Lessons in PROTAC design from selective degradation with a promiscuous warhead DP Bondeson, BE Smith, GM Burslem, AD Buhimschi, J Hines, ... Cell chemical biology 25 (1), 78-87. e5, 2018 | 694 | 2018 |
Proteolysis-targeting chimeras as therapeutics and tools for biological discovery GM Burslem, CM Crews Cell 181 (1), 102-114, 2020 | 651 | 2020 |
The advantages of targeted protein degradation over inhibition: an RTK case study GM Burslem, BE Smith, AC Lai, S Jaime-Figueroa, DC McQuaid, ... Cell chemical biology 25 (1), 67-77. e3, 2018 | 544 | 2018 |
Small-Molecule Modulation of Protein Homeostasis GM Burslem, CM Crews Chemical Reviews 117 (17), 11269-11301, 2017 | 267 | 2017 |
Targeting BCR-ABL1 in Chronic Myeloid Leukemia by PROTAC-mediated Targeted Protein Degradation GM Burslem, AR Schultz, DP Bondeson, CA Eide, SLS Stevens, ... Cancer research 79 (18), 4744-4753, 2019 | 168 | 2019 |
Enhancing Antiproliferative Activity and Selectivity of a FLT-3 Inhibitor by Proteolysis Targeting Chimera Conversion GM Burslem, J Song, X Chen, J Hines, CM Crews Journal of the American Chemical Society 140 (48), 16428-16432, 2018 | 148 | 2018 |
Double quick, double click reversible peptide “stapling” CM Grison, GM Burslem, JA Miles, LKA Pilsl, DJ Yeo, Z Imani, ... Chemical science 8 (7), 5166-5171, 2017 | 92 | 2017 |
Small‐Molecule Proteomimetic Inhibitors of the HIF‐1α–p300 Protein–Protein Interaction GM Burslem, HF Kyle, AL Breeze, TA Edwards, A Nelson, SL Warriner, ... ChemBioChem 15 (8), 1083-1087, 2014 | 75 | 2014 |
Click-enabled heterotrifunctional template for sequential bioconjugations. DM Beal, VE Albrow, G Burslem, L Hitchen, C Fernandes, C Lapthorn, ... Org. Biomol. Chem., 2011 | 75 | 2011 |
A modular lead-oriented synthesis of diverse piperazine, 1, 4-diazepane and 1, 5-diazocane scaffolds T James, P MacLellan, GM Burslem, I Simpson, JA Grant, S Warriner, ... Organic & biomolecular chemistry 12 (16), 2584-2591, 2014 | 65 | 2014 |
Exploration of the HIF-1α/p300 interface using peptide and Adhiron phage display technologies HF Kyle, KF Wickson, J Stott, GM Burslem, AL Breeze, C Tiede, ... Molecular BioSystems 11 (10), 2738-2749, 2015 | 46 | 2015 |
Hypoxia inducible factor (HIF) as a model for studying inhibition of protein–protein interactions GM Burslem, HF Kyle, A Nelson, TA Edwards, AJ Wilson Chemical Science 8 (6), 4188-4202, 2017 | 43 | 2017 |
Development of solvent-free synthesis of hydrogen-bonded supramolecular polyurethanes KA Houton, GM Burslem, AJ Wilson Chemical Science 6 (4), 2382-2388, 2015 | 39 | 2015 |
Egfr proteolysis targeting chimeric molecules and associated methods of use AP Crew, K Zimmermann, J Wang, CM Crews, S Jaime-Figueroa, ... US Patent 10,994,015, 2021 | 36 | 2021 |
Protein folding state-dependent sorting at the Golgi apparatus D Hellerschmied, YV Serebrenik, L Shao, GM Burslem, CM Crews Molecular biology of the cell 30 (17), 2296-2308, 2019 | 33 | 2019 |
Efficient Synthesis of Immunomodulatory Drug Analogues Enables Exploration of Structure–Degradation Relationships GM Burslem, P Ottis, S Jaime‐Figueroa, A Morgan, PM Cromm, M Toure, ... ChemMedChem 13 (15), 1508-1512, 2018 | 33 | 2018 |
Compounds and methods for the targeted degradation of fetal liver kinase polypeptides AP Crew, KR Hornberger, CM Crews, G Burslem US Patent 10,806,737, 2020 | 32 | 2020 |
Orthogonal functionalisation of α-helix mimetics A Barnard, K Long, DJ Yeo, JA Miles, V Azzarito, GM Burslem, ... Organic & biomolecular chemistry 12 (35), 6794-6799, 2014 | 31 | 2014 |
The copper chaperone CCS facilitates copper binding to MEK1/2 to promote kinase activation M Grasso, GJ Bond, YJ Kim, S Boyd, MM Dzebo, S Valenzuela, T Tsang, ... Journal of Biological Chemistry 297 (6), 2021 | 28 | 2021 |
Towards “bionic” proteins: replacement of continuous sequences from HIF-1α with proteomimetics to create functional p300 binding HIF-1α mimics GM Burslem, HF Kyle, AL Breeze, TA Edwards, A Nelson, SL Warriner, ... Chemical Communications 52 (31), 5421-5424, 2016 | 25 | 2016 |