathway. SHP2 inhibition has demonstrated tumor growth inhibition in RTK-activated cancers in preclinical …

Supplementary information from Allosteric SHP2 Inhibitor, IACS-13909, Overcomes EGFR-Dependent and EGFR-Independent Resistance Mechanisms toward Osimertinib

Yuting Sun, Brooke A. Meyers, Barbara Czakó, Paul G. Leonard et autres

Supplementary Materials and Methods Supplementary References Tables S1 to S3 and legends Figures S1 to S4 and legends

Supplementary information from Allosteric SHP2 Inhibitor, IACS-13909, Overcomes EGFR-Dependent and EGFR-Independent Resistance Mechanisms toward Osimertinib

Yuting Sun, Brooke A. Meyers, Barbara Czakó, Paul G. Leonard et autres

Supplementary Materials and Methods Supplementary References Tables S1 to S3 and legends Figures S1 to S4 and legends

Prodrugs of a 1-Hydroxy-2-oxopiperidin-3-yl Phosphonate Enolase Inhibitor for the Treatment of ENO1-Deleted Cancers

Victoria C. Yan, Cong-Dat Pham, Elliot Ballato, Kristine L. Yang et autres

. The activity of select prodrugs was also probed using the NCI-60 cell line screen, supporting its use to examine the relationship between prodrugs and cell line-dependent bioactivation.

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CCDC 2191608: Experimental Crystal Structure Determination

Barbara Czakó, Yuting Sun, Timothy McAfoos, Jason B. Cross et autres

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, …

Screening of Hydrocarbon-Stapled Peptides for Inhibition of Calcium-Triggered Exocytosis

Ying Lai, Michael J. Tuvim, Jeremy Leitz, John Jacob Peters et autres

The so-called primary interface between the SNARE complex and synaptotagmin-1 (Syt1) is essential for Ca 2+ -triggered neurotransmitter release in neuronal synapses. The interacting residues of the primary interface are conserved across different species for synaptotagmins (Syt1, Syt2, Syt9), SNAP-25, and syntaxin-1A …

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Screening of hydrocarbon-stapled peptides for inhibition of calcium-triggered exocytosis

Ying Lai, Michael J. Tuvim, Jeremy Leitz, John Jacob Peters et autres

Abstract The so-called primary interface between the SNARE complex and synaptotagmin-1 (Syt1) is essential for Ca 2+ -triggered neurotransmitter release in neuronal synapses. The interacting residues of the primary interface are conserved across different species for synaptotagmins (Syt1, Syt2, Syt9), SNAP-25, and …

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Abstract P207: BBP-398, a potent, small molecule inhibitor of SHP2, enhances the response of established NSCLC xenografts to KRASG12C and mutEGFR inhibitors

James P. Stice, Sofia Donovan, Yuting Sun, Nancy E. Kohl et autres

Abstract Src homology 2 domain-containing phosphatase (SHP2), a ubiquitously expressed non-receptor tyrosine phosphatase, plays a critical role in the regulation of the MAPK signaling pathway and cellular proliferation. Activating mutations in SHP2 are associated with the development of multiple malignancies including leukemia, …

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