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Swen Hoelder - Publications

Affiliations: 
1998- University of California, Berkeley, Berkeley, CA, United States 
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40/45 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
2023 Liu M, Mirza A, McAndrew PC, Thapaliya A, Pierrat OA, Stubbs M, Hahner T, Chessum NEA, Innocenti P, Caldwell J, Cheeseman MD, Bellenie BR, van Montfort RLM, Newton GK, Burke R, ... ... Hoelder S, et al. Determination of Ligand-Binding Affinity () Using Transverse Relaxation Rate () in the Ligand-Observed H NMR Experiment and Applications to Fragment-Based Drug Discovery. Journal of Medicinal Chemistry. PMID 37467168 DOI: 10.1021/acs.jmedchem.3c00758  0.594
2023 Harnden AC, Davis OA, Box GM, Hayes A, Johnson LD, Henley AT, de Haven Brandon AK, Valenti M, Cheung KJ, Brennan A, Huckvale R, Pierrat OA, Talbot R, Bright MD, Akpinar HA, ... ... Hoelder S, et al. Discovery of an Chemical Probe for BCL6 Inhibition by Optimization of Tricyclic Quinolinones. Journal of Medicinal Chemistry. PMID 37026591 DOI: 10.1021/acs.jmedchem.3c00155  0.337
2022 Pierrat OA, Liu M, Collie GW, Shetty K, Rodrigues MJ, Le Bihan YV, Gunnell EA, McAndrew PC, Stubbs M, Rowlands MG, Yahya N, Shehu E, Talbot R, Pickard L, Bellenie BR, ... ... Hoelder S, et al. Discovering cell-active BCL6 inhibitors: effectively combining biochemical HTS with multiple biophysical techniques, X-ray crystallography and cell-based assays. Scientific Reports. 12: 18633. PMID 36329085 DOI: 10.1038/s41598-022-23264-z  0.767
2022 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, ... ... Hoelder S, et al. Optimizing Shape Complementarity Enables the Discovery of Potent Tricyclic BCL6 Inhibitors. Journal of Medicinal Chemistry. PMID 35657291 DOI: 10.1021/acs.jmedchem.1c02174  0.375
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  0.316
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  0.792
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  0.804
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  0.546
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  0.784
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  0.74
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  0.805
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  0.775
2017 Anderhub SJ, Mak GW, Faisal A, Walsh K, Gurden M, Day L, Innocenti P, Woodward HL, Westwood IM, Cheung KJ, Naud S, Hayes A, Box G, Brandon AdH, Valenti MR, ... ... Hoelder S, et al. Abstract 4036: Induction of detrimental aneuploidy in basal breast cancer cells treated by MPS1 inhibitors in combination with paclitaxel Cancer Research. 77: 4036-4036. DOI: 10.1158/1538-7445.Am2017-4036  0.386
2017 Woodward HL, Innocenti P, Cheung KJ, Naud S, Hayes A, Henley AT, Faisal A, Mak G, Box G, Westwood IM, Carter M, Valenti M, Brandon ADH, O’Fee L, Saville H, ... ... Hoelder S, et al. Abstract 193: Inhibitors of MPS1: Discovery of CCT289346, a highly potent, selective and orally available preclinical candidate Cancer Research. 77: 193-193. DOI: 10.1158/1538-7445.Am2017-193  0.576
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  0.79
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  0.823
2016 Carvalho D, Taylor K, Olaciregui NG, Valenti M, Ruddle R, Henley A, Hayes A, Brandon ADH, MacKay A, Molinari V, Vinci M, Popov S, Brennan P, Moore A, Hudson L, ... Hoelder S, et al. PDTB-20. PRECLINICAL EFFICACY OF ALK2 INHIBITORS IN ACVR1 MUTANT DIPG Neuro-Oncology. 18: vi154-vi154. DOI: 10.1093/Neuonc/Now212.639  0.794
2016 Carvalho D, Taylor K, Olaciregui NG, Valenti M, Ruddle R, Henley A, Hayes A, Brandon ADH, Hallsworth A, Mackay A, Molinari V, Vinci M, Popov S, Boudhar A, Brennan P, ... ... Hoelder S, et al. HG-67PRECLINICAL EFFICACY OF ALK2 INHIBITORS IN ACVR1 MUTANT DIPG Neuro-Oncology. 18: iii63.1-iii63. DOI: 10.1093/Neuonc/Now073.63  0.79
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  0.432
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  0.811
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  0.802
2015 Pawlyn C, Chambers T, Macleod V, Sappington D, Buros A, Stein CK, Kaiser MF, Burke R, Hoelder S, Boysen G, Edmondson RD, Morgan GJ, Davies FE. Identifying Targets for Therapy in High Risk t(4;14) Myeloma Using Multi-Level Molecular and Phenotypic Analysis of Isogenic MMSET and MMSET Knock out Cell Lines Blood. 126: 1792-1792. DOI: 10.1182/Blood.V126.23.1792.1792  0.388
2015 Gurden MD, Westwood I, Faisal A, Naud S, Cheung J, McAndrew C, Wood A, Schmitt J, Boxall K, Mak G, Workman P, Burke R, Hoelder S, Blagg J, Montfort RV, et al. Abstract 5450: Naturally occurring mutations in the MPS1 gene predispose cells to kinase inhibitor drug-resistance Cancer Research. 75: 5450-5450. DOI: 10.1158/1538-7445.Am2015-5450  0.677
2015 Innocenti P, Woodward H, Cheung KJ, Naud S, Solanki S, Westwood IM, Faisal A, Hayes A, Schmitt J, Baker R, Matijssen B, Burke R, Eccles SA, Raynaud FI, Linardopoulos S, ... ... Hoelder S, et al. Abstract 3642: Structure enabled design of inhibitors of the mitotic kinase MPS1 Cancer Research. 75: 3642-3642. DOI: 10.1158/1538-7445.Am2015-3642  0.824
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  0.548
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  0.786
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  0.528
2013 Faisal A, Innocenti P, Westwood I, Naud S, Schmitt J, Hayes A, Mak G, Gurden M, Bavetsias V, Cheung J, Woodward H, Sheldrake P, Atrash B, Burke R, Baker R, ... ... Hoelder S, et al. Abstract 3242: CCT271850, a novel, selective, highly potent and orally bioavailable Mps1 kinase inhibitor. Cancer Research. 73: 3242-3242. DOI: 10.1158/1538-7445.Am2013-3242  0.822
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  0.419
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  0.591
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  0.341
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  0.738
2012 Haegebarth A, Politz O, Liu N, Ince S, Neuhaus R, Boemer U, Gekeler V, Hoelder S, Zuelch A, Mumberg D, Brands M, Ziegelbauer K. Abstract 3751: In vitro and in vivo pharmacological profile of BAY 1001931, a novel highly potent allosteric AKT1/2 inhibitor Cancer Research. 72: 3751-3751. DOI: 10.1158/1538-7445.Am2012-3751  0.42
2012 Faisal A, Naud S, Schmitt J, Westwood I, Hayes A, Gurden M, Bavetsias V, Berry T, Mak G, Innocenti P, Cheung J, Sheldrake P, Atrash B, Sun C, Matijssen B, ... ... Hoelder S, et al. Abstract 1817: Characterisation of CCT251455, a novel, selective and highly potent Mps1 kinase inhibitor Cancer Research. 72: 1817-1817. DOI: 10.1158/1538-7445.Am2012-1817  0.793
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  0.721
2011 Darby JF, Vidler L, Simpson PJ, Sharp S, Prodromou C, Matthews S, Hoelder S, Pearl L, Workman P. Abstract B99: Targeting TPR cochaperones of the Hsp90 molecular chaperone complex for specific inhibition. Molecular Cancer Therapeutics. 10. DOI: 10.1158/1535-7163.Targ-11-B99  0.513
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  0.488
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  0.694
2006 Vogtherr M, Saxena K, Hoelder S, Grimme S, Betz M, Schieborr U, Pescatore B, Robin M, Delarbre L, Langer T, Wendt KU, Schwalbe H. NMR characterization of kinase p38 dynamics in free and ligand-bound forms. Angewandte Chemie (International Ed. in English). 45: 993-7. PMID 16374788 DOI: 10.1002/Anie.200502770  0.31
2006 Vogtherr M, Saxena K, Hoelder S, Grimme S, Betz M, Schieborr U, Pescatore B, Robin M, Delarbre L, Langer T, Wendt KU, Schwalbe H. Charakterisierung der Dynamik der Kinase p38 in freiem und ligandgebundenem Zustand durch NMR-Spektroskopie Angewandte Chemie. 118: 1008-1012. DOI: 10.1002/Ange.200502770  0.34
Low-probability matches (unlikely to be authored by this person)
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  0.277
2022 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, ... ... Hoelder S, et al. Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 . Journal of Medicinal Chemistry. PMID 35653645 DOI: 10.1021/acs.jmedchem.1c02175  0.276
2021 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, ... ... Hoelder S, et al. Into Deep Water: Optimizing BCL6 Inhibitors by Growing into a Solvated Pocket. Journal of Medicinal Chemistry. PMID 34846884 DOI: 10.1021/acs.jmedchem.1c00946  0.269
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  0.25
2010 HOELDER S, BLECHERT S. ChemInform Abstract: A Concise Synthesis of Coronafacic Acid via Ring Closing Olefin Metathesis. Cheminform. 27: no-no. DOI: 10.1002/CHIN.199642249  0.072
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