Publications RSS feed from the library

Achieving in vivo target depletion through the discovery and optimization of benzimidazolone BCL6 degraders

Bellenie B.R., Cheung K.M.J., Varela A., Pierrat O.A., Collie G.W., Box G.M., Bright M.D., Gowan S., Hayes A., Rodrigues M.J., Shetty K.N., Carter M., Davis O.A., Henley A.T., Innocenti P., Johnson L.D., Liu M., de Klerk S., Le Bihan Y.V., Lloyd M.G., McAndrew P.C., Shehu E., Talbot R., Woodward H.L., Burke R., Kirkin V., van Montfort R.L.M., Raynaud F.I., Rossanese O.W., Hoelder S.,
Journal of Medicinal Chemistry 63, 4047-4068 (2020)

Discovery of BAY-985, a highly selective TBK1/IKKε inhibitor

Lefranc J., Schulze V.K., Hillig R.C., Briem H., Prinz F., Mengel A., Heinrich T., Balint J., Rengachari S., Irlbacher H., Stöckigt D., Bömer U., Bader B., Gradl S.N., Nising C.F., von Nussbaum F., Mumberg D., Panne D., Wengner A.M.,
Journal of Medicinal Chemistry 63, 601-612 (2020)

Recurrent activating mutations of PPARγ associated with luminal bladder tumors

Rochel N., Krucker C., Coutos-Thevenot L., Osz J., Zhang R., Guyon E., Zita W., Vanthong S., Alba Hernandez O., Bourguet M., Al Badawy K., Dufour F., Peluso-Iltis C., Heckler-Beji S., Dejaegere A., Kamoun A., de Reynies A., Neuzillet Y., Rebouissou S., Béraud C., Lang H., Massfelder T., Allory Y., Cianférani S., Stote R.H., Radvanyi F., Bernard-Pierrot I.,
Nature Communications 10, 253-1-253-12 (2019)

2-Benzylpiperazine: A new scaffold for potent human carbonic anhydrase inhibitors. Synthesis, enzyme inhibition, enantioselectivity, computational and crystallographic studies and in vivo activity for a new class of intraocular pressure lowering agents

Chiaramonte N., Bua S., Ferraroni M., Nocentini A., Bonardi A., Bartolucci G., Durante M., Lucarini L., Chiapponi D., Dei S., Manetti D., Teodori E., Gratteri P., Masini E., Supuran C.T., Romanelli M.N.,
European Journal of Medicinal Chemistry 151, 363-375 (2018)

Phosphorylation of Parkin at serine 65 is essential for its activation in vivo

McWilliams T.G., Barini E., Pohjolan-Pirhonen R., Brooks S.P., Singh F., Burel S., Balk K., Kumar A., Montava-Garriga L., Prescott A.R., Hassoun S.M., Mouton-Liger F., Ball G., Hills R., Knebel A., Ulusoy A., Di Monte D.A., Tamjar J., Antico O., Fears K., Smith L., Brambilla R., Palin E., Valori M., Eerola-Rautio J., Tienari P., Corti O., Dunnett S.B., Ganley I.G., Suomalainen A., Muqit M.M.K.,
Open Biology 8, 180108-1-180108-18 (2018)

Discovery of a chemical probe bisamide (CCT251236): An orally bioavailable efficacious pirin ligand from a heat shock transcription factor 1 (HSF1) phenotypic screen

Cheeseman M.D., Chessum N.E.A., Rye C.S., Pasqua A.E., Tucker M.J., Wilding B., Evans L.E., Lepri S., Richards M., Sharp S.Y., Ali S., Rowlands M., O'Fee L., Miah A., Hayes A., Henley A.T., Powers M., te Poele R., De Billy E., Pellegrino L., Raynaud F., Burke R., van Montfort R.L.M., Eccles S.A., Workman P., Jones K.,
Journal of Medicinal Chemistry 60, 180-201 (2017)

De novo active sites for resurrected Precambrian enzymes

Risso V.A., Martínez-Rodríguez S., Candel A.M., Krüger D.M., Pantoja-Uceda D., Ortega-Muñoz M., Santoyo-González F., Gaucher E.A., Kamerlin S.C.L., Bruix M., Gavira J.A., Sánchez-Ruiz J.M.,
Nature Communications 8, 16113-1-16113-13 (2017)