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Page 1
Encoding BRAF inhibitor functions in protein degraders.
Miller DSJ, Voell SA, Sosič I, Proj M, Rossanese OW, Schnakenburg G, Gütschow M, Collins I, Steinebach C. Miller DSJ, et al. Among authors: rossanese ow. RSC Med Chem. 2022 May 5;13(6):731-736. doi: 10.1039/d2md00064d. eCollection 2022 Jun 22. RSC Med Chem. 2022. PMID: 35814929 Free PMC article.
Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 In Vivo.
Huckvale R, Harnden AC, Cheung KJ, Pierrat OA, Talbot R, Box GM, Henley AT, de Haven Brandon AK, Hallsworth AE, Bright MD, Akpinar HA, Miller DSJ, Tarantino D, Gowan S, Hayes A, Gunnell EA, Brennan A, Davis OA, Johnson LD, de Klerk S, McAndrew C, Le Bihan YV, Meniconi M, Burke R, Kirkin V, van Montfort RLM, Raynaud FI, Rossanese OW, Bellenie BR, Hoelder S. Huckvale R, et al. Among authors: rossanese ow. J Med Chem. 2022 Jun 23;65(12):8191-8207. doi: 10.1021/acs.jmedchem.1c02175. Epub 2022 Jun 2. J Med Chem. 2022. PMID: 35653645 Free PMC article.
Optimizing Shape Complementarity Enables the Discovery of Potent Tricyclic BCL6 Inhibitors.
Davis OA, Cheung KJ, Brennan A, Lloyd MG, Rodrigues MJ, Pierrat OA, Collie GW, Le Bihan YV, Huckvale R, Harnden AC, Varela A, Bright MD, Eve P, Hayes A, Henley AT, Carter MD, McAndrew PC, Talbot R, Burke R, van Montfort RLM, Raynaud FI, Rossanese OW, Meniconi M, Bellenie BR, Hoelder S. Davis OA, et al. Among authors: rossanese ow. J Med Chem. 2022 Jun 23;65(12):8169-8190. doi: 10.1021/acs.jmedchem.1c02174. Epub 2022 Jun 3. J Med Chem. 2022. PMID: 35657291 Free PMC article.
Discovery of Aminopiperidine Indoles That Activate the Guanine Nucleotide Exchange Factor SOS1 and Modulate RAS Signaling.
Abbott JR, Hodges TR, Daniels RN, Patel PA, Kennedy JP, Howes JE, Akan DT, Burns MC, Sai J, Sobolik T, Beesetty Y, Lee T, Rossanese OW, Phan J, Waterson AG, Fesik SW. Abbott JR, et al. Among authors: rossanese ow. J Med Chem. 2018 Jul 26;61(14):6002-6017. doi: 10.1021/acs.jmedchem.8b00360. Epub 2018 Jul 11. J Med Chem. 2018. PMID: 29856609
Discovery and Structure-Based Optimization of Benzimidazole-Derived Activators of SOS1-Mediated Nucleotide Exchange on RAS.
Hodges TR, Abbott JR, Little AJ, Sarkar D, Salovich JM, Howes JE, Akan DT, Sai J, Arnold AL, Browning C, Burns MC, Sobolik T, Sun Q, Beesetty Y, Coker JA, Scharn D, Stadtmueller H, Rossanese OW, Phan J, Waterson AG, McConnell DB, Fesik SW. Hodges TR, et al. Among authors: rossanese ow. J Med Chem. 2018 Oct 11;61(19):8875-8894. doi: 10.1021/acs.jmedchem.8b01108. Epub 2018 Sep 28. J Med Chem. 2018. PMID: 30205005 Free PMC article.
Achieving In Vivo Target Depletion through the Discovery and Optimization of Benzimidazolone BCL6 Degraders.
Bellenie BR, Cheung KJ, Varela A, Pierrat OA, Collie GW, Box GM, Bright MD, Gowan S, Hayes A, Rodrigues MJ, Shetty KN, Carter M, Davis OA, Henley AT, Innocenti P, Johnson LD, Liu M, de Klerk S, Le Bihan YV, Lloyd MG, McAndrew PC, Shehu E, Talbot R, Woodward HL, Burke R, Kirkin V, van Montfort RLM, Raynaud FI, Rossanese OW, Hoelder S. Bellenie BR, et al. Among authors: rossanese ow. J Med Chem. 2020 Apr 23;63(8):4047-4068. doi: 10.1021/acs.jmedchem.9b02076. Epub 2020 Apr 10. J Med Chem. 2020. PMID: 32275432 Free PMC article.
Discovery of Dabrafenib: A Selective Inhibitor of Raf Kinases with Antitumor Activity against B-Raf-Driven Tumors.
Rheault TR, Stellwagen JC, Adjabeng GM, Hornberger KR, Petrov KG, Waterson AG, Dickerson SH, Mook RA Jr, Laquerre SG, King AJ, Rossanese OW, Arnone MR, Smitheman KN, Kane-Carson LS, Han C, Moorthy GS, Moss KG, Uehling DE. Rheault TR, et al. Among authors: rossanese ow. ACS Med Chem Lett. 2013 Feb 7;4(3):358-62. doi: 10.1021/ml4000063. eCollection 2013 Mar 14. ACS Med Chem Lett. 2013. PMID: 24900673 Free PMC article.
Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5-MYC Protein-Protein Interaction.
Macdonald JD, Chacón Simon S, Han C, Wang F, Shaw JG, Howes JE, Sai J, Yuh JP, Camper D, Alicie BM, Alvarado J, Nikhar S, Payne W, Aho ER, Bauer JA, Zhao B, Phan J, Thomas LR, Rossanese OW, Tansey WP, Waterson AG, Stauffer SR, Fesik SW. Macdonald JD, et al. Among authors: rossanese ow. J Med Chem. 2019 Dec 26;62(24):11232-11259. doi: 10.1021/acs.jmedchem.9b01411. Epub 2019 Dec 5. J Med Chem. 2019. PMID: 31724864 Free PMC article.
Discovery of Quinazolines That Activate SOS1-Mediated Nucleotide Exchange on RAS.
Abbott JR, Patel PA, Howes JE, Akan DT, Kennedy JP, Burns MC, Browning CF, Sun Q, Rossanese OW, Phan J, Waterson AG, Fesik SW. Abbott JR, et al. Among authors: rossanese ow. ACS Med Chem Lett. 2018 Aug 8;9(9):941-946. doi: 10.1021/acsmedchemlett.8b00296. eCollection 2018 Sep 13. ACS Med Chem Lett. 2018. PMID: 30258545 Free PMC article.
Into Deep Water: Optimizing BCL6 Inhibitors by Growing into a Solvated Pocket.
Lloyd MG, Huckvale R, Cheung KJ, Rodrigues MJ, Collie GW, Pierrat OA, Gatti Iou M, Carter M, Davis OA, McAndrew PC, Gunnell E, Le Bihan YV, Talbot R, Henley AT, Johnson LD, Hayes A, Bright MD, Raynaud FI, Meniconi M, Burke R, van Montfort RLM, Rossanese OW, Bellenie BR, Hoelder S. Lloyd MG, et al. Among authors: rossanese ow. J Med Chem. 2021 Dec 9;64(23):17079-17097. doi: 10.1021/acs.jmedchem.1c00946. Epub 2021 Nov 30. J Med Chem. 2021. PMID: 34846884 Free PMC article.
43 results