Výsledky vyhledávání - "Fiona P. Bailey"

Towards 20,20-difluorinated bryostatin: synthesis and biological evaluation of C17,C27-fragments

Autor: Steven Hoekman, Claire E. Rye, Patrick A. Eyers, Fiona P. Bailey, Paul R. Mears, Dominic P. Byrne, Eric J. Thomas

Publikováno v: Mears, P R, Hoekman, S, Rye, C E, Bailey, F P, Byrne, D P, Eyers, P A & Thomas, E J 2019, ' Towards 20,20-difluorinated bryostatin: synthesis and biological evaluation of C17,C27-fragments ', Organic & biomolecular chemistry, vol. 17, no. 6, pp. 1487-1505 . https://doi.org/10.1039/C8OB03152E
ORGANIC & BIOMOLECULAR CHEMISTRY

Bryostatins with modified C17-C27 fragments have not been widely studied. The synthesis of 20,20-difluorinated analogues was therefore investigated. Such substitution would inhibit dehydration involving the C19-hydroxyl group and stabilise the ring-c

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eeafbece8e1b98ac0b670119369fcca4
https://doi.org/10.1039/c8ob03152e

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Adaptation of the human Cell Line Activation Test (h-CLAT) to animal-product-free conditions

Autor: Christopher Longmore, Carol Treasure, Lottie Roscoe, Alexander J.P. Edwards, Bushra Sim, Fiona P. Bailey

Publikováno v: ALTEX. :477-488

Skin sensitisers are substances that can elicit allergic responses following skin contact and the process by which this occurs is described as skin sensitisation. Skin sensitisation is defined as a series of key events, that form an adverse outcome p

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ed10beef5c22c617c21630340fd42ab3
https://doi.org/10.14573/altex.1710051

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Covalent inhibitors of EGFR family protein kinases induce degradation of human Tribbles 2 (TRIB2) pseudokinase in cancer cells

Autor: Karen Keeshan, Wayland Yeung, Claire E. Eyers, Patrick A. Eyers, Safal Shrestha, William J. Zuercher, Daniel M. Foulkes, Natarajan Kannan, Samantha Ferries, Fiona P. Bailey, Dominic P. Byrne, David H. Drewry, Carrow I. Wells

Publikováno v: SCIENCE SIGNALING

A major challenge associated with biochemical and cellular analysis of pseudokinases is a lack of target-validated small-molecule compounds with which to probe function. Tribbles 2 (TRIB2) is a cancer-associated pseudokinase with a diverse interactom

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::48d753464f4954c9661d392a921d3b13
https://doi.org/10.1126/scisignal.aat7951

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Repurposing covalent EGFR/HER2 inhibitors for on-target degradation of human Tribbles 2 (TRIB2) pseudokinase

Autor: Samantha Ferries, Daniel M. Foulkes, David H. Drewry, Patrick A. Eyers, Carrow I. Wells, Karen Keeshan, Dominic P. Byrne, William J. Zuercher, Natarajan Kannan, Wayland Yeung, Fiona P. Bailey, Safal Shrestha, Claire E. Eyers

ONE SENTENCE SUMMARYA Tribbles 2 pseudokinase small molecule screen led to the identification of known EGFR/HER2 inhibitors that alter the stability of TRIB2in vitroand lead to rapid on-target degradation of TRIB2 in human cancer cells.SHORT ABSTRACT

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fec59122559e339ac00dc6f0be71b968

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Kinome-wide transcriptional profiling of uveal melanoma reveals new vulnerabilities to targeted therapeutics

Autor: Helen Kalirai, Kim Clarke, Judy M. Coulson, Francesco Falciani, Jenna Kenyani, Haleh Shahidipour, Sarah E. Coupland, Fiona P. Bailey, Joseph J. Sacco, Patrick A. Eyers

Publikováno v: Pigment Cell and Melanoma Research

Metastatic uveal melanoma (UM) is invariably fatal, usually within a year of diagnosis. There are currently no effective therapies, and clinical studies employing kinase inhibitors have so far demonstrated limited success. This is despite common acti

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::df8e0755e7a1ae96516ed291436a7317
https://pubmed.ncbi.nlm.nih.gov/28972303

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The hVps34-SGK3 pathway alleviates sustained PI3K/Akt inhibition by stimulating mTORC1 and tumour growth

Autor: Ruzica Bago, Claire Crafter, Pau Castel, Eeva Sommer, José Baselga, Natalia Shpiro, Dario R. Alessi, Fiona P. Bailey, Patrick A. Eyers, Darren Cross

Publikováno v: The EMBO Journal
EMBO JOURNAL

We explore mechanisms that enable cancer cells to tolerate PI3K or Akt inhibitors. Prolonged treatment of breast cancer cells with PI3K or Akt inhibitors leads to increased expression and activation of a kinase termed SGK3 that is related to Akt. Und

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3392caacfd1f3426baa077a6be0197a6
https://pubmed.ncbi.nlm.nih.gov/27481935

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Tribbles pseudokinases: novel targets for chemical biology and drug discovery?

Autor: Daniel M. Foulkes, Patrick A. Eyers, Fiona P. Bailey, Dominic P. Byrne

Publikováno v: Biochemical Society transactions. 43(5)

Tribbles (TRIB) proteins are pseudokinase mediators of eukaryotic signalling that have evolved important roles in lipoprotein metabolism, immune function and cellular differentiation and proliferation. In addition, an evolutionary-conserved modulatio

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::65b5804f39e77c1001b947830d0e6d5a
https://pubmed.ncbi.nlm.nih.gov/26517930

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The Tribbles 2 (TRB2) pseudokinase binds to ATP and autophosphorylates in a metal-independent manner

Autor: Christopher Novotny, Patrick A. Eyers, Claire E. Eyers, Dominic P. Byrne, Krishnadev Oruganty, Kevan M. Shokat, Natarajan Kannan, Fiona P. Bailey

Publikováno v: The Biochemical journal. 467(1)

The human Tribbles (TRB)-related pseudokinases are CAMK (calcium/calmodulin-dependent protein kinase)-related family members that have evolved a series of highly unusual motifs in the ‘pseudocatalytic’ domain. In canonical kinases, conserved amin

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f14eb9afe7d1e9b7008e299dd5ce51b7
https://pubmed.ncbi.nlm.nih.gov/25583260

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Going for broke: targeting the human cancer pseudokinome

Autor: Daniel I. McSkimming, Fiona P. Bailey, Patrick A. Eyers, Dominic P. Byrne, Natarajan Kannan

Publikováno v: The Biochemical journal. 465(2)

Protein phosphorylation lies at the heart of cell signalling, and somatic mutation(s) in kinases drives and sustains a multitude of human diseases, including cancer. The human protein kinase superfamily (the kinome) encodes approximately 50 ‘pseudo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::89c1edb594be4af268cd9447a51f5569
https://pubmed.ncbi.nlm.nih.gov/25656056

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The resistance tetrad: amino acid hotspots for kinome-wide exploitation of drug-resistant protein kinase alleles

Autor: Fiona P, Bailey, Veselin I, Andreev, Patrick A, Eyers

Publikováno v: Methods in enzymology. 548

Acquired resistance to targeted kinase inhibitors is a well-documented clinical problem that is potentially fatal for patients to whom a suitable back-up is not available. However, protein kinase alleles that promote resistance to inhibitors can be e

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::e07bf93043b14cb4022265e7d868115b
https://pubmed.ncbi.nlm.nih.gov/25399644

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