Main Menu

Publications

Publications Highlights View all by category

Types of Publications


Journal Articles

Pierrat, O.A. Liu, M. Collie, G.W. Shetty, K. Rodrigues, M.J. Le Bihan, Y.-. Gunnell, E.A. McAndrew, P.C. Stubbs, M. Rowlands, M.G. Yahya, N. Shehu, E. Talbot, R. Pickard, L. Bellenie, B.R. Cheung, K.-. 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. (2022). Discovering cell-active BCL6 inhibitors: effectively combining biochemical HTS with multiple biophysical techniques, X-ray crystallography and cell-based assays. Sci rep, Vol.12 (1), p. 18633.  show abstract

Miller, D.S. Voell, S.A. Sosič, I. Proj, M. Rossanese, O.W. Schnakenburg, G. Gütschow, M. Collins, I. Steinebach, C. (2022). Encoding BRAF inhibitor functions in protein degraders. Rsc med chem, Vol.13 (6), pp. 731-736.  show abstract

Davis, O.A. Cheung, K.-. Brennan, A. Lloyd, M.G. Rodrigues, M.J. Pierrat, O.A. Collie, G.W. Le Bihan, Y.-. 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. Raynaud, F.I. Rossanese, O.W. Meniconi, M. Bellenie, B.R. Hoelder, S. (2022). Optimizing Shape Complementarity Enables the Discovery of Potent Tricyclic BCL6 Inhibitors. J med chem, Vol.65 (12), pp. 8169-8190.  show abstract

Huckvale, R. Harnden, A.C. Cheung, K.-. Pierrat, O.A. Talbot, R. Box, G.M. Henley, A.T. de Haven Brandon, A.K. Hallsworth, A.E. Bright, M.D. Akpinar, H.A. Miller, D.S. Tarantino, D. Gowan, S. Hayes, A. Gunnell, E.A. Brennan, A. Davis, O.A. Johnson, L.D. de Klerk, S. McAndrew, C. Le Bihan, Y.-. Meniconi, M. Burke, R. Kirkin, V. van Montfort, R.L. Raynaud, F.I. Rossanese, O.W. Bellenie, B.R. Hoelder, S. (2022). Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 In Vivo. J med chem, Vol.65 (12), pp. 8191-8207.  show abstract

Walters, Z.S. Aladowicz, E. Villarejo-Balcells, B. Nugent, G. Selfe, J.L. Eve, P. Blagg, J. Rossanese, O. Shipley, J. (2021). Role for the Histone Demethylase KDM4B in Rhabdomyosarcoma via CDK6 and CCNA2: Compensation by KDM4A and Apoptotic Response of Targeting Both KDM4B and KDM4A. Cancers (basel), Vol.13 (7).  show abstract

Lloyd, M.G. Huckvale, R. Cheung, K.-. 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.-. Talbot, R. Henley, A.T. Johnson, L.D. Hayes, A. Bright, M.D. Raynaud, F.I. Meniconi, M. Burke, R. van Montfort, R.L. Rossanese, O.W. Bellenie, B.R. Hoelder, S. (2021). Into Deep Water: Optimizing BCL6 Inhibitors by Growing into a Solvated Pocket. J med chem, Vol.64 (23), pp. 17079-17097.  show abstract

Bellenie, B.R. Cheung, K.-. 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.-. Lloyd, M.G. McAndrew, P.C. Shehu, E. Talbot, R. Woodward, H.L. Burke, R. Kirkin, V. van Montfort, R.L. Raynaud, F.I. Rossanese, O.W. Hoelder, S. (2020). Achieving In Vivo Target Depletion through the Discovery and Optimization of Benzimidazolone BCL6 Degraders. J med chem, Vol.63 (8), pp. 4047-4068.  show abstract

Le Bihan, Y.-. Lanigan, R.M. Atrash, B. McLaughlin, M.G. Velupillai, S. Malcolm, A.G. England, K.S. Ruda, G.F. Mok, N.Y. Tumber, A. Tomlin, K. Saville, H. Shehu, E. McAndrew, C. Carmichael, L. Bennett, J.M. Jeganathan, F. Eve, P. Donovan, A. Hayes, A. Wood, F. Raynaud, F.I. Fedorov, O. Brennan, P.E. Burke, R. van Montfort, R.L. Rossanese, O.W. Blagg, J. Bavetsias, V. (2019). 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. Eur j med chem, Vol.177, pp. 316-337.  show abstract

Macdonald, J.D. Chacón Simon, S. Han, C. Wang, F. Shaw, J.G. Howes, J.E. Sai, J. Yuh, J.P. Camper, D. Alicie, B.M. Alvarado, J. Nikhar, S. Payne, W. Aho, E.R. Bauer, J.A. Zhao, B. Phan, J. Thomas, L.R. Rossanese, O.W. Tansey, W.P. Waterson, A.G. Stauffer, S.R. Fesik, S.W. (2019). Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5-MYC Protein-Protein Interaction. J med chem, Vol.62 (24), pp. 11232-11259.  show abstract

Burns, M.C. Howes, J.E. Sun, Q. Little, A.J. Camper, D.V. Abbott, J.R. Phan, J. Lee, T. Waterson, A.G. Rossanese, O.W. Fesik, S.W. (2018). High-throughput screening identifies small molecules that bind to the RAS:SOS:RAS complex and perturb RAS signaling. Anal biochem, Vol.548, pp. 44-52.  show abstract

Howes, J.E. Akan, D.T. Burns, M.C. Rossanese, O.W. Waterson, A.G. Fesik, S.W. (2018). Small Molecule-Mediated Activation of RAS Elicits Biphasic Modulation of Phospho-ERK Levels that Are Regulated through Negative Feedback on SOS1. Mol cancer ther, Vol.17 (5), pp. 1051-1060.  show abstract

Hodges, T.R. Abbott, J.R. Little, A.J. Sarkar, D. Salovich, J.M. Howes, J.E. Akan, D.T. Sai, J. Arnold, A.L. Browning, C. Burns, M.C. Sobolik, T. Sun, Q. Beesetty, Y. Coker, J.A. Scharn, D. Stadtmueller, H. Rossanese, O.W. Phan, J. Waterson, A.G. McConnell, D.B. Fesik, S.W. (2018). Discovery and Structure-Based Optimization of Benzimidazole-Derived Activators of SOS1-Mediated Nucleotide Exchange on RAS. J med chem, Vol.61 (19), pp. 8875-8894.  show abstract

Wang, F. Jeon, K.O. Salovich, J.M. Macdonald, J.D. Alvarado, J. Gogliotti, R.D. Phan, J. Olejniczak, E.T. Sun, Q. Wang, S. Camper, D. Yuh, J.P. Shaw, J.G. Sai, J. Rossanese, O.W. Tansey, W.P. Stauffer, S.R. Fesik, S.W. (2018). Discovery of Potent 2-Aryl-6,7-dihydro-5 H-pyrrolo[1,2- a]imidazoles as WDR5-WIN-Site Inhibitors Using Fragment-Based Methods and Structure-Based Design. J med chem, Vol.61 (13), pp. 5623-5642.  show abstract

Abbott, J.R. Patel, P.A. Howes, J.E. Akan, D.T. Kennedy, J.P. Burns, M.C. Browning, C.F. Sun, Q. Rossanese, O.W. Phan, J. Waterson, A.G. Fesik, S.W. (2018). Discovery of Quinazolines That Activate SOS1-Mediated Nucleotide Exchange on RAS. Acs med chem lett, Vol.9 (9), pp. 941-946.  show abstract

Shaw, S. Bian, Z. Zhao, B. Tarr, J.C. Veerasamy, N. Jeon, K.O. Belmar, J. Arnold, A.L. Fogarty, S.A. Perry, E. Sensintaffar, J.L. Camper, D.V. Rossanese, O.W. Lee, T. Olejniczak, E.T. Fesik, S.W. (2018). Optimization of Potent and Selective Tricyclic Indole Diazepinone Myeloid Cell Leukemia-1 Inhibitors Using Structure-Based Design. J med chem, Vol.61 (6), pp. 2410-2421.  show abstract

Abbott, J.R. Hodges, T.R. Daniels, R.N. Patel, P.A. Kennedy, J.P. Howes, J.E. Akan, D.T. Burns, M.C. Sai, J. Sobolik, T. Beesetty, Y. Lee, T. Rossanese, O.W. Phan, J. Waterson, A.G. Fesik, S.W. (2018). Discovery of Aminopiperidine Indoles That Activate the Guanine Nucleotide Exchange Factor SOS1 and Modulate RAS Signaling. J med chem, Vol.61 (14), pp. 6002-6017.  show abstract

Lee, T. Bian, Z. Zhao, B. Hogdal, L.J. Sensintaffar, J.L. Goodwin, C.M. Belmar, J. Shaw, S. Tarr, J.C. Veerasamy, N. Matulis, S.M. Koss, B. Fischer, M.A. Arnold, A.L. Camper, D.V. Browning, C.F. Rossanese, O.W. Budhraja, A. Opferman, J. Boise, L.H. Savona, M.R. Letai, A. Olejniczak, E.T. Fesik, S.W. (2017). Discovery and biological characterization of potent myeloid cell leukemia-1 inhibitors. Febs lett, Vol.591 (1), pp. 240-251.  show abstract

Hatch, S.B. Yapp, C. Montenegro, R.C. Savitsky, P. Gamble, V. Tumber, A. Ruda, G.F. Bavetsias, V. Fedorov, O. Atrash, B. Raynaud, F. Lanigan, R. Carmichael, L. Tomlin, K. Burke, R. Westaway, S.M. Brown, J.A. Prinjha, R.K. Martinez, E.D. Oppermann, U. Schofield, C.J. Bountra, C. Kawamura, A. Blagg, J. Brennan, P.E. Rossanese, O. Müller, S. (2017). Assessing histone demethylase inhibitors in cells: lessons learned. Epigenetics chromatin, Vol.10, p. 9.  show abstract

Pelz, N.F. Bian, Z. Zhao, B. Shaw, S. Tarr, J.C. Belmar, J. Gregg, C. Camper, D.V. Goodwin, C.M. Arnold, A.L. Sensintaffar, J.L. Friberg, A. Rossanese, O.W. Lee, T. Olejniczak, E.T. Fesik, S.W. (2016). Discovery of 2-Indole-acylsulfonamide Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods. J med chem, Vol.59 (5), pp. 2054-2066.  show abstract

Kanu, N. Cerone, M.A. Goh, G. Zalmas, L.-. Bartkova, J. Dietzen, M. McGranahan, N. Rogers, R. Law, E.K. Gromova, I. Kschischo, M. Walton, M.I. Rossanese, O.W. Bartek, J. Harris, R.S. Venkatesan, S. Swanton, C. (2016). DNA replication stress mediates APOBEC3 family mutagenesis in breast cancer. Genome biol, Vol.17 (1), p. 185.  show abstract

Patrone, J.D. Pelz, N.F. Bates, B.S. Souza-Fagundes, E.M. Vangamudi, B. Camper, D.V. Kuznetsov, A.G. Browning, C.F. Feldkamp, M.D. Frank, A.O. Gilston, B.A. Olejniczak, E.T. Rossanese, O.W. Waterson, A.G. Chazin, W.J. Fesik, S.W. (2016). Identification and Optimization of Anthranilic Acid Based Inhibitors of Replication Protein A. Chemmedchem, Vol.11 (8), pp. 893-899.  show abstract

Goodwin, C.M. Rossanese, O.W. Olejniczak, E.T. Fesik, S.W. (2015). Myeloid cell leukemia-1 is an important apoptotic survival factor in triple-negative breast cancer. Cell death differ, Vol.22 (12), pp. 2098-2106.  show abstract

Waterson, A.G. Kennedy, J.P. Patrone, J.D. Pelz, N.F. Feldkamp, M.D. Frank, A.O. Vangamudi, B. Souza-Fagundes, E.M. Rossanese, O.W. Chazin, W.J. Fesik, S.W. (2015). Diphenylpyrazoles as replication protein a inhibitors. Acs med chem lett, Vol.6 (2), pp. 140-145.  show abstract

Burke, J.P. Bian, Z. Shaw, S. Zhao, B. Goodwin, C.M. Belmar, J. Browning, C.F. Vigil, D. Friberg, A. Camper, D.V. Rossanese, O.W. Lee, T. Olejniczak, E.T. Fesik, S.W. (2015). Discovery of tricyclic indoles that potently inhibit Mcl-1 using fragment-based methods and structure-based design. J med chem, Vol.58 (9), pp. 3794-3805.  show abstract

Bhave, M. Papanikou, E. Iyer, P. Pandya, K. Jain, B.K. Ganguly, A. Sharma, C. Pawar, K. Austin, J. Day, K.J. Rossanese, O.W. Glick, B.S. Bhattacharyya, D. (2014). Golgi enlargement in Arf-depleted yeast cells is due to altered dynamics of cisternal maturation. J cell sci, Vol.127 (Pt 1), pp. 250-257.  show abstract

Burns, M.C. Sun, Q. Daniels, R.N. Camper, D. Kennedy, J.P. Phan, J. Olejniczak, E.T. Lee, T. Waterson, A.G. Rossanese, O.W. Fesik, S.W. (2014). Approach for targeting Ras with small molecules that activate SOS-mediated nucleotide exchange. Proc natl acad sci u s a, Vol.111 (9), pp. 3401-3406.  show abstract

Frank, A.O. Vangamudi, B. Feldkamp, M.D. Souza-Fagundes, E.M. Luzwick, J.W. Cortez, D. Olejniczak, E.T. Waterson, A.G. Rossanese, O.W. Chazin, W.J. Fesik, S.W. (2014). Discovery of a potent stapled helix peptide that binds to the 70N domain of replication protein A. J med chem, Vol.57 (6), pp. 2455-2461.  show abstract

Patrone, J.D. Kennedy, J.P. Frank, A.O. Feldkamp, M.D. Vangamudi, B. Pelz, N.F. Rossanese, O.W. Waterson, A.G. Chazin, W.J. Fesik, S.W. (2013). Discovery of Protein-Protein Interaction Inhibitors of Replication Protein A. Acs med chem lett, Vol.4 (7), pp. 601-605.  show abstract

Rheault, T.R. Stellwagen, J.C. Adjabeng, G.M. Hornberger, K.R. Petrov, K.G. Waterson, A.G. Dickerson, S.H. Mook, R.A. Laquerre, S.G. King, A.J. Rossanese, O.W. Arnone, M.R. Smitheman, K.N. Kane-Carson, L.S. Han, C. Moorthy, G.S. Moss, K.G. Uehling, D.E. (2013). Discovery of Dabrafenib: A Selective Inhibitor of Raf Kinases with Antitumor Activity against B-Raf-Driven Tumors. Acs med chem lett, Vol.4 (3), pp. 358-362.  show abstract

Frank, A.O. Feldkamp, M.D. Kennedy, J.P. Waterson, A.G. Pelz, N.F. Patrone, J.D. Vangamudi, B. Camper, D.V. Rossanese, O.W. Chazin, W.J. Fesik, S.W. (2013). Discovery of a potent inhibitor of replication protein a protein-protein interactions using a fragment-linking approach. J med chem, Vol.56 (22), pp. 9242-9250.  show abstract

Souza-Fagundes, E.M. Frank, A.O. Feldkamp, M.D. Dorset, D.C. Chazin, W.J. Rossanese, O.W. Olejniczak, E.T. Fesik, S.W. (2012). A high-throughput fluorescence polarization anisotropy assay for the 70N domain of replication protein A. Anal biochem, Vol.421 (2), pp. 742-749.  show abstract

Sun, Q. Burke, J.P. Phan, J. Burns, M.C. Olejniczak, E.T. Waterson, A.G. Lee, T. Rossanese, O.W. Fesik, S.W. (2012). Discovery of small molecules that bind to K-Ras and inhibit Sos-mediated activation. Angew chem int ed engl, Vol.51 (25), pp. 6140-6143.

Stellwagen, J.C. Adjabeng, G.M. Arnone, M.R. Dickerson, S.H. Han, C. Hornberger, K.R. King, A.J. Mook, R.A. Petrov, K.G. Rheault, T.R. Rominger, C.M. Rossanese, O.W. Smitheman, K.N. Waterson, A.G. Uehling, D.E. (2011). Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup. Bioorg med chem lett, Vol.21 (15), pp. 4436-4440.  show abstract

Losev, E. Papanikou, E. Rossanese, O.W. Glick, B.S. (2008). Cdc1p is an endoplasmic reticulum-localized putative lipid phosphatase that affects Golgi inheritance and actin polarization by activating Ca2+ signaling. Mol cell biol, Vol.28 (10), pp. 3336-3343.  show abstract

Patel, J.C. Rossanese, O.W. Galán, J.E. (2005). The functional interface between Salmonella and its host cell: opportunities for therapeutic intervention. Trends pharmacol sci, Vol.26 (11), pp. 564-570.  show abstract

Jiang, X. Rossanese, O.W. Brown, N.F. Kujat-Choy, S. Galán, J.E. Finlay, B.B. Brumell, J.H. (2004). The related effector proteins SopD and SopD2 from Salmonella enterica serovar Typhimurium contribute to virulence during systemic infection of mice. Mol microbiol, Vol.54 (5), pp. 1186-1198.  show abstract

Rossanese, O.W. Reinke, C.A. Bevis, B.J. Hammond, A.T. Sears, I.B. O'Connor, J. Glick, B.S. (2001). A role for actin, Cdc1p, and Myo2p in the inheritance of late Golgi elements in Saccharomyces cerevisiae. J cell biol, Vol.153 (1), pp. 47-62.  show abstract

Rossanese, O.W. Glick, B.S. (2001). Deconstructing Golgi inheritance. Traffic, Vol.2 (9), pp. 589-596.  show abstract

Rossanese, O.W. Soderholm, J. Bevis, B.J. Sears, I.B. O'Connor, J. Williamson, E.K. Glick, B.S. (1999). Golgi structure correlates with transitional endoplasmic reticulum organization in Pichia pastoris and Saccharomyces cerevisiae. J cell biol, Vol.145 (1), pp. 69-81.  show abstract

Séron, K. Tieaho, V. Prescianotto-Baschong, C. Aust, T. Blondel, M.O. Guillaud, P. Devilliers, G. Rossanese, O.W. Glick, B.S. Riezman, H. Keränen, S. Haguenauer-Tsapis, R. (1998). A yeast t-SNARE involved in endocytosis. Mol biol cell, Vol.9 (10), pp. 2873-2889.  show abstract

Sears, I.B. O'Connor, J. Rossanese, O.W. Glick, B.S. (1998). A versatile set of vectors for constitutive and regulated gene expression in Pichia pastoris. Yeast, Vol.14 (8), pp. 783-790.  show abstract

In this section

Research Overview Publications