Rob L M van Montfort
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Explore the profile of Rob L M van Montfort including associated specialties, affiliations and a list of published articles.
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1011
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Recent Articles
1.
Specific radiation damage to halogenated inhibitors and ligands in protein-ligand crystal structures
Rodrigues M, Cabry M, Collie G, Carter M, McAndrew C, Owen R, et al.
J Appl Crystallogr
. 2024 Dec;
57(Pt 6):1951-1965.
PMID: 39628887
Protein-inhibitor crystal structures aid medicinal chemists in efficiently improving the potency and selectivity of small-molecule inhibitors. It is estimated that a quarter of lead molecules in drug discovery projects are...
2.
Bouguenina H, Nicolaou S, Le Bihan Y, Bowling E, Calderon C, Caldwell J, et al.
iScience
. 2024 Apr;
27(5):109727.
PMID: 38646177
[This corrects the article DOI: 10.1016/j.isci.2023.107059.].
3.
Liu M, Mirza A, McAndrew P, Thapaliya A, Pierrat O, Stubbs M, et al.
J Med Chem
. 2023 Jul;
66(15):10617-10627.
PMID: 37467168
High hit rates from initial ligand-observed NMR screening can make it challenging to prioritize which hits to follow up, especially in cases where there are no available crystal structures of...
4.
Bouguenina H, Scarpino A, OHanlon J, Warne J, Wang H, Wah Hak L, et al.
Chembiochem
. 2023 Jul;
24(23):e202300351.
PMID: 37418539
Small molecules inducing protein degradation are important pharmacological tools to interrogate complex biology and are rapidly translating into clinical agents. However, to fully realise the potential of these molecules, selectivity...
5.
Bouguenina H, Nicolaou S, Le Bihan Y, Bowling E, Calderon C, Caldwell J, et al.
iScience
. 2023 Jun;
26(7):107059.
PMID: 37360684
To address the limitation associated with degron based systems, we have developed iTAG, a synthetic tag based on IMiDs/CELMoDs mechanism of action that improves and addresses the limitations of both...
6.
Harnden A, Davis O, Box G, Hayes A, Johnson L, Henley A, et al.
J Med Chem
. 2023 Apr;
66(8):5892-5906.
PMID: 37026591
B-cell lymphoma 6 (BCL6) is a transcriptional repressor and oncogenic driver of diffuse large B-cell lymphoma (DLBCL). Here, we report the optimization of our previously reported tricyclic quinolinone series for...
7.
Pierrat O, Liu M, Collie G, Shetty K, Rodrigues M, Le Bihan Y, et al.
Sci Rep
. 2022 Nov;
12(1):18633.
PMID: 36329085
By suppressing gene transcription through the recruitment of corepressor proteins, B-cell lymphoma 6 (BCL6) protein controls a transcriptional network required for the formation and maintenance of B-cell germinal centres. As...
8.
Davis O, Cheung K, Brennan A, Lloyd M, Rodrigues M, Pierrat O, et al.
J Med Chem
. 2022 Jun;
65(12):8169-8190.
PMID: 35657291
To identify new chemical series with enhanced binding affinity to the BTB domain of B-cell lymphoma 6 protein, we targeted a subpocket adjacent to Val18. With no opportunities for strong...
9.
Huckvale R, Harnden A, Cheung K, Pierrat O, Talbot R, Box G, et al.
J Med Chem
. 2022 Jun;
65(12):8191-8207.
PMID: 35653645
The transcriptional repressor BCL6 is an oncogenic driver found to be deregulated in lymphoid malignancies. Herein, we report the optimization of our previously reported benzimidazolone molecular glue-type degrader to ,...
10.
Lloyd M, Huckvale R, Cheung K, Rodrigues M, Collie G, Pierrat O, et al.
J Med Chem
. 2021 Nov;
64(23):17079-17097.
PMID: 34846884
We describe the optimization of modestly active starting points to potent inhibitors of BCL6 by growing into a subpocket, which was occupied by a network of five stably bound water...