C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays

Autor: Le Bihan, Y-V, Lanigan, RM, Atrash, B, McLaughlin, MG, Velupillai, S, Malcolm, AG, England, KS, Ruda, GF, Mok, NY, Tumber, A, Tomlin, K, Saville, H, Shehu, E, McAndrew, C, Carmichael, L, Bennett, JM, Jeganathan, F, Eve, P, Donovan, A, Hayes, A, Wood, F, Raynaud, FI, Fedorov, O, Brennan, PE, Burke, R, Van Montfort, RLM, Rossanese, OW, Blagg, J, Bavetsias, V

Publikováno v: European Journal of Medicinal Chemistry
Le Bihan, Y-V, Lanigan, R M, Atrash, B, McLaughlin, M G, Velupillai, S, Malcolm, A G, England, K S, Ruda, G F, Mok, N Y, Tumber, A, Tomlin, K, Saville, H, Shehu, E, McAndrew, C, Carmichael, L, Bennett, J M, Jeganathan, F, Eve, P, Donovan, A, Hayes, A, Wood, F, Raynaud, F I, Fedorov, O, Brennan, P, Burke, R, van Montfort, R L M, Rossanese, O W, Blagg, J & Bavetsias, V 2019, ' C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays ', European Journal of Medicinal Chemistry, vol. 177, pp. 316-337 . https://doi.org/10.1016/j.ejmech.2019.05.041

Residues in the histone substrate binding sites that differ between the KDM4 and KDM5 subfamilies were identified. Subsequently, a C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-one series was designed to rationally exploit these residue differences bet

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid_dedup__::b23e38e79895cd396b4e21c1fb1c9678
http://europepmc.org/articles/PMC6580095

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Publikováno v: Solid-State Electronics. Jan2017, Vol. 127, pIFC-IFC. 1p.

Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 In Vivo .

Autor: Huckvale R; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K., Harnden AC; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K., Cheung KJ; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K., Pierrat OA; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K., Talbot R; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K., Box GM; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K., Henley AT; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K., de Haven Brandon AK; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K., Hallsworth AE; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K., Bright MD; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K., Akpinar HA; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K., Miller DSJ; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K., Tarantino D; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K., Gowan S; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K., Hayes A; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K., Gunnell EA; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K.; Division of Structural Biology, The Institute of Cancer Research, London SM2 5NG, U.K., Brennan A; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K., Davis OA; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K., Johnson LD; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K., de Klerk S; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K., McAndrew C; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K., Le Bihan YV; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K.; Division of Structural Biology, The Institute of Cancer Research, London SM2 5NG, U.K., Meniconi M; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K., Burke R; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K., Kirkin V; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K., van Montfort RLM; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K.; Division of Structural Biology, The Institute of Cancer Research, London SM2 5NG, U.K., Raynaud FI; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K., Rossanese OW; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K., Bellenie BR; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K., Hoelder S; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, U.K.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2022 Jun 23; Vol. 65 (12), pp. 8191-8207. Date of Electronic Publication: 2022 Jun 02.

A super-potent tetramerized ACE2 protein displays enhanced neutralization of SARS-CoV-2 virus infection.

Autor: Miller A; Institute of Cancer Research, 15 Cotswold Road, Sutton, London, SM2 5NG, UK., Leach A; Institute of Cancer Research, 15 Cotswold Road, Sutton, London, SM2 5NG, UK., Thomas J; Institute of Cancer Research, 15 Cotswold Road, Sutton, London, SM2 5NG, UK., McAndrew C; Institute of Cancer Research, 15 Cotswold Road, Sutton, London, SM2 5NG, UK., Bentley E; National Institute for Biological Standards and Control, Blanche Lane, South Mimms, Hertfordshire, EN6 3QG, UK., Mattiuzzo G; National Institute for Biological Standards and Control, Blanche Lane, South Mimms, Hertfordshire, EN6 3QG, UK., John L; Department of LABMED, National Veterinary Institute (SVA), 751 89, Uppsala, Sweden.; Karolinska Institute, 17177, Stockholm, Sweden., Mirazimi A; Department of LABMED, National Veterinary Institute (SVA), 751 89, Uppsala, Sweden.; Karolinska Institute, 17177, Stockholm, Sweden., Harris G; Research Complex at Harwell, Rutherford Appleton Laboratory, Oxon, OX11 0FA, UK., Gamage N; Membrane Protein Laboratory, Diamond Light Source, Harwell Science and Innovation Campus, Didcot, OX11 0DE, UK., Carr S; Research Complex at Harwell, Rutherford Appleton Laboratory, Oxon, OX11 0FA, UK., Ali H; Quadrucept Limited, 1010 Cambourne Road, Cambridge, CB23 6DW, UK., Van Montfort R; Institute of Cancer Research, 15 Cotswold Road, Sutton, London, SM2 5NG, UK., Rabbitts T; Institute of Cancer Research, 15 Cotswold Road, Sutton, London, SM2 5NG, UK. terry.rabbitts@icr.ac.uk.

Publikováno v: Scientific reports [Sci Rep] 2021 May 19; Vol. 11 (1), pp. 10617. Date of Electronic Publication: 2021 May 19.

Successful transatlantic bilateral hand transplant in a young female highly sensitized to HLA class II antigens.

Autor: Azoury SC; Division of Plastic Surgery, Department of Surgery, University of Pennsylvania, Philadelphia, PA, USA., Johnson FB; Department of Pathology and Laboratory Medicine, University of Pennsylvania, Philadelphia, PA, USA., Levine M; Penn Transplant Institute, University of Pennsylvania, Philadelphia, PA, USA., Veasey S; Penn Transplant Institute, University of Pennsylvania, Philadelphia, PA, USA., McAndrew C; Department of Orthopedic Surgery, University of Pennsylvania, Philadelphia, PA, USA., Shaked A; Penn Transplant Institute, University of Pennsylvania, Philadelphia, PA, USA., Lantieri L; Department of Plastic, Reconstructive, and Aesthetic Surgery, Hôpital Européen Georges Pompidou, Assistance Publique-Hôpitaux de Paris, Paris, France, Université de Paris, Paris Descartes, Paris, France., Kamoun M; Department of Pathology and Laboratory Medicine, Hospital of the University of Pennsylvania, Philadelphia, PA, USA., Levin LS; Division of Plastic Surgery, Department of Surgery, University of Pennsylvania, Philadelphia, PA, USA; Penn Transplant Institute, University of Pennsylvania, Philadelphia, PA, USA; Department of Orthopedic Surgery, University of Pennsylvania, Philadelphia, PA, USA. Electronic address: Scott.levin@pennmedicine.upenn.edu.

Publikováno v: Transplant immunology [Transpl Immunol] 2021 Apr; Vol. 65, pp. 101377. Date of Electronic Publication: 2021 Feb 18.