From Peptides to Mimetics: Towards Smaller More Stable Drug-like Protein-protein Interaction Inhibitors
Lead Research Organisation:
University of Bath
Department Name: Biology and Biochemistry
Abstract
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Publications
Brennan A
(2022)
The effect of helix-inducing constraints and downsizing upon a transcription block survival-derived functional cJun antagonist.
in Cell reports. Physical science
Brennan A
(2025)
An Intracellular Peptide Library Screening Platform Identifies Irreversible Covalent Transcription Factor Inhibitors
in Advanced Science
Brennan A
(2022)
An Approach to Derive Functional Peptide Inhibitors of Transcription Factor Activity.
in JACS Au
Brennan A
(2020)
Selective antagonism of cJun for cancer therapy.
in Journal of experimental & clinical cancer research : CR
Hoang H
(2020)
Correction: Twists or turns: stabilising alpha vs. beta turns in tetrapeptides
in Chemical Science
Leech JT
(2022)
In vitro single molecule and bulk phase studies reveal the AP-1 transcription factor cFos binds to DNA without its partner cJun.
in The Journal of biological chemistry
Madden SK
(2021)
Taking the Myc out of cancer: toward therapeutic strategies to directly inhibit c-Myc.
in Molecular cancer
Meade RM
(2021)
A Downsized and Optimised Intracellular Library-Derived Peptide Prevents Alpha-Synuclein Primary Nucleation and Toxicity Without Impacting Upon Lipid Binding.
in Journal of molecular biology
Nadal-Bufi F
(2021)
Designed ß-Hairpins Inhibit LDH5 Oligomerization and Enzymatic Activity.
in Journal of medicinal chemistry
| Title | CROSS-LINIKING METHODS |
| Description | Disclosed are methods and kits for producing a conformationally constrained peptide, such as a helix constrained peptide, in a cell. In some cases, the methods comprise contacting a cell comprising an intracellularly-localised recombinant peptide with a cross-linker and culturing the cell in the presence of the cross-linker, wherein the cross-linker forms thioether cross-links with at least two derivatisable amino acids located at anchoring positions in the recombinant peptide. The methods and kits and cells find application, for example, in the identification of inhibitors that can be used to disrupt protein-protein interactions. |
| IP Reference | US2023313258 |
| Protection | Patent / Patent application |
| Year Protection Granted | 2023 |
| Licensed | Yes |
| Title | SCREENING ASSAY |
| Description | Disclosed are methods, kits and cells for screening for test compounds that are capable of inhibiting DNA-binding activity of a DNA-binding protein. The disclosed methods, kits and cells may include a reporter expression cassette that encodes a reporter expression product, wherein the reporter expression cassette comprises at least one binding site for the DNA-binding protein such that binding of the DNA-binding protein to the binding site inhibits expression of the reporter expression product. Also disclosed are methods for producing a helix-constrained peptide that may be used in the screening methods disclosed herein. The methods, kits and cells find application, for example, in the identification of antagonists that may be useful in the treatment of cancers involving the DNA-binding protein. |
| IP Reference | US2021396736 |
| Protection | Patent / Patent application |
| Year Protection Granted | 2021 |
| Licensed | Yes |
| Title | c-Jun???? |
| Description | A c-Jun antagonist is described. Also described are compositions comprising these c-Jun antagonists, as well as methods, methods of treatment comprising the c-Jun antagonists, and therapeutic uses. |
| IP Reference | CN118984835 |
| Protection | Patent / Patent application |
| Year Protection Granted | 2024 |
| Licensed | Yes |
| Company Name | Revolver Therapeutics |
| Description | Revolver Therapeutics researches and develops peptide-based inhibitors with the aim of producing treatments for cancers currently considered undruggable. |
| Year Established | 2023 |
| Impact | Revolver has only recenely spunout and is developing lead molecules and seeking fundraising. |
| Website | http://revolvertherapeutics.com |
| Description | In cellulo library-derived peptide-based inhibitors of alpha-synuclein aggregation and toxicity |
| Form Of Engagement Activity | A talk or presentation |
| Part Of Official Scheme? | No |
| Geographic Reach | International |
| Primary Audience | Other audiences |
| Results and Impact | International Peptide Symposium, Brisbane 2023 |
| Year(s) Of Engagement Activity | 2023 |
| URL | https://www.peptides2023.org/ |
| Description | Invited speaker at 11th annual conference of the International Chemical Biology Society (ICBS) |
| Form Of Engagement Activity | A talk or presentation |
| Part Of Official Scheme? | No |
| Geographic Reach | International |
| Primary Audience | Industry/Business |
| Results and Impact | https://icbs2022.chemical-biology.org/invited-speakers |
| Year(s) Of Engagement Activity | 2022 |
| URL | https://icbs2022.chemical-biology.org/invited-speakers |