Selective inhibitors of the Aurora A-TPX2 protein-protein interaction exhibitin vivoefficacy as targeted anti-mitotic agents

Autor: Simon R. Stockwell, Duncan E. Scott, Gerhard Fischer, Estrella Guarino, Timothy P. C. Rooney, Tzu-Shean Feng, Tommaso Moschetti, Rajavel Srinivasan, Esther Alza, Alice Asteian, Claudio Dagostin, Anna Alcaide, Mathieu Rocaboy, Beata Blaszczyk, Alicia Higueruelo, Xuelu Wang, Maxim Rossmann, Trevor R. Perrior, Tom L. Blundell, David R. Spring, Grahame McKenzie, Chris Abell, John Skidmore, Marko Hyvönen, Ashok R. Venkitaraman

The protein kinase Aurora A, and its close relative, Aurora B, regulate human cell division. Aurora A is frequently overexpressed in cancers of the breast, ovary, pancreas and blood, provoking genome instability and resistance to anti-mitotic chemoth

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::d989dbb8823cab17b2cfdce4dae22a7b
https://doi.org/10.1101/2023.03.22.533679

SLAP reagents for the photocatalytic synthesis of C3/C5-substituted, N-unprotected selenomorpholines and 1,4-selenazepanes

Autor: Rajamani Lakshminarayanan, Xingwang Deng, Eunice Tze Leng Goh, Chenyu Pan, Rajavel Srinivasan, Guan Zhou

Publikováno v: Chemical Communications. 56:12546-12549

Herein, we disclose the first set of unique selenium-containing SLAP (SiLicon Amine Protocol) reagents for the direct synthesis of C3/C5-substituted selenomorpholines and 1,4-selenazepanes from diverse (hetero)aldehydes under mild photocatalytic cond

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ad602395ce03c2a6911516ec6c7e3cd7
https://doi.org/10.1039/d0cc04471g

SnAP reagents for the synthesis of selenomorpholines and 1,4-selenazepanes and their biological evaluation

Autor: Xingwang Deng, Guan Zhou, Rajamani Lakshminarayanan, Rajavel Srinivasan, Mobashar Hussain Urf Turabe Fazil, Jing Tian

Publikováno v: Chemical Communications. 56:1780-1783

Herein, we disclose the first set of unique selenium-containing SnAP reagents for the direct synthesis of C-substituted selenomorpholines and 1,4-selenazepanes, including their amino acid derivatives from commercially available aldehydes under mild c

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a812823acef04fa325e3d5b372b1900f
https://doi.org/10.1039/c9cc09337k

Divergent synthesis of 5′,7′-difluorinated dihydroxanthene-hemicyanine fused near-infrared fluorophores

Autor: Gu Lingyue, Shasha Zheng, Jean-Alexandre Richard, Denis Jacquemin, Rajavel Srinivasan, Michelle Jui Hsien Ong, Anthony Romieu

Publikováno v: Organic and Biomolecular Chemistry
Organic and Biomolecular Chemistry, Royal Society of Chemistry, 2019, 17 (17), pp.4291-4300. ⟨10.1039/c9ob00568d⟩

International audience; We describe an expedient access to a 5', 6', 7'-trifluoro dihydroxanthene-hemicyanine fused scaffold in 2 steps and 54% overall yield from the corresponding salicylic aldehyde. A 6'-regioselective nucleophilic aromatic substit

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e4e0d305caa4743b5750fb8af4e462c5
https://doi.org/10.1039/c9ob00568d

A small-molecule inhibitor of the BRCA2-RAD51 interaction modulates RAD51 assembly and potentiates DNA damage-induced cell death

Autor: Chris Abell, Kalina T. Haas, Matthias T. Ehebauer, Luca Pellegrini, Amy Emery, May Marsh, David J. Huggins, Chiara R. Valenzano, Tom L. Blundell, Ashok R. Venkitaraman, Bryn Hardwick, Miyoung Lee, Lorraine Barber, Timothy Sharpe, Rajavel Srinivasan, John Skidmore, Nicola J. Francis-Newton, Alessandro Esposito, Duncan Scott, Claudio Dagostin, Marko Hyvönen, Gerhard Fischer, Andrew R. Bayly, Grahame J. McKenzie, Trevor Perrior, Tommaso Moschetti, Anthony G. Coyne

Publikováno v: Cell Chemical Biology
'Cell Chemical Biology ', vol: 28, pages: 835-847 (2021)

Summary BRCA2 controls RAD51 recombinase during homologous DNA recombination (HDR) through eight evolutionarily conserved BRC repeats, which individually engage RAD51 via the motif Phe-x-x-Ala. Using structure-guided molecular design, templated on a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::20e8b51ead91fb6e0441f1e51a013c4f