JmjC Histone Demethylases: Beyond Histone Lysine Demethylation

Συγγραφείς: Bonnici, J, Schofield, CJ, Kawamura, A

Πηγή: CHIMIA. 80:138-144

Σύνδεσμος πρόσβασης: https://ora.ox.ac.uk/objects/uuid:0dc2906e-6c7b-43ad-9079-4ae1ac96a8cc
https://doi.org/10.2533/chimia.2026.138

KDM3A catalyses the oxidation of acetyl-lysine to hydroxyacetyl-lysine on histone H3K9

Συγγραφείς: Belle, R, Bukowski, J-P, Schiller, R, Cutler, R, Salah, E, Dawber, RS, Tumber, A, Bonnici, J, Kindrick, JD, Serrano, L, Rabe, P, Johansson, C, Ruchaud, M-H, Hopkinson, RJ, Figg, Sr, WD, Brennan, PE, Mole, DR, Sidoli, S, Kawamura, A, Schofield, CJ

Πηγή: Nature Chemistry.

Structural and Functional Validation of Pseudomonas Savastanoi Ethylene Forming Enzymes Reveals Flexibility in 2‐Oxoglutarate Binding Mode and Conformation

Συγγραφείς: Sun, Y, Dhingra, S, Allen, MD, Cheng, ESZ, Zhang, Z, Schofield, CJ, Brewitz, L

Πηγή: Chembiochem

Θεματικοί όροι: Research Article

Σύνδεσμος πρόσβασης: https://pubmed.ncbi.nlm.nih.gov/41797450/
https://pmc.ncbi.nlm.nih.gov/articles/PMC12968597/
https://doi.org/10.1002/cbic.202500702

Light-Induced, Lysine-Targeting Irreversible Covalent Inhibition of the Human Oxygen Sensing Hydroxylase Factor Inhibiting HIF (FIH)

Συγγραφείς: Wu, Y, Li, Z, Kaur, S, Zhang, Z, Yue, J, Tumber, A, Zhang, H, Song, Z, Yang, P, Dong, Y, Yang, F, Li, X, Schofield, CJ, Zhang, X

Πηγή: J Am Chem Soc

Θεματικοί όροι: Repressor Proteins, Models, Molecular, Light, Molecular Structure, Lysine, Humans, Enzyme Inhibitors, Article, Mixed Function Oxygenases

Σύνδεσμος πρόσβασης: https://pubmed.ncbi.nlm.nih.gov/40344676
https://ora.ox.ac.uk/objects/uuid:38373a76-473b-4de1-bdc7-fe1b9ba8e33f
https://doi.org/10.1021/jacs.5c01935

Derivatives of the Clinically Used HIF Prolyl Hydroxylase Inhibitor Desidustat Are Efficient Inhibitors of Human γ-Butyrobetaine Hydroxylase

Συγγραφείς: Corner, TP, Tumber, A, Salah, E, Jabbary, M, Nakashima, Y, Schnaubelt, LI, Basak, S, Alshref, FM, Brewitz, L, Schofield, CJ

Πηγή: J Med Chem

Θεματικοί όροι: Structure-Activity Relationship, gamma-Butyrobetaine Dioxygenase, Humans, Prolyl-Hydroxylase Inhibitors, Enzyme Inhibitors, Triazoles, Hypoxia-Inducible Factor-Proline Dioxygenases

Σύνδεσμος πρόσβασης: https://pubmed.ncbi.nlm.nih.gov/40263713
https://ora.ox.ac.uk/objects/uuid:b7dbcf1a-aba4-4564-bdf3-e7ee7091d8e9
https://doi.org/10.1021/acs.jmedchem.5c00586

Structure-guided optimisation of fenofibrate-derived oxidative phosphorylation inhibitors to modify tumour hypoxia

Συγγραφείς: Holt-Martyn, JP, Machado, N, Coates, JTT, Puliyadi, R, Ashton, T, Traynor, E, Aslam, S, Wise, TK, Rodriguez-Berriguete, G, Schofield, CJ, Higgins, GS

Πηγή: RSC Medicinal Chemistry.

Σύνδεσμος πρόσβασης: https://ora.ox.ac.uk/objects/uuid:6814b016-3818-4ff6-af06-3c450edfcaac
https://doi.org/10.1039/d5md00742a

Expanding the Alkene‐Forming Capability of the Pseudomonas Savastanoi Ethylene‐Forming Enzyme

Συγγραφείς: Dhingra, S, Sun, Y, Zhang, Z, Schofield, CJ, Brewitz, L

Πηγή: ChemCatChem. 18

Σύνδεσμος πρόσβασης: https://ora.ox.ac.uk/objects/uuid:4325cd06-c064-4fc3-a6a0-9f8906eeb9aa
https://doi.org/10.1002/cctc.202501291

Investigating the N-terminal linker histone H1 subtypes as substrates for JmjC lysine demethylases

Συγγραφείς: Türkmen, VA, Tumber, A, Salah, E, Kaur, S, Schofield, CJ, Mecinović, J

Πηγή: RSC Chem Biol
Türkmen, V A, Tumber, A, Salah, E, Kaur, S, Schofield, C J & Mecinović, J 2025, 'Investigating the N-terminal linker histone H1 subtypes as substrates for JmjC lysine demethylases', RSC Chemical Biology, vol. 6, no. 10, pp. 1607-1615. https://doi.org/10.1039/D5CB00083A

Θεματικοί όροι: Chemistry

Περιγραφή αρχείου: application/pdf

Σύνδεσμος πρόσβασης: https://pubmed.ncbi.nlm.nih.gov/40843439
https://pubmed.ncbi.nlm.nih.gov/40843439/
https://pmc.ncbi.nlm.nih.gov/articles/PMC12363342/
https://doi.org/10.1039/d5cb00083a
https://ora.ox.ac.uk/objects/uuid:68009fc4-69dd-4f7e-a2c2-bd6760faacc6
https://doi.org/10.1039/d5cb00083a

Binding assays enable discovery of Tet(X) inhibitors that combat tetracycline destructase resistance

Συγγραφείς: Beech, MJ, Toma, EC, Smith, HG, Trush, MM, Ang, JHJ, Wong, MY, Wong, CHJ, Ali, HS, Butt, Z, Goel, V, Duarte, F, Farley, AJM, Walsh, TR, Schofield, CJ

Πηγή: Chem Sci

Θεματικοί όροι: Chemistry

Σύνδεσμος πρόσβασης: https://pubmed.ncbi.nlm.nih.gov/40342919

RaPID discovery of cell-permeable helical peptide inhibitors con-taining cyclic β-amino acids against SARS-CoV-2 main protease

Συγγραφείς: Kawai, M, Malla, TR, Chan, HTH, Tumber, A, Brewitz, L, Salah, E, Terasaka, N, Katoh, T, Kawamura, A, Schofield, CJ, Duarte, F, Suga, H

Πηγή: RSC Chem Biol

Θεματικοί όροι: Chemistry

Σύνδεσμος πρόσβασης: https://pubmed.ncbi.nlm.nih.gov/40406165

C6-Alkoxy substituted penicillins are potent non-covalently binding inhibitors of the SARS-CoV-2 main protease

Συγγραφείς: Muntean, D, Treyde, W, Kinena, L, Salah, E, Choudhry, H, Duarte, F, Brewitz, L, Schofield, CJ

Πηγή: RSC Med Chem

Θεματικοί όροι: Chemistry

Σύνδεσμος πρόσβασης: https://pubmed.ncbi.nlm.nih.gov/41199995
https://pubmed.ncbi.nlm.nih.gov/41199995/
https://doi.org/10.1039/d5md00789e
https://pmc.ncbi.nlm.nih.gov/articles/PMC12588090/
https://ora.ox.ac.uk/objects/uuid:32b85d93-ae0d-40fd-a50d-56cbf956bbda
https://doi.org/10.1039/d5md00789e

Electrostatic interactions influence diazabicyclooctane inhibitor potency against OXA-48-like β-lactamases

Συγγραφείς: Hoff, JF, Goudar, KE, Calvopiña, K, Beer, M, Hinchliffe, P, Shaw, JM, Tooke, CL, Takebayashi, Y, Cadzow, AF, Harmer, NJ, Mulholland, AJ, Schofield, CJ, Spencer, J

Πηγή: RSC Med Chem

Θεματικοί όροι: Chemistry

Σύνδεσμος πρόσβασης: https://pubmed.ncbi.nlm.nih.gov/40927637
https://pmc.ncbi.nlm.nih.gov/articles/PMC12415477/
https://doi.org/10.1039/d5md00512d
https://pubmed.ncbi.nlm.nih.gov/40927637/

Biochemical investigations using mass spectrometry to monitor JMJD6-catalysed hydroxylation of multi-lysine containing bromodomain-derived substrates

Συγγραφείς: Corner, TP, Salah, E, Tumber, A, Brewitz, L, Schofield, CJ

Πηγή: RSC Chem Biol

Θεματικοί όροι: Chemistry

Σύνδεσμος πρόσβασης: https://pubmed.ncbi.nlm.nih.gov/40046450
https://ora.ox.ac.uk/objects/uuid:01a47446-fbb3-4daf-9b2b-addb82103a35
https://doi.org/10.1039/d4cb00311j

Profiling Inhibitor Scaffolds for the Cancer Target Jumonji‐C Domain‐Containing Protein 6

Συγγραφείς: Corner, TP, Salah, E, Tumber, A, Holt‐Martyn, JP, Brewitz, L, Schofield, CJ

Πηγή: ChemMedChem

Θεματικοί όροι: Jumonji Domain-Containing Histone Demethylases, Structure-Activity Relationship, Molecular Structure, Dose-Response Relationship, Drug, Humans, Antineoplastic Agents, Enzyme Inhibitors, Research Article

Σύνδεσμος πρόσβασης: https://pubmed.ncbi.nlm.nih.gov/41170613

In Vitro and In Vivo Evaluation of Nitroxoline as an Effective Antimicrobial Alternative to Poultry Production

Συγγραφείς: Zhou, Y, Trush, MM, Ibbotson, L, Espina, L, Lankapalli, AK, Farley, AJM, Song, H, Wu, C, Cao, X, Xia, X, Gray-Hammerton, CJ, Moorey, A, Delaitre, A, Siegwart, G, Wang, S, Wang, Y, Shen, J, Schofield, CJ, Walsh, TR

Relation: https://doi.org/10.3390/antibiotics15010062

Διαθεσιμότητα: https://doi.org/10.3390/antibiotics15010062
https://ora.ox.ac.uk/objects/uuid:f5d8bf96-dd72-4e32-88c4-25944d7bd096

Fixing the Achilles Heel of Pfizer’s Paxlovid for COVID-19 Treatment

Συγγραφείς: Brewitz, L, Schofield, CJ

Πηγή: J Med Chem

Θεματικοί όροι: Ritonavir, Indazoles, Lactams, Proline, SARS-CoV-2, Leucine, Nitriles, Humans, Antiviral Agents, Coronavirus 3C Proteases, COVID-19 Drug Treatment

Σύνδεσμος πρόσβασης: https://pubmed.ncbi.nlm.nih.gov/38967233
https://ora.ox.ac.uk/objects/uuid:6e76ff3a-ed0e-4274-802c-d1f3a297186a
https://doi.org/10.1021/acs.jmedchem.4c01342

The selective prolyl hydroxylase inhibitor IOX5 stabilizes HIF-1α and compromises development and progression of acute myeloid leukemia

Συγγραφείς: Lawson, H, Holt-Martyn, JP, Dembitz, V, Kabayama, Y, Wang, LM, Bellani, A, Atwal, S, Saffoon, N, Durko, J, van de Lagemaat, LN, De Pace, AL, Tumber, A, Corner, T, Salah, E, Arndt, C, Brewitz, L, Bowen, M, Dubusse, L, George, D, Allen, L, Guitart, AV, Fung, TK, So, CWE, Schwaller, J, Gallipoli, P, O'Carroll, D, Schofield, CJ, Kranc, KR

Συνεισφορές: University of Zagreb. University of Zagreb, School of Medicine. Department of Physiology and Immunology, Bellani, Aarushi, Kranc, Kamil

Πηγή: Nat Cancer
Lawson, H, Holt-Martyn, J P, Dembitz, V, Kabayama, Y, Wang, L M, Bellani, A, Atwal, S, Saffoon, N, Durko, J, van de Lagemaat, L N, De Pace, A L, Tumber, A, Corner, T, Salah, E, Arndt, C, Brewitz, L, Bowen, M, Dubusse, L, George, D, Allen, L, Guitart, A V, Fung, T K, So, C W E, Schwaller, J, Gallipoli, P, O'Carroll, D, Schofield, C J & Kranc, K R 2024, 'The selective prolyl hydroxylase inhibitor IOX5 stabilizes HIF-1α and compromises development and progression of acute myeloid leukemia', nature cancer, vol. 5, no. 6, pp. 916-937. https://doi.org/10.1038/s43018-024-00761-w

Θεματικοί όροι: Myeloid, 0301 basic medicine, Sulfonamides / therapeutic use, Proto-Oncogene Proteins / metabolism, Hypoxia-Inducible Factor 1, alpha Subunit / metabolism, Apoptosis, Mice, Temeljne medicinske znanosti, Hypoxia-Inducible Factor-Proline Dioxygenases / antagonists & inhibitors, Sulfonamides, 0303 health sciences, Leukemia, Tumor, Protein Stability, Heterocyclic, Protein Stability / drug effects, Prolyl-Hydroxylase Inhibitors / pharmacology, Membrane Proteins / metabolism, 3. Good health, Leukemia, Myeloid, Acute, Proto-Oncogene Proteins c-bcl-2, Biomedicina i zdravstvo, Leukemia, Myeloid, Acute / metabolism, Disease Progression, Hypoxia-Inducible Factor 1, Proto-Oncogene Proteins c-bcl-2 / metabolism, Acute, alpha Subunit, Apoptosis / drug effects, Article, Cell Line, Hypoxia-Inducible Factor-Proline Dioxygenases, Hypoxia-Inducible Factor-Proline Dioxygenases / metabolism, Bridged Bicyclo Compounds, 03 medical and health sciences, Proto-Oncogene Proteins, Cell Line, Tumor, Humans, Animals, Biomedicine and Health Sciences, Sulfonamides / pharmacology, Membrane Proteins / genetics, Prolyl-Hydroxylase Inhibitors / therapeutic use, Membrane Proteins, Basic Medical Sciences, Prolyl-Hydroxylase Inhibitors, Hypoxia-Inducible Factor 1, alpha Subunit, Bridged Bicyclo Compounds, Heterocyclic, Human Physiology, fiziologija čovjeka, Leukemia, Myeloid, Acute / drug therapy

Περιγραφή αρχείου: application/pdf; Print-Electronic

Σύνδεσμος πρόσβασης: https://pubmed.ncbi.nlm.nih.gov/38637657
https://www.research.ed.ac.uk/en/publications/493491ab-d111-46df-b299-a28599f819ec
https://hdl.handle.net/20.500.11820/493491ab-d111-46df-b299-a28599f819ec
https://doi.org/10.1038/s43018-024-00761-w
https://www.ncbi.nlm.nih.gov/geo/query/acc.cgi?acc=GSE232644
https://www.pure.ed.ac.uk/ws/files/508611763/s43018-024-00761-w.pdf

Aldehyde-mediated inhibition of asparagine biosynthesis has implications for diabetes and alcoholism

Συγγραφείς: John, T, Saffoon, N, Walsby-Tickle, J, Hester, SS, Dingler, FA, Millington, CL, McCullagh, JSO, Patel, KJ, Hopkinson, RJ, Schofield, CJ

Πηγή: Chem Sci

Θεματικοί όροι: 0301 basic medicine, Chemistry, 0303 health sciences, 03 medical and health sciences, 3. Good health

Σύνδεσμος πρόσβασης: https://pubmed.ncbi.nlm.nih.gov/38362406
https://ora.ox.ac.uk/objects/uuid:4d17df1f-8820-4bbd-8ce4-6f06d13e15a9
https://doi.org/10.1039/d3sc06551k

Structural basis of Pseudomonas aeruginosa penicillin binding protein 3 inhibition by the siderophore-antibiotic cefiderocol

Συγγραφείς: Smith, HG, Basak, S, Aniebok, V, Beech, MJ, Alshref, FM, Allen, MD, Farley, AJM, Schofield, CJ

Πηγή: Chem Sci

Θεματικοί όροι: Chemistry

Σύνδεσμος πρόσβασης: https://pubmed.ncbi.nlm.nih.gov/39328188
https://ora.ox.ac.uk/objects/uuid:b9609e62-5991-45e2-9c5f-fdba72fc82d3
https://doi.org/10.1039/d4sc04937c

Thiophene-fused γ-lactams inhibit the SARS-CoV-2 main protease via reversible covalent acylation

Συγγραφείς: Gayatri, Brewitz, L, Ibbotson, L, Salah, E, Basak, S, Choudhry, H, Schofield, CJ

Πηγή: Chem Sci

Θεματικοί όροι: Chemistry, 3. Good health

Σύνδεσμος πρόσβασης: https://pubmed.ncbi.nlm.nih.gov/38784729
https://ora.ox.ac.uk/objects/uuid:6f80c033-1a7b-41d4-9b1a-1125146956e6
https://doi.org/10.1039/d4sc01027b