iTAG an optimized IMiD-induced degron for targeted protein degradation in human and murine cells

Authors: Bouguenina, Habib, Nicolaou, Stephanos, Le Bihan, Yann-Vaï, Bowling, Elizabeth A., Calderon, Cheyenne, Caldwell, John J., Harrington, Brinley, Hayes, Angela, McAndrew, P. Craig, Mitsopoulos, Costas, Sialana, Fernando Jr., Scarpino, Andrea, Stubbs, Mark, Thapaliya, Arjun, Tyagi, Siddhartha, Wang, Hannah Z., Wood, Francesca, Burke, Rosemary, Raynaud, Florence, Choudhary, Jyoti, van Montfort, Rob L.M., Sadok, Amine, Westbrook, Thomas F., Collins, Ian, Chopra, Rajesh

Source: In iScience 21 July 2023 26(7)

C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays

Authors: Le Bihan, Yann-Vaï, Lanigan, Rachel M., Atrash, Butrus, McLaughlin, Mark G., Velupillai, Srikannathasan, Malcolm, Andrew G., England, Katherine S., Ruda, Gian Filippo, Mok, N. Yi, Tumber, Anthony, Tomlin, Kathy, Saville, Harry, Shehu, Erald, McAndrew, Craig, Carmichael, LeAnne, Bennett, James M., Jeganathan, Fiona, Eve, Paul, Donovan, Adam, Hayes, Angela, Wood, Francesca, Raynaud, Florence I., Fedorov, Oleg, Brennan, Paul E., Burke, Rosemary, van Montfort, Rob L.M., Rossanese, Olivia W., Blagg, Julian, Bavetsias, Vassilios

Source: In European Journal of Medicinal Chemistry 1 September 2019 177:316-337

Synthesis and profiling of a 3-aminopyridin-2-one-based kinase targeted fragment library: Identification of 3-amino-5-(pyridin-4-yl)pyridin-2(1H)-one scaffold for monopolar spindle 1 (MPS1) and Aurora kinases inhibition

Authors: Fearon, Daren, Westwood, Isaac M., van Montfort, Rob L.M., Bayliss, Richard, Jones, Keith, Bavetsias, Vassilios

Source: In Bioorganic & Medicinal Chemistry 15 July 2018 26(11):3021-3029

iTAG an optimized IMiD-induced degron for targeted protein degradation in human and murine cells

Authors: Bouguenina, Habib ^∗, Nicolaou, Stephanos, Bihan, Yann-Vaï Le, Bowling, Elizabeth A., Calderon, Cheyenne, Caldwell, John J., Harrington, Brinley, Hayes, Angela, McAndrew, P. Craig, Mitsopoulos, Costas, Sialana, Fernando Jr., Scarpino, Andrea, Stubbs, Mark, Thapaliya, Arjun, Tyagi, Siddhartha, Wang, Hannah Z., Wood, Francesca, Burke, Rosemary, Raynaud, Florence, Choudhary, Jyoti, van Montfort, Rob L.M., Sadok, Amine, Westbrook, Thomas F., Collins, Ian, Chopra, Rajesh

Source: In iScience 17 May 2024 27(5)

Identification of Autophosphorylation Inhibitors of the Inositol-Requiring Enzyme 1 Alpha (IRE1α) by High-Throughput Screening Using a DELFIA Assay

Authors: Newbatt, Yvette, Hardcastle, Anthea, McAndrew, P. Craig, Strover, Jade A., Mirza, Amin, Morgan, Gareth J., Burke, Rosemary ^*, Davies, Faith E., Collins, Ian, van Montfort, Rob L.M. ^**

Source: In SLAS Discovery March 2013 18(3):298-308

Benzimidazole inhibitors of the protein kinase CHK2: Clarification of the binding mode by flexible side chain docking and protein–ligand crystallography

Authors: Matijssen, Cornelis, Silva-Santisteban, M. Cris, Westwood, Isaac M., Siddique, Samerene, Choi, Vanessa, Sheldrake, Peter, van Montfort, Rob L.M., Blagg, Julian

Source: In Bioorganic & Medicinal Chemistry 15 November 2012 20(22):6630-6639

Unveiling the Secrets of the Ancestral PI3 Kinase Vps34

Authors: Workman, Paul, van Montfort, Rob L.M.

Source: In Cancer Cell 2010 17(5):421-423

Insights into the Conformational Variability and Regulation of Human Nek2 Kinase

Authors: Westwood, Isaac, Cheary, Donna-Marie, Baxter, Joanne E., Richards, Mark W., van Montfort, Rob L.M., Fry, Andrew M., Bayliss, Richard

Source: In Journal of Molecular Biology 20 February 2009 386(2):476-485

Structure-based design of molecular cancer therapeutics

Authors: van Montfort, Rob L.M., Workman, Paul

Source: In Trends in Biotechnology 2009 27(5):315-328

Crystal structure of truncated human βB1-crystallin.

Authors: van Montfort, Rob L.M., Bateman, Orval A., Lubsen, Nicolette H., Slingsby, Christine

Source: Protein Science: A Publication of the Protein Society; 2003, Vol. 12 Issue 11, p2606-2612, 7p

Crystallization of Enzyme IIB of the Cellobiose-specific Phosphotransferase System of Escherichia coli

Authors: van Montfort, Rob L.M., Pijning, Tjaard, Kalk, Kor H., Schuurman-Wolters, Gea K., Reizer, Jonathan, Saier, Milton H., Jr, Robillard, George, Dijkstra, Bauke W.

Source: In Journal of Molecular Biology 16 June 1994 239(4):588-590