Zobrazeno 1 - 10 of 109 pro vyhledávání: '"Simon P. MacKay"'
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Akademický článek
Design and Synthesis of Novel Aminoindazole-pyrrolo[2,3-b]pyridine Inhibitors of IKKα That Selectively Perturb Cellular Non-Canonical NF-κB Signalling
Autor: Christopher Riley, Usama Ammar, Aisha Alsfouk, Nahoum G. Anthony, Jessica Baiget, Giacomo Berretta, David Breen, Judith Huggan, Christopher Lawson, Kathryn McIntosh, Robin Plevin, Colin J. Suckling, Louise C. Young, Andrew Paul, Simon P. Mackay
Publikováno v: Molecules, Vol 29, Iss 15, p 3515 (2024)
The inhibitory-kappaB kinases (IKKs) IKKα and IKKβ play central roles in regulating the non-canonical and canonical NF-κB signalling pathways. Whilst the proteins that transduce the signals of each pathway have been extensively characterised, the
Externí odkaz: https://doaj.org/article/e3e2e03e3b834ed6981a0d5113267e5c
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2
Akademický článek
Stereoselective synthesis of carbocyclic analogues of the nucleoside Q precursor (PreQ0)
Autor: Sabin Llona-Minguez, Simon P. Mackay
Publikováno v: Beilstein Journal of Organic Chemistry, Vol 10, Iss 1, Pp 1333-1338 (2014)
A convergent and stereoselective synthesis of chiral cyclopentyl- and cyclohexylamine derivatives of nucleoside Q precursor (PreQ0) has been accomplished. This synthetic route allows for an efficient preparation of 4-substituted analogues with intere
Externí odkaz: https://doaj.org/article/f6a5198eb26f4f25862d9823e031a2fd
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3
Akademický článek
Manganese dioxide mediated one-pot synthesis of methyl 9H-pyrido[3,4-b]indole-1-carboxylate: Concise synthesis of alangiobussinine
Autor: Jessica Baiget, Sabin Llona-Minguez, Stuart Lang, Simon P. MacKay, Colin J. Suckling, Oliver B. Sutcliffe
Publikováno v: Beilstein Journal of Organic Chemistry, Vol 7, Iss 1, Pp 1407-1411 (2011)
The carboline ring system is an important pharmacophore found in a number of biologically important targets. Development of synthetic routes for the preparation of these compounds is important in order to prepare a range of analogues containing the c
Externí odkaz: https://doaj.org/article/7eafbe07aa394bfcad65cac6184099fa
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4
Suporting Video Legends from Is the Fate of Clinical Candidate Arry-520 Already Sealed? Predicting Resistance in Eg5–Inhibitor Complexes
Autor: Dimitrios A. Skoufias, Frank Kozielski, Simon P. Mackay, Shozeb Haider, Fangzhu Lin, Sandeep K. Talapatra, Rose-Laure Indorato
SV1-SV6: Time lapse imaging of untreated, Arry-520 and ispinesib treated naive U2OS cells, Eg5(D130) and Eg5(L214) expressing U2OS cells followed for 16h. SV7-SV12: Molecular dynamics simulations of either Eg5(WT), or Eg5(D130) or Eg5(L214) motor dom
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1855f5c63102b4238bd43f7be5c78df1
https://doi.org/10.1158/1535-7163.22509877
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7
Data from Is the Fate of Clinical Candidate Arry-520 Already Sealed? Predicting Resistance in Eg5–Inhibitor Complexes
Autor: Dimitrios A. Skoufias, Frank Kozielski, Simon P. Mackay, Shozeb Haider, Fangzhu Lin, Sandeep K. Talapatra, Rose-Laure Indorato
Arry-520 is an advanced drug candidate from the Eg5 inhibitor class undergoing clinical evaluation in patients with relapsed or refractory multiple myeloma. Here, we show by structural analysis that Arry-520 binds stoichiometrically to the motor doma
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8658ffd7e7127ff5b22cc8e9e92334dd
https://doi.org/10.1158/1535-7163.c.6539407.v1
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8
Supplementary Table 1 and Supplementary Figures 1-3 from Is the Fate of Clinical Candidate Arry-520 Already Sealed? Predicting Resistance in Eg5–Inhibitor Complexes
Autor: Dimitrios A. Skoufias, Frank Kozielski, Simon P. Mackay, Shozeb Haider, Fangzhu Lin, Sandeep K. Talapatra, Rose-Laure Indorato
Table S1: Crystallographic table of data corresponding to the Eg5-Arry-520 complexes. Figure S1: Interactions of the inhibitor and conformational changes upon inhibitor binding. Figure S2: Surface representation of the allosteric inhibitor-binding po
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1039447504df500c420ed42e4c047371
https://doi.org/10.1158/1535-7163.22509871.v1
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9
Regulation of Bcl-XL by non-canonical NF-κB in the context of CD40-induced drug resistance in CLL
Autor: Marco Haselager, Rachel Thijssen, Arnon P. Kater, Christopher West, Roel J. W. van Kampen, Elaine Willmore, Simon P. Mackay, Eric Eldering, Louise C. Young
Publikováno v: Cell Death and Differentiation
Cell death and differentiation, 28(5), 1658-1668. Nature Publishing Group
In chronic lymphocytic leukemia (CLL), the lymph node (LN) microenvironment delivers critical survival signals by inducing the expression of anti-apoptotic Bcl-2 members Bcl-XL, Bfl-1, and Mcl-1, resulting in apoptosis blockade. We determined previou
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9cd804475140f3409a2804c3a88a8de7
http://europepmc.org/articles/PMC8167103
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10
Targeting the non-canonical NF-κB pathway in chronic lymphocytic leukemia and multiple myeloma
Autor: Thomas A. Burley, Emma Kennedy, Georgia Broad, Melanie Boyd, David Li, Timothy Woo, Christopher West, Eleni E. Ladikou, Iona Ashworth, Christopher Fegan, Rosalynd Johnston, Simon Mitchell, Simon P. Mackay, Andrea G. S. Pepper, Chris Pepper
Publikováno v: Cancers; Volume 14; Issue 6; Pages: 1489
In this study, we evaluated an NF-κB inducing kinase (NIK) inhibitor, CW15337, in primary chronic lymphocytic leukemia (CLL) cells, CLL and multiple myeloma (MM) cell lines and normal B- and T-lymphocytes. Basal NF-κB subunit activity was character
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6226df78d8c7a92096c67c5e3c187033
https://strathprints.strath.ac.uk/80165/1/Burley_etal_Cancers_2022_Targeting_the_non_canonical_NF_B_pathway_in_chronic_lymphocytic_leukemia.pdf
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