Yusuf Hamied Department of Chemistry

Publications by Professor Sir Alan Fersht FRS

From covalent transition states in chemistry to noncovalent in biology: from β- to Φ-value analysis of protein folding
AR Fersht
Q Rev Biophys
(2024)
57
(doi: 10.1017/s0033583523000045)
NF-κB Rel subunit exchange on a physiological timescale
M Biancalana, E Natan, MJ Lenardo, AR Fersht
Protein Sci
(2021)
30
(doi: 10.1002/pro.4134)
AlphaFold - A Personal Perspective on the Impact of Machine Learning
AR Fersht
J Mol Biol
(2021)
433
(doi: 10.1016/j.jmb.2021.167088)
Targeting Cavity-Creating p53 Cancer Mutations with Small-Molecule Stabilizers: the Y220X Paradigm
MR Bauer, A Krämer, G Settanni, RN Jones, X Ni, R Khan Tareque, AR Fersht, J Spencer, AC Joerger
ACS Chemical Biology
(2020)
15
(doi: 10.1021/acschembio.9b00748)
ChemBioChem@20-Some Reflections
AR Fersht, P Gölitz, J-M Lehn
Chembiochem
(2019)
21
(doi: 10.1002/cbic.201900658)
A structure-guided molecular chaperone approach for restoring the transcriptional activity of the p53 cancer mutant Y220C
MR Bauer, RN Jones, RK Tareque, B Springett, FA Dingler, L Verduci, KJ Patel, AR Fersht, AC Joerger, J Spencer
Future Med Chem
(2019)
11
(doi: 10.4155/fmc-2019-0181)
SLMP53-2 restoreswild-type-like function to mutant p53 through hsp70: Promising activity in hepatocellular carcinoma
S Gomes, B Bosco, JB Loureiro, H Ramos, L Raimundo, J Soares, N Nazareth, V Barcherini, L Domingues, C Oliveira, A Bisio, S Piazza, MR Bauer, JP Brás, MI Almeida, C Gomes, F Reis, AR Fersht, A Inga, MMM Santos, L Saraiva
Cancers
(2019)
11
(doi: 10.3390/cancers11081151)
Aminobenzothiazole derivatives stabilize the thermolabile p53 cancer mutant Y220C and show anticancer activity in p53-Y220C cell lines.
MGJ Baud, MR Bauer, L Verduci, FA Dingler, KJ Patel, D Horil Roy, AC Joerger, AR Fersht
European Journal of Medicinal Chemistry
(2018)
152
(doi: 10.1016/j.ejmech.2018.04.035)
The curcumin analog HO-3867 selectively kills cancer cells by converting mutant p53 protein to transcriptionally active wildtype p53.
E Madan, TM Parker, MR Bauer, A Dhiman, CJ Pelham, M Nagane, ML Kuppusamy, M Holmes, TR Holmes, K Shaik, K Shee, S Kiparoidze, SD Smith, Y-SA Park, JJ Gomm, LJ Jones, AR Tomás, AC Cunha, K Selvendiran, LA Hansen, AR Fersht, K Hideg, R Gogna, P Kuppusamy
Journal of Biological Chemistry
(2018)
293
(doi: 10.1074/jbc.RA117.000950)
Mutant p53 as a therapeutic target for the treatment of triple-negative breast cancer: Preclinical investigation with the anti-p53 drug, PK11007.
NC Synnott, MR Bauer, S Madden, A Murray, R Klinger, N O'Donovan, D O'Connor, WM Gallagher, J Crown, AR Fersht, MJ Duffy
Cancer letters
(2017)
414
(doi: 10.1016/j.canlet.2017.09.053)
Targeting mutant p53 with PK11007: A new approach for the treatment of patients with triple-negative breast cancer?
NC Synnott, MR Bauer, SF Madden, AM Murray, R Klinger, N O'Donovan, D O'Connor, WM Gallagher, J Crown, AR Fersht, MJ Duffy
Journal of Clinical Oncology
(2017)
35
(doi: 10.1200/jco.2017.35.15_suppl.e14099)
Structures of closed and open conformations of dimeric human ATM
D Baretić, HK Pollard, DI Fisher, CM Johnson, B Santhanam, CM Truman, T Kouba, AR Fersht, C Phillips, RL Williams
Science advances
(2017)
3
(doi: 10.1126/sciadv.1700933)
Multisite aggregation of p53 and implications for drug rescue
GZ Wang, AR Fersht
Proceedings of the National Academy of Sciences of the United States of America
(2017)
114
(doi: 10.1073/pnas.1700308114)
Design of a molecular support for cryo-EM structure determination
TG Martin, TAM Bharat, AC Joerger, X-C Bai, F Praetorius, AR Fersht, H Dietz, SHW Scheres
Proceedings of the National Academy of Sciences
(2016)
113
(doi: 10.1073/pnas.1612720113)
2-Sulfonylpyrimidines: Mild alkylating agents with anticancer activity toward p53-compromised cells.
MR Bauer, AC Joerger, AR Fersht
Proceedings of the National Academy of Sciences of the United States of America
(2016)
113
(doi: 10.1073/pnas.1610421113)
Anin silicoalgorithm for identifying stabilizing pockets in proteins: test case, the Y220C mutant of the p53 tumor suppressor protein
D Bromley, MR Bauer, AR Fersht, V Daggett
Protein engineering, design & selection : PEDS
(2016)
29
(doi: 10.1093/protein/gzw035)
Harnessing Fluorine-Sulfur Contacts and Multipolar Interactions for the Design of p53 Mutant Y220C Rescue Drugs
MR Bauer, RN Jones, MGJ Baud, R Wilcken, FM Boeckler, AR Fersht, AC Joerger, J Spencer
ACS chemical biology
(2016)
11
(doi: 10.1021/acschembio.6b00315)
The p53 Pathway: Origins, Inactivation in Cancer, and Emerging Therapeutic Approaches.
AC Joerger, AR Fersht
Annual Review of Biochemistry
(2016)
85
(doi: 10.1146/annurev-biochem-060815-014710)
Exploiting Transient Protein States for the Design of Small-Molecule Stabilizers of Mutant p53
AC Joerger, MR Bauer, R Wilcken, MGJ Baud, H Harbrecht, TE Exner, FM Boeckler, J Spencer, AR Fersht
Structure
(2015)
23
(doi: 10.1016/j.str.2015.10.016)
Experimental and Theoretical Evaluation of the Ethynyl Moiety as a Halogen Bioisostere
R Wilcken, MO Zimmermann, MR Bauer, TJ Rutherford, AR Fersht, AC Joerger, FM Boeckler
ACS Chemical Biology
(2015)
10
(doi: 10.1021/acschembio.5b00515)
Yusuf Hamied Department of Chemistry
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