Swen Hoelder - Publications

1998- University of California, Berkeley, Berkeley, CA 

25 high-probability publications. We are testing a new system for linking publications to authors. You can help! If you notice any inaccuracies, please sign in and mark papers as correct or incorrect matches. If you identify any major omissions or other inaccuracies in the publication list, please let us know.

Year Citation  Score
2020 Darby JF, Vidler LR, Simpson PJ, Al-Lazikani B, Matthews SJ, Sharp SY, Pearl LH, Hoelder S, Workman P. Solution structure of the Hop TPR2A domain and investigation of target druggability by NMR, biochemical and in silico approaches. Scientific Reports. 10: 16000. PMID 32994435 DOI: 10.1038/s41598-020-71969-w  0.48
2020 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, ... ... Hoelder S, et al. Achieving Target Depletion through the Discovery and Optimization of Benzimidazolone BCL6 Degraders. Journal of Medicinal Chemistry. PMID 32275432 DOI: 10.1021/acs.jmedchem.9b02076  0.8
2019 Anderhub SJ, Mak GW, Gurden MD, Faisal A, Drosopoulos K, Walsh K, Woodward HL, Innocenti P, Westwood IM, Naud S, Hayes A, Theofani E, Filosto S, Saville H, Burke R, ... ... Hoelder S, et al. High Proliferation Rate and a Compromised Spindle Assembly Checkpoint Confers Sensitivity to the MPS1 Inhibitor BOS172722 in Triple-Negative Breast Cancers. Molecular Cancer Therapeutics. 18: 1696-1707. PMID 31575759 DOI: 10.1158/1535-7163.MCT-18-1203  0.8
2019 Watts E, Heidenreich D, Tucker E, Raab M, Strebhardt K, Chesler L, Knapp S, Bellenie B, Hoelder S. Designing Dual Inhibitors of Anaplastic Lymphoma Kinase (ALK) and Bromodomain-4 (BRD4) by Tuning Kinase Selectivity. Journal of Medicinal Chemistry. PMID 30789735 DOI: 10.1021/acs.jmedchem.8b01947  0.48
2018 Woodward HL, Innocenti P, Cheung KJ, Hayes A, Roberts J, Henley AT, Faisal A, Mak GW, Box G, Westwood IM, Cronin N, Carter M, Valenti M, De Haven Brandon A, O'Fee L, ... ... Hoelder S, et al. Introduction of a Methyl Group Curbs Metabolism of Pyrido[3,4- d]pyrimidine Monopolar Spindle 1 (MPS1) Inhibitors and Enables the Discovery of the Phase 1 Clinical Candidate N-(2-Ethoxy-4-(4-methyl-4 H-1,2,4-triazol-3-yl)phenyl)-6-methyl- N-neopentylpyrido[3,4- d]pyrimidine-2,8-diamine (BOS172722). Journal of Medicinal Chemistry. PMID 30199249 DOI: 10.1021/acs.jmedchem.8b00690  0.8
2018 Hudson L, Mui J, Vázquez S, Carvalho DM, Williams E, Jones C, Bullock AN, Hoelder S. Novel Quinazolinone Inhibitors of ALK2 Flip between Alternate Binding Modes: Structure-Activity Relationship, Structural Characterization, Kinase Profiling, and Cellular Proof of Concept. Journal of Medicinal Chemistry. PMID 30085668 DOI: 10.1021/acs.jmedchem.8b00782  0.4
2017 Faisal A, Mak GW, Gurden MD, Xavier CP, Anderhub SJ, Innocenti P, Westwood IM, Naud S, Hayes A, Box G, Valenti MR, De Haven Brandon AK, O'Fee L, Schmitt J, Woodward HL, ... ... Hoelder S, et al. Characterisation of CCT271850, a selective, oral and potent MPS1 inhibitor, used to directly measure in vivo MPS1 inhibition vs therapeutic efficacy. British Journal of Cancer. PMID 28334731 DOI: 10.1038/bjc.2017.75  0.8
2017 McGrath S, Tortorici M, Drouin L, Solanki S, Vidler L, Westwood I, Gimeson P, vanMontfort R, Hoelder S. Structure Enabled Discovery of a Stapled Peptide Inhibitor to Target the Oncogenic Transcriptional Repressor TLE1. Chemistry (Weinheim An Der Bergstrasse, Germany). PMID 28326635 DOI: 10.1002/chem.201700747  0.4
2016 Tisi D, Chiarparin E, Tamanini E, Pathuri P, Coyle JE, Hold A, Holding FP, Martin AC, Rich SJ, Berdini V, Yon J, Acklam P, Burke R, Drouin L, Harmer JE, ... ... Hoelder S, et al. Structure of the Epigenetic Oncogene MMSET & Inhibition by N-Alkyl Sinefungin Derivatives. Acs Chemical Biology. PMID 27571355 DOI: 10.1021/acschembio.6b00308  0.4
2016 Innocenti P, Woodward HL, Solanki S, Naud S, Westwood IM, Cronin N, Hayes A, Roberts J, Henley AT, Baker R, Faisal A, Mak GW, Box G, Valenti M, De Haven Brandon A, ... ... Hoelder S, et al. Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach. Journal of Medicinal Chemistry. PMID 27055065 DOI: 10.1021/acs.jmedchem.5b01811  0.48
2015 Gurden MD, Westwood IM, Faisal A, Naud S, Cheung KM, McAndrew C, Wood A, Schmitt J, Boxall K, Mak G, Workman P, Burke R, Hoelder S, Blagg J, Van Montfort RL, et al. Naturally Occurring Mutations in the MPS1 Gene Predispose Cells to Kinase Inhibitor Drug Resistance. Cancer Research. 75: 3340-54. PMID 26202014 DOI: 10.1158/0008-5472.CAN-14-3272  0.48
2015 Drouin L, McGrath S, Vidler LR, Chaikuad A, Monteiro O, Tallant C, Philpott M, Rogers C, Fedorov O, Liu M, Akhtar W, Hayes A, Raynaud F, Müller S, Knapp S, ... Hoelder S, et al. Structure enabled design of BAZ2-ICR, a chemical probe targeting the bromodomains of BAZ2A and BAZ2B. Journal of Medicinal Chemistry. 58: 2553-9. PMID 25719566 DOI: 10.1021/jm501963e  0.48
2015 Innocenti P, Woodward H, O'Fee L, Hoelder S. Expanding the scope of fused pyrimidines as kinase inhibitor scaffolds: synthesis and modification of pyrido[3,4-d]pyrimidines. Organic & Biomolecular Chemistry. 13: 893-904. PMID 25407826 DOI: 10.1039/c4ob02238f  0.8
2013 Naud S, Westwood IM, Faisal A, Sheldrake P, Bavetsias V, Atrash B, Cheung KM, Liu M, Hayes A, Schmitt J, Wood A, Choi V, Boxall K, Mak G, Gurden M, ... ... Hoelder S, et al. Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1). Journal of Medicinal Chemistry. 56: 10045-65. PMID 24256217 DOI: 10.1021/jm401395s  0.48
2013 Vidler LR, Filippakopoulos P, Fedorov O, Picaud S, Martin S, Tomsett M, Woodward H, Brown N, Knapp S, Hoelder S. Discovery of novel small-molecule inhibitors of BRD4 using structure-based virtual screening. Journal of Medicinal Chemistry. 56: 8073-88. PMID 24090311 DOI: 10.1021/jm4011302  0.48
2013 Morley AD, Pugliese A, Birchall K, Bower J, Brennan P, Brown N, Chapman T, Drysdale M, Gilbert IH, Hoelder S, Jordan A, Ley SV, Merritt A, Miller D, Swarbrick ME, et al. Fragment-based hit identification: thinking in 3D. Drug Discovery Today. 18: 1221-7. PMID 23906694 DOI: 10.1016/j.drudis.2013.07.011  0.48
2013 Silva-Santisteban MC, Westwood IM, Boxall K, Brown N, Peacock S, McAndrew C, Barrie E, Richards M, Mirza A, Oliver AW, Burke R, Hoelder S, Jones K, Aherne GW, Blagg J, et al. Fragment-based screening maps inhibitor interactions in the ATP-binding site of checkpoint kinase 2. Plos One. 8: e65689. PMID 23776527 DOI: 10.1371/journal.pone.0065689  0.48
2012 Vidler LR, Brown N, Knapp S, Hoelder S. Druggability analysis and structural classification of bromodomain acetyl-lysine binding sites. Journal of Medicinal Chemistry. 55: 7346-59. PMID 22788793 DOI: 10.1021/jm300346w  0.48
2012 Wylie L, Innocenti P, Whelligan DK, Hoelder S. Synthesis of amino-substituted indoles using the Bartoli reaction. Organic & Biomolecular Chemistry. 10: 4441-7. PMID 22565609 DOI: 10.1039/c2ob25256b  0.8
2012 Hoelder S, Clarke PA, Workman P. Discovery of small molecule cancer drugs: successes, challenges and opportunities. Molecular Oncology. 6: 155-76. PMID 22440008 DOI: 10.1016/j.molonc.2012.02.004  0.48
2012 Innocenti P, Cheung KM, Solanki S, Mas-Droux C, Rowan F, Yeoh S, Boxall K, Westlake M, Pickard L, Hardy T, Baxter JE, Aherne GW, Bayliss R, Fry AM, Hoelder S. Design of potent and selective hybrid inhibitors of the mitotic kinase Nek2: structure-activity relationship, structural biology, and cellular activity. Journal of Medicinal Chemistry. 55: 3228-41. PMID 22404346 DOI: 10.1021/jm201683b  0.48
2011 Solanki S, Innocenti P, Mas-Droux C, Boxall K, Barillari C, van Montfort RL, Aherne GW, Bayliss R, Hoelder S. Benzimidazole inhibitors induce a DFG-out conformation of never in mitosis gene A-related kinase 2 (Nek2) without binding to the back pocket and reveal a nonlinear structure-activity relationship. Journal of Medicinal Chemistry. 54: 1626-39. PMID 21366329 DOI: 10.1021/jm1011726  0.8
2010 Whelligan DK, Solanki S, Taylor D, Thomson DW, Cheung KM, Boxall K, Mas-Droux C, Barillari C, Burns S, Grummitt CG, Collins I, van Montfort RL, Aherne GW, Bayliss R, Hoelder S. Aminopyrazine inhibitors binding to an unusual inactive conformation of the mitotic kinase Nek2: SAR and structural characterization. Journal of Medicinal Chemistry. 53: 7682-98. PMID 20936789 DOI: 10.1021/jm1008727  0.4
2010 Whelligan DK, Thomson DW, Taylor D, Hoelder S. Two-step synthesis of aza- and diazaindoles from chloroamino-N-heterocycles using ethoxyvinylborolane. The Journal of Organic Chemistry. 75: 11-5. PMID 19950955 DOI: 10.1021/jo902143f  0.32
2009 Richards MW, O'Regan L, Mas-Droux C, Blot JM, Cheung J, Hoelder S, Fry AM, Bayliss R. An autoinhibitory tyrosine motif in the cell-cycle-regulated Nek7 kinase is released through binding of Nek9. Molecular Cell. 36: 560-70. PMID 19941817 DOI: 10.1016/j.molcel.2009.09.038  0.48
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