Search Results - "Chessari, G."

380 Induction of apoptosis with a novel dual cIAP1/XIAP antagonist in models of melanoma by Ward, G, Chessari, G, Johnson, C.N, Lewis, J, Rich, S, Thompson, N

Get full text

SAHA overcomes FLIP-mediated inhibition of SMAC mimetic-induced apoptosis in mesothelioma by Crawford, N, Stasik, I, Holohan, C, Majkut, J, McGrath, M, Johnston, P G, Chessari, G, Ward, G A, Waugh, D J, Fennell, D A, Longley, D B

“…Malignant pleural mesothelioma (MPM) is a highly pro-inflammatory malignancy that is rapidly fatal and increasing in incidence. Cytokine signaling within the…”
Get full text

85 Characterization of a Potent XIAP and CIAP1 Dual Antagonist in Models of Melanoma and Leukemia by Thompson, N, Ahn, M, Chessari, G, Hearn, K, Johnson, C.N, Lewis, J, Ward, G, Williams, P, Woolford, A

Get full text

871 FRAGMENT BASED DISCOVERY AND GENOTYPIC PROFILING OF A SERIES OF DIRECT ACTING ANTIVIRAL AGENTS WITH A NOVEL MODE OF ACTION by Saalau-Bethell, S, Woodhead, A, Graham, B, Richardson, C, Murray, C, Holding, F, Chessari, G, Jhotti, H, Willems, H, Coyle, J, Verdonk, M, Vinkovic, M, Thompson, N, Williams, P, Rich, S, Hiscock, S

Get full text

592 Characterisation of novel, small molecule antagonists of XIAP, cIAP1 and cIAP2 generated by fragment based drug discovery (FBDD) by Ward, G, Chessari, G, Woolford, A, Williams, P, Hearn, K, Richardson, C, Coyle, J, Buck, I, Day, J, Tamanini, E

Get full text

289 (PB277): Pulsatile induction of the p53 pathway by MDM2 antagonist ASTX295 shows an enhanced therapeutic index in vivo by Fazal, L., Biondo, A., Ahn, M., Bevan, L., Hearn, K., Howard, S., Jueliger, S., Chessari, G., Kucia-Tran, J., Shah, A., Sims, M., Wilsher, N., Keer, H., Organesian, A., Wedge, S., Thomas, H., Zhao, Y., Newell, D., Wallis, N., Courtin, A.

Get full text

42 (PB030): A novel small-molecule CBP/p300 HAT domain inhibitor demonstrates potent in vivo activity and a favorable safety profile in preclinical species by Hearn, K., Ahn, M., Bevan, L., Chessari, G., Clark, M., Cons, B., Espana-agusti, J., Ferro, K., Howard, A., Lyons, J., Martins, V., Morgillo, C., Palmer, N., Rapti, M., Shah, A., Smyth, T., Unbekandt, M., Varshney, D., Hamlett, C.

Get full text

73 (PB061): Targeting the catalytic HAT domain of CBP/p300 for the treatment of hormone-dependent breast and prostate cancers by Hearn, K., Bevan, L., Chessari, G., Clark, M., Cons, B., Espana-agusti, J., Ferro, K., Hamlett, C., Howard, A., Lyons, J., Martins, V., Morgillo, C., Palmer, N., Rapti, M., Shah, A., Smyth, T., Unbekandt, M., Varshney, D., Ahn, M.

Get full text

28 (PB016): Identification of biomarkers predictive of response to ASTX295, a nextgeneration MDM2 antagonist, in solid tumors carrying wild-type p53 by Ahn, M., Bevan, L., Biondo, A., Brothwood, J., Chessari, G., Fazal, L., Ferraldeschi, R., Ferrari, N., Gewinner, C., Jueliger, S., Kucia-Tran, J., Saini, H., Sims, M., Thompson, N., Wallis, N., Ward, G., Lyons, J.

Get full text

Low SKP2 expression is predictive of sensitivity to an MDM2 antagonist in p53 wild-type AML by Kucia-Tran, J., Bevan, L., Chessari, G., Fazal, L., Ferrari, N., Lyons, J., Saini, H., Wallis, N., Ward, G., Ahn, M.

Get full text

Detection of Localized Water Clusters in a Charged Peptidyl Resin by Chessari, Gianni, Wieruszeski, Jean-Michel, Lippens, Guy

Get full text

573 POSTER Identification of potent, selective JAK2 inhibitors using a fragment-based screening approach by Wallis, N.G, Chessari, G, Curry, J.E, Hamlett, C, Lewry, K.A, Lyons, J, Richardson, C.J, Tisi, D, Walker, D, Woodhead, A.J

Get full text

High resolution magic angle spinning NMR in combinatorial chemistry by Lippens, G, Warrass, R, Wieruszeski, J M, Rousselot-Pailley, P, Chessari, G

“…Solid phase organic chemistry coupled with combinatorial methods promises to increase dramatically the diversity and number of small molecules available for…”
Get more information

Modeling Water Molecules in Protein−Ligand Docking Using GOLD by Verdonk, Marcel L, Chessari, Gianni, Cole, Jason C, Hartshorn, Michael J, Murray, Christopher W, Nissink, J. Willem M, Taylor, Richard D, Taylor, Robin

“…We implemented a novel approach to score water mediation and displacement in the protein−ligand docking program GOLD. The method allows water molecules to…”
Get full text

Identification of potent small molecule allosteric inhibitors of SHP2 by Hearn, K., Berdini, V., Chessari, G., Davies, T.G., Day, J.E.H., Hamlett, C., Hiscock, S., Martins, V., Muench, S., Nakatsuru, Y., Ochiiwa, H., Price, A., Rich, S., Shah, A., Shibata, Y., Shimamura, T., Smyth, T., Wallis, N.G., Wilsher, N.E., Johnson, C.N.

Get full text

Application of Fragment Screening by X-ray Crystallography to the Discovery of Aminopyridines as Inhibitors of β-Secretase by Congreve, Miles, Aharony, David, Albert, Jeffrey, Callaghan, Owen, Campbell, James, Carr, Robin A. E, Chessari, Gianni, Cowan, Suzanna, Edwards, Philip D, Frederickson, Martyn, McMenamin, Rachel, Murray, Christopher W, Patel, Sahil, Wallis, Nicola

“…Fragment-based lead discovery has been successfully applied to the aspartyl protease enzyme β-secretase (BACE-1). Fragment hits that contained an aminopyridine…”
Get full text

Application of Fragment Screening and Fragment Linking to the Discovery of Novel Thrombin Inhibitors by Howard, Nigel, Abell, Chris, Blakemore, Wendy, Chessari, Gianni, Congreve, Miles, Howard, Steven, Jhoti, Harren, Murray, Christopher W, Seavers, Lisa C. A, van Montfort, Rob L. M

“…The screening of fragments is an alternative approach to high-throughput screening for the identification of leads for therapeutic targets. Fragment hits have…”
Get full text

PS988 CHARACTERIZATION OF A NOVEL, POTENT SMALL MOLECULE MDM2 ANTAGONIST WHICH ACTIVATES WILD‐TYPE P53 AND INDUCES APOPTOSIS IN AML by Ferrari, N., Bevan, L., Castro, J., Chessari, G., Fazal, L., Howard, S., Kucia‐Tran, J., Sims, M., Ward, G., Wedge, S., Willmore, E., Ahn, M.

“…Background: In the presence of various stress signals, p53 acts as a tumor suppressor by regulating the expression of a multitude of genes to elicit cellular…”
Get full text

Trisubstituted Acridine Derivatives as Potent and Selective Telomerase Inhibitors by Harrison, R. John, Cuesta, Javier, Chessari, Gianni, Read, Martin A, Basra, Sanji K, Reszka, Anthony P, Morrell, James, Gowan, Sharon M, Incles, Christopher M, Tanious, Farial A, Wilson, W. David, Kelland, Lloyd R, Neidle, Stephen

“…The synthesis and evaluation for telomerase-inhibitory and quadruplex DNA binding properties of three related series of rationally designed trisubstituted…”
Get full text

Sequence‐specific minor groove binding by bis‐benzimidazoles: water molecules in ligand recognition by Bailly, Christian, Chessari, Gianni, Carrasco, Carolina, Joubert, Alexandra, Mann, John, Wilson, W. David, Neidle, Stephen

“…The binding of two symmetric bis‐benzimidazole compounds, 2,2‐bis‐[4′‐(3″‐dimethylamino‐1″‐propyloxy)phenyl]‐5,5‐bi‐1H‐benzimidazole and its…”
Get full text