Jonathan P Orme
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Explore the profile of Jonathan P Orme including associated specialties, affiliations and a list of published articles.
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11
Citations
107
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Recent Articles
1.
McCoull W, Thomson C, Braybrooke E, Chan C, Colclough N, Cortes Gonzalez M, et al.
J Med Chem
. 2025 Jan;
68(3):3700-3748.
PMID: 39869768
Despite recent advances in the inhibition of EGFR (epidermal growth factor receptor), there remains a clinical need for new EGFR Exon20 insertion (Ex20Ins) inhibitors that spare EGFR WT. Herein, we...
2.
Johannes J, Balazs A, Barratt D, Bista M, Chuba M, Cosulich S, et al.
J Med Chem
. 2024 Dec;
67(24):21717-21728.
PMID: 39655996
PARP inhibitors have attracted considerable interest in drug discovery due to the clinical success of first-generation agents such as olaparib, niraparib, rucaparib, and talazoparib. Their success lies in their ability...
3.
Thomson C, Braybrooke E, Colclough N, Davies N, Floch N, Greenwood R, et al.
J Med Chem
. 2024 Sep;
PMID: 39340451
Herein, we report the optimization of a series of epidermal growth factor receptor (EGFR) Exon20 insertion (Ex20Ins) inhibitors using structure-based drug design (SBDD), leading to the discovery of compound ,...
4.
Thomson C, Barton P, Braybrooke E, Colclough N, Dong Z, Evans L, et al.
J Med Chem
. 2024 May;
67(11):8988-9027.
PMID: 38770784
Herein, we report the identification and optimization of a series of potent inhibitors of EGFR Exon20 insertions with significant selectivity over wild-type EGFR. A strategically designed HTS campaign, multiple iterations...
5.
Pemberton N, Compagne N, Argyrou A, Evertsson E, Gunnarsson A, Kettle J, et al.
ACS Med Chem Lett
. 2024 May;
15(5):583-589.
PMID: 38746885
To further facilitate the discovery of cysteine reactive covalent inhibitors, there is a need to develop new reactive groups beyond the traditional acrylamide-type warheads. Herein we describe the design and...
6.
Johannes J, Balazs A, Barratt D, Bista M, Chuba M, Cosulich S, et al.
J Med Chem
. 2021 Sep;
64(19):14498-14512.
PMID: 34570508
Poly-ADP-ribose-polymerase (PARP) inhibitors have achieved regulatory approval in oncology for homologous recombination repair deficient tumors including BRCA mutation. However, some have failed in combination with first-line chemotherapies, usually due to...
7.
Finlay M, Barton P, Bickerton S, Bista M, Colclough N, Cross D, et al.
J Med Chem
. 2021 Sep;
64(18):13704-13718.
PMID: 34491761
The epidermal growth factor receptor (EGFR) harboring activating mutations is a clinically validated target in non-small-cell lung cancer, and a number of inhibitors of the EGFR tyrosine kinase domain, including...
8.
Shaw J, Dale I, Hemsley P, Leach L, Dekki N, Orme J, et al.
SLAS Discov
. 2018 Dec;
24(2):121-132.
PMID: 30543471
Methods to measure cellular target engagement are increasingly being used in early drug discovery. The Cellular Thermal Shift Assay (CETSA) is one such method. CETSA can investigate target engagement by...
9.
Floch N, Martin M, Riess J, Orme J, Staniszewska A, Menard L, et al.
Mol Cancer Ther
. 2018 Feb;
17(5):885-896.
PMID: 29483211
EGFR exon 20 insertions (Ex20Ins) account for 4% to 10% of EGFR activating mutations in non-small cell lung cancer (NSCLC). EGFR Ex20Ins tumors are generally unresponsive to first- and second-generation...
10.
Hennessy E, Chuaqui C, Ashton S, Colclough N, Cross D, Debreczeni J, et al.
ACS Med Chem Lett
. 2016 May;
7(5):514-9.
PMID: 27190603
A novel series of covalent inhibitors of EGFR (epidermal growth factor receptor) kinase was discovered through a combination of subset screening and structure-based design. These compounds preferentially inhibit mutant forms...