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Optimizing shape complementarity enables the discovery of potent tricyclic BCL6 inhibitors

Davis O.A., Cheung K.M.J., Brennan A., Lloyd M.G., Rodrigues M.J., Pierrat O.A., Collie G.W., Le Bihan Y.V., Huckvale R., Harnden A.C., Varela A., Bright M.D., Eve P., Hayes A., Henley A.T., Carter M.D., McAndrew P.C., Talbot R., Burke R., van Montfort R.L.M., Raynaud F.I., Rossanese O.W., Meniconi M., Bellenie B.R., Hoelder S.,
Journal of Medicinal Chemistry 65, 8169-8190 (2022)

Discovery of BLU-945, a reversible, potent, and wild-type-sparing next-generation EGFR mutant inhibitor for treatment-resistant non-small-cell lung cancer

Eno M.S., Brubaker J.D., Campbell J.E., De Savi C., Guzi T.J., Williams B.D., Wilson D., Wilson K., Brooijmans N., Kim J., Özen A., Perola E., Hsieh J., Brown V., Fetalvero K., Garner A., Zhang Z., Stevison F., Woessner R., Singh J., Timsit Y., Kinkema C., Medendorp C., Lee C., Albayya F., Zalutskaya A., Schalm S., Dineen T.A.,
Journal of Medicinal Chemistry 65, 9662-9677 (2022)

A broadly neutralizing monoclonal antibody overcomes the mutational landscape of emerging SARS-CoV-2 variants of concern

Parray H.A., Narayanan N., Garg S., Rizvi Z.A., Shrivastava T., Kushwaha S., Singh J., Murugavelu P., Anantharaj A., Mehdi F., Raj N., Singh S., Dandotiya J., Lukose A., Jamwal D., Kumar S., Chiranjivi A., Dhyani S., Mishra N., Jakhar K., Sonar S., Panchal A.K., Tripathy M.R., Chowdhury S.R., Ahmed S., Samal S., Mani S., Bhattacharyya S., Das S., Sinha S., Luthra K., Batra G., Sehgal D., Medigeshi G.R., Sharma C., Awasthi A., Garg P.K., Nair D.T., Kumar R.,
PLoS Pathogens 18, e1010994-1-e1010994-20 (2022)

Discovering cell-active BCL6 inhibitors: Effectively combining biochemical HTS with multiple biophysical techniques, X-ray crystallography and cell-based assays

Pierrat O.A., Liu M., Collie G.W., Shetty K., Rodrigues M.J., Le Bihan Y.V., Gunnell E.A., McAndrew P.C., Stubbs M., Rowlands M.G., Yahya N., Shehu E., Talbot R., Pickard L., Bellenie B.R., Cheung K.M.J., Drouin L., Innocenti P., Woodward H., Davis O.A., Lloyd M.G., Varela A., Huckvale R., Broccatelli F., Carter M., Galiwango D., Hayes A., Raynaud F.I., Bryant C., Whittaker S., Rossanese O.W., Hoelder S., Burke R., van Montfort R.L.M.,
Scientific Reports 12, 18633-1-18633-15 (2022)

PHF3 regulates neuronal gene expression through the Pol II CTD reader domain SPOC

Appel L.M., Franke V., Bruno M., Grishkovskaya I., Kasiliauskaite A., Kaufmann T., Schoeberl U.E., Puchinger M.G., Kostrhon S., Ebenwaldner C., Sebesta M., Beltzung E., Mechtler K., Lin G., Vlasova A., Leeb M., Pavri R., Stark A., Akalin A., Stefl R., Bernecky C., Djinovic-Carugo K., Slade D.,
Nature Communications 12, 6078-1-6078-24 (2021)

Cross-reactive SARS-CoV-2 neutralizing antibodies from deep mining of early patient responses

Bullen G., Galson J.D., Hall G., Villar P., Moreels L., Ledsgaard L., Mattiuzzo G., Bentley E.M., Masters E.W., Tang D., Millett S., Tongue D., Brown R., Diamantopoulos I., Parthiban K., Tebbutt C., Leah R., Chaitanya K., Ergueta-Carballo S., Pazeraitis D., Surade S.B., Ashiru O., Crippa L., Cowan R., Bowler M.W., Campbell J.I., Lee W.Y.J., Carr M.D., Matthews D., Pfeffer P., Hufton S.E., Sawmynaden K., Osbourn J., McCafferty J., Karatt-Vellatt A.,
Frontiers in Immunology 12, 678570-1-678570-16 (2021)

Discovery of GSK251: A highly potent, highly selective, orally bioavailable inhibitor of PI3Kδ with a novel binding mode

Down K., Amour A., Anderson N.A., Barton N., Campos S., Cannons E.P., Clissold C., Convery M.A., Coward J.J., Doyle K., Duempelfeld B., Edwards C.D., Goldsmith M.D., Krause J., Mallett D.N., McGonagle G.A., Patel V.K., Rowedder J., Rowland P., Sharpe A., Sriskantharajah S., Thomas D.A., Thomson D.W., Uddin S., Hamblin J.N., Hessel E.M.,
Journal of Medicinal Chemistry 64, 13780-13792 (2021)

Into deep water: Optimizing BCL6 inhibitors by growing into a solvated pocket

Lloyd M.G., Huckvale R., Cheung K.M.J., Rodrigues M.J., Collie G.W., Pierrat O.A., Gatti Iou M., Carter M., Davis O.A., McAndrew P.C., Gunnell E., Le Bihan Y.V., Talbot R., Henley A.T., Johnson L.D., Hayes A., Bright M.D., Raynaud F.I., Meniconi M., Burke R., van Montfort R.L.M., Rossanese O.W., Bellenie B.R., Hoelder S.,
Journal of Medicinal Chemistry 64, 17079-17097 (2021)

Structure-based exploration of selectivity for ATM inhibitors in Huntington's disease

Van de Poël A., Toledo-Sherman L., Breccia P., Cachope R., Bate J.R., Angulo-Herrera I., Wishart G., Matthews K.L., Martin S.L., Peacock M., Barnard A., Cox H.C., Jones G., McAllister G., Vater H., Esmieu W., Clissold C., Lamers M., Leonard P., Jarvis R.E., Blackaby W., Eznarriaga M., Lazari O., Yates D., Rose M., Jang S.W., Muñoz-Sanjuan I., Dominguez C.,
Journal of Medicinal Chemistry 64, 5018-5036 (2021)

Metabolic fate of human immunoactive sterols in Mycobacterium tuberculosis

Varaksa T., Bukhdruker S., Grabovec I., Marin E., Kavaleuski A., Gusach A., Kovalev K., Maslov I., Luginina A., Zabelskii D., Astashkin R., Shevtsov M., Smolskaya S., Kavaleuskaya A., Shabunya P., Baranovsky A., Dolgopalets V., Charnou Y., Savachka A., Litvinovskaya R., Hurski A., Shevchenko E., Rogachev A., Mishin A., Gordeliy V., Gabrielian A., Hurt D.E., Nikonenko B., Majorov K., Apt A., Rosenthal A., Gilep A., Borshchevskiy V., Strushkevich N.,
Journal of Molecular Biology 433, 166763-1-166763-16 (2021)

Discovery of a potent dual inhibitor of acetylcholinesterase and butyrylcholinesterase with antioxidant activity that alleviates Alzheimer-like pathology in old APP/PS1 mice

Viayna E., Coquelle N., Cieslikiewicz-Bouet M., Cisternas P., Oliva C.A., Sánchez-López E., Ettcheto M., Bartolini M., De Simone A., Ricchini M., Rendina M., Pons M., Firuzi O., Pérez B., Saso L., Andrisano V., Nachon F., Brazzolotto X., Garciá M.L., Camins A., Silman I., Jean L., Inestrosa N.C., Colletier J.P., Renard P.Y., Muñoz-Torrero D.,
Journal of Medicinal Chemistry 64, 812-839 (2021)

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)

Deep mining of early antibody response in COVID-19 patients yields potent neutralisers and reveals high level of convergence

Bullen G., Galson J.D., Villar P., Moreels L., Ledsgaard L., Mattiuzzo G., Hall G., Bentley E.M., Masters E.W., Tang D., Millett S., Tongue D., Brown R., Diamantopoulos I., Parthiban K., Tebbutt C., Leah R., Chaitanya K., Pazeraitis D., Surade S.B., Ashiru O., Crippa L., Cowan R., Bowler M.W., Campbell J.I., Lee W., Carr M.D., Matthews D., Pfeffer P., Hufton S.E., Sawmynaden K., Osbourn J., McCafferty J., Karatt-Vellatt A.,
BioRxiv , epub (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)

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