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  1. Article ; Online: Precision Targeting of Mutant PI3Kα.

    Gong, Grace Q / Vanhaesebroeck, Bart

    Cancer discovery

    2024  Volume 14, Issue 2, Page(s) 204–207

    Abstract: PIK3CA, which encodes the p110α catalytic subunit of PI 3-kinase alpha (PI3Kα), is one of the most frequently genetically activated kinases in solid tumors. In two back-to-back papers, Varkaris and colleagues report on the development of a novel ... ...

    Abstract PIK3CA, which encodes the p110α catalytic subunit of PI 3-kinase alpha (PI3Kα), is one of the most frequently genetically activated kinases in solid tumors. In two back-to-back papers, Varkaris and colleagues report on the development of a novel allosteric PI3Kα-mutant-selective inhibitor and early clinical experience with this compound. See related article by Varkaris et al., p. 227 (6) . See related article by Varkaris et al., p. 240 (5) .
    MeSH term(s) Humans ; Phosphatidylinositol 3-Kinases/genetics ; Mutation ; Phosphoinositide-3 Kinase Inhibitors ; Class I Phosphatidylinositol 3-Kinases/genetics ; Antineoplastic Agents/pharmacology ; Protein Kinase Inhibitors/pharmacology ; Protein Kinase Inhibitors/therapeutic use
    Chemical Substances Phosphatidylinositol 3-Kinases (EC 2.7.1.-) ; Phosphoinositide-3 Kinase Inhibitors ; Class I Phosphatidylinositol 3-Kinases (EC 2.7.1.137) ; Antineoplastic Agents ; Protein Kinase Inhibitors
    Language English
    Publishing date 2024-01-29
    Publishing country United States
    Document type Journal Article
    ZDB-ID 2625242-9
    ISSN 2159-8290 ; 2159-8274
    ISSN (online) 2159-8290
    ISSN 2159-8274
    DOI 10.1158/2159-8290.CD-23-1392
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 6916: Show issues Location:
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  2. Article ; Online: A single discrete Rab5-binding site in phosphoinositide 3-kinase β is required for tumor cell invasion.

    Heitz, Samantha D / Hamelin, David J / Hoffmann, Reece M / Greenberg, Nili / Salloum, Gilbert / Erami, Zahra / Khalil, Bassem D / Shymanets, Aliaksei / Steidle, Elizabeth A / Gong, Grace Q / Nürnberg, Bernd / Burke, John E / Flanagan, Jack U / Bresnick, Anne R / Backer, Jonathan M

    The Journal of biological chemistry

    2019  Volume 294, Issue 12, Page(s) 4621–4633

    Abstract: Phosphoinositide 3-kinase β (PI3Kβ) is regulated by receptor tyrosine kinases (RTKs), G protein-coupled receptors (GPCRs), and small GTPases such as Rac1 and Rab5. Our lab previously identified two residues ( ... ...

    Abstract Phosphoinositide 3-kinase β (PI3Kβ) is regulated by receptor tyrosine kinases (RTKs), G protein-coupled receptors (GPCRs), and small GTPases such as Rac1 and Rab5. Our lab previously identified two residues (Gln
    MeSH term(s) Binding Sites ; Breast Neoplasms/metabolism ; Breast Neoplasms/pathology ; Cell Line, Tumor ; Chemotaxis ; Gelatin/metabolism ; HEK293 Cells ; Humans ; Mass Spectrometry/methods ; Mutation ; Neoplasm Invasiveness ; Phosphatidylinositol 3-Kinase/genetics ; Phosphatidylinositol 3-Kinase/metabolism ; Protein Binding ; rab5 GTP-Binding Proteins/metabolism
    Chemical Substances Gelatin (9000-70-8) ; Phosphatidylinositol 3-Kinase (EC 2.7.1.137) ; RAB5C protein, human (EC 3.6.1.-) ; rab5 GTP-Binding Proteins (EC 3.6.5.2)
    Language English
    Publishing date 2019-01-18
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2997-x
    ISSN 1083-351X ; 0021-9258
    ISSN (online) 1083-351X
    ISSN 0021-9258
    DOI 10.1074/jbc.RA118.006032
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Uc I Zs.108: Show issues Location:
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  3. Article ; Online: Combining properties of different classes of PI3Kα inhibitors to understand the molecular features that confer selectivity.

    Gong, Grace Q / Kendall, Jackie D / Dickson, James M J / Rewcastle, Gordon W / Buchanan, Christina M / Denny, William A / Shepherd, Peter R / Flanagan, Jack U

    The Biochemical journal

    2017  Volume 474, Issue 13, Page(s) 2261–2276

    Abstract: Phosphoinositide 3-kinases (PI3Ks) are major regulators of many cellular functions, and hyperactivation of PI3K cell signalling pathways is a major target for anticancer drug discovery. PI3Kα is the isoform most implicated in cancer, and our aim is to ... ...

    Abstract Phosphoinositide 3-kinases (PI3Ks) are major regulators of many cellular functions, and hyperactivation of PI3K cell signalling pathways is a major target for anticancer drug discovery. PI3Kα is the isoform most implicated in cancer, and our aim is to selectively inhibit this isoform, which may be more beneficial than concurrent inhibition of all Class I PI3Ks. We have used structure-guided design to merge high-selectivity and high-affinity characteristics found in existing compounds. Molecular docking, including the prediction of water-mediated interactions, was used to model interactions between the ligands and the PI3Kα affinity pocket. Inhibition was tested using lipid kinase assays, and active compounds were tested for effects on PI3K cell signalling. The first-generation compounds synthesized had IC
    MeSH term(s) Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacology ; Catalytic Domain ; Cell Proliferation/drug effects ; Class I Phosphatidylinositol 3-Kinases ; Drug Design ; Enzyme Inhibitors/chemistry ; Enzyme Inhibitors/pharmacology ; Humans ; Ligands ; Molecular Docking Simulation ; Molecular Dynamics Simulation ; Neoplasms/drug therapy ; Neoplasms/enzymology ; Neoplasms/pathology ; Phosphatidylinositol 3-Kinases/antagonists & inhibitors ; Protein Binding ; Protein Conformation
    Chemical Substances Antineoplastic Agents ; Enzyme Inhibitors ; Ligands ; Phosphatidylinositol 3-Kinases (EC 2.7.1.-) ; Class I Phosphatidylinositol 3-Kinases (EC 2.7.1.137) ; PIK3CA protein, human (EC 2.7.1.137)
    Language English
    Publishing date 2017-06-26
    Publishing country England
    Document type Journal Article
    ZDB-ID 2969-5
    ISSN 1470-8728 ; 0006-2936 ; 0306-3275 ; 0264-6021
    ISSN (online) 1470-8728
    ISSN 0006-2936 ; 0306-3275 ; 0264-6021
    DOI 10.1042/BCJ20161098
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article ; Online: A small-molecule PI3Kα activator for cardioprotection and neuroregeneration.

    Gong, Grace Q / Bilanges, Benoit / Allsop, Ben / Masson, Glenn R / Roberton, Victoria / Askwith, Trevor / Oxenford, Sally / Madsen, Ralitsa R / Conduit, Sarah E / Bellini, Dom / Fitzek, Martina / Collier, Matt / Najam, Osman / He, Zhenhe / Wahab, Ben / McLaughlin, Stephen H / Chan, A W Edith / Feierberg, Isabella / Madin, Andrew /
    Morelli, Daniele / Bhamra, Amandeep / Vinciauskaite, Vanesa / Anderson, Karen E / Surinova, Silvia / Pinotsis, Nikos / Lopez-Guadamillas, Elena / Wilcox, Matthew / Hooper, Alice / Patel, Chandni / Whitehead, Maria A / Bunney, Tom D / Stephens, Len R / Hawkins, Phillip T / Katan, Matilda / Yellon, Derek M / Davidson, Sean M / Smith, David M / Phillips, James B / Angell, Richard / Williams, Roger L / Vanhaesebroeck, Bart

    Nature

    2023  Volume 618, Issue 7963, Page(s) 159–168

    Abstract: Harnessing the potential beneficial effects of kinase signalling through the generation of direct kinase activators remains an underexplored area of drug ... ...

    Abstract Harnessing the potential beneficial effects of kinase signalling through the generation of direct kinase activators remains an underexplored area of drug development
    MeSH term(s) Humans ; Neoplasms/drug therapy ; Nerve Regeneration/drug effects ; Protein Isoforms/agonists ; Signal Transduction/drug effects ; Class I Phosphatidylinositol 3-Kinases/chemistry ; Class I Phosphatidylinositol 3-Kinases/drug effects ; Cardiotonic Agents/pharmacology ; Animals ; Biocatalysis/drug effects ; Protein Conformation/drug effects ; Neurites/drug effects ; Reperfusion Injury/prevention & control ; Nerve Crush ; Cell Proliferation/drug effects
    Chemical Substances Protein Isoforms ; PIK3CA protein, human (EC 2.7.1.137) ; Class I Phosphatidylinositol 3-Kinases (EC 2.7.1.137) ; Cardiotonic Agents
    Language English
    Publishing date 2023-05-24
    Publishing country England
    Document type Journal Article
    ZDB-ID 120714-3
    ISSN 1476-4687 ; 0028-0836
    ISSN (online) 1476-4687
    ISSN 0028-0836
    DOI 10.1038/s41586-023-05972-2
    Database MEDical Literature Analysis and Retrieval System OnLINE

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