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Publications in the selection

20 hits

Bibliografisk träff 2024-05-28

Discovery of GLPG3667, a Selective ATP Competitive Tyrosine Kinase 2 Inhibitor for the Treatment of Autoimmune Diseases.

Mammoliti O, Martina S, Claes P, Coti G, Blanque R, Jagerschmidt C, Shoji K, Borgonovi M, De Vos S, Marsais F, Oste L, Quinton E, López-Ramos M, Amantini D, Brys R, Jimenez JM, Galien R, van der Plas S.

J Med Chem · research support, non-u.s. gov't; research-article; clinical trial, phase i; journal article · DOI 10.1021/acs.jmedchem.4c00769

Bibliografisk träff 2023-12-20

Discovery of pyrazolo[3,4-d]pyrimidines as novel mitogen-activated protein kinase kinase 3 (MKK3) inhibitors.

Takarada JE, Cunha MR, Almeida VM, Vasconcelos SNS, Santiago AS, Godoi PH, Salmazo A, Ramos PZ, Fala AM, de Souza LR, Da Silva IEP, Bengtson MH, Massirer KB, Couñago RM.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2023.117561

Bibliografisk träff 2023-11-30

Identification and Biological Evaluation of a Potent and Selective JAK1 Inhibitor for the Treatment of Pulmonary Fibrosis.

Park E, Park S, Lee SJ, Jeong D, Jin H, Moon H, Cha B, Kim D, Ma S, Seo W, Han SH, Lee YS, Kang S.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.3c01712

Bibliografisk träff 2023-09-29

Synthesis and clinical application of small-molecule inhibitors of Janus kinase.

Zhang JY, Sun JF, Nie P, Herdewijn P, Wang YT.

Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2023.115848

Bibliografisk träff 2022-12-13

Identification of TUL01101: A Novel Potent and Selective JAK1 Inhibitor for the Treatment of Rheumatoid Arthritis.

Zhou S, Mao W, Su Y, Zheng X, Qian W, Shen M, Shan N, Li Y, Wang D, Wu S, Sun T, Mu L.

J Med Chem · journal article · DOI 10.1021/acs.jmedchem.2c01550

Bibliografisk träff 2022-06-18

Dual-target Janus kinase (JAK) inhibitors: Comprehensive review on the JAK-based strategies for treating solid or hematological malignancies and immune-related diseases.

Shen P, Wang Y, Jia X, Xu P, Qin L, Feng X, Li Z, Qiu Z.

Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2022.114551

Bibliografisk träff 2021-03-10

Synergistic effects of type I PRMT and PARP inhibitors against non-small cell lung cancer cells.

Dominici C, Sgarioto N, Yu Z, Sesma-Sanz L, Masson JY, Richard S, Raynal NJ.

Clin Epigenetics · research support, non-u.s. gov't; research-article; journal article · DOI 10.1186/s13148-021-01037-1

Bibliografisk träff 2021-02-18

Small molecule approaches to treat autoimmune and inflammatory diseases (Part I): Kinase inhibitors.

Zheng J, Wu J, Ding X, Shen HC, Zou G.

Bioorg Med Chem Lett · review; journal article · DOI 10.1016/j.bmcl.2021.127862

Bibliografisk träff 2021-02-04

Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.

Raghuvanshi R, Bharate SB.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.0c01467

Bibliografisk träff 2021-01-11

Discovery and Biological Evaluation of N-Methyl-pyrrolo[2,3-b]pyridine-5-carboxamide Derivatives as JAK1-Selective Inhibitors.

Park E, Lee SJ, Moon H, Park J, Jeon H, Hwang JS, Hwang H, Hong KB, Han SH, Choi S, Kang S.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.0c01026

Bibliografisk träff 2020-04-28

Discovery of triazolo [1,5-a] pyridine derivatives as novel JAK1/2 inhibitors.

Lu K, Wu W, Zhang C, Liu Z, Xiao B, Yuan Z, Li A, Chen D, Zhai X, Jiang Y.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2020.127225

Bibliografisk träff 2020-02-18

Janus kinases (JAKs): The efficient therapeutic targets for autoimmune diseases and myeloproliferative disorders.

Xu P, Shen P, Yu B, Xu X, Ge R, Cheng X, Chen Q, Bian J, Li Z, Wang J.

Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2020.112155

Bibliografisk träff 2018-02-03

Development of selective inhibitors for the treatment of rheumatoid arthritis: (R)-3-(3-(Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)pyrrolidin-1-yl)-3-oxopropanenitrile as a JAK1-selective inhibitor.

Chough C, Joung M, Lee S, Lee J, Kim JH, Kim BM.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2018.01.021

Bibliografisk träff 2018-01-15

Design, synthesis and evaluation of (R)-3-(7-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-5-azaspiro[2.4]heptan-5-yl)-3-oxopropanenitrile as a JAK1-selective inhibitor.

Chough C, Lee S, Joung M, Lee J, Kim JH, Kim BM.

Medchemcomm · research-article; journal article · DOI 10.1039/c7md00568g

Bibliografisk träff 2017-12-01

The target landscape of clinical kinase drugs.

Klaeger S, Heinzlmeir S, Wilhelm M, Polzer H, Vick B, Koenig PA, Reinecke M, Ruprecht B, Petzoldt S, Meng C, Zecha J, Reiter K, Qiao H, Helm D, Koch H, Schoof M, Canevari G, Casale E, Depaolini SR, Feuchtinger A, Wu Z, Schmidt T, Rueckert L, Becker W, Huenges J, Garz AK, Gohlke BO, Zolg DP, Kayser G, Vooder T, Preissner R, Hahne H, Tõnisson N, Kramer K, Götze K, Bassermann F, Schlegl J, Ehrlich HC, Aiche S, Walch A, Greif PA, Schneider S, Felder ER, Ruland J, Médard G, Jeremias I, Spiekermann K, Kuster B.

Science · research support, non-u.s. gov't; research-article; journal article · DOI 10.1126/science.aan4368

Bibliografisk träff 2017-05-17

JAK2 JH2 Fluorescence Polarization Assay and Crystal Structures for Complexes with Three Small Molecules.

Newton AS, Deiana L, Puleo DE, Cisneros JA, Cutrona KJ, Schlessinger J, Jorgensen WL.

ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/acsmedchemlett.7b00154

Bibliografisk träff 2015-09-01

Benzimidazole Derivatives as Potent JAK1-Selective Inhibitors.

Kim MK, Shin H, Park KS, Kim H, Park J, Kim K, Nam J, Choo H, Chong Y.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.5b01263

Bibliografisk träff 2014-11-17

Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.

Menet CJ, Fletcher SR, Van Lommen G, Geney R, Blanc J, Smits K, Jouannigot N, Deprez P, van der Aar EM, Clement-Lacroix P, Lepescheux L, Galien R, Vayssiere B, Nelles L, Christophe T, Brys R, Uhring M, Ciesielski F, Van Rompaey L.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm501262q

Bibliografisk träff 2014-01-23

Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases.

Clark JD, Flanagan ME, Telliez JB.

J Med Chem · research support, non-u.s. gov't; review; journal article · DOI 10.1021/jm401490p

Bibliografisk träff 2013-09-04

Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases.

Van Rompaey L, Galien R, van der Aar EM, Clement-Lacroix P, Nelles L, Smets B, Lepescheux L, Christophe T, Conrath K, Vandeghinste N, Vayssiere B, De Vos S, Fletcher S, Brys R, van 't Klooster G, Feyen JH, Menet C.

J Immunol · research support, non-u.s. gov't; journal article · DOI 10.4049/jimmunol.1201348

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Publications in the selection

Discovery of GLPG3667, a Selective ATP Competitive Tyrosine Kinase 2 Inhibitor for the Treatment of Autoimmune Diseases.

Discovery of pyrazolo[3,4-d]pyrimidines as novel mitogen-activated protein kinase kinase 3 (MKK3) inhibitors.

Identification and Biological Evaluation of a Potent and Selective JAK1 Inhibitor for the Treatment of Pulmonary Fibrosis.

Synthesis and clinical application of small-molecule inhibitors of Janus kinase.

Identification of TUL01101: A Novel Potent and Selective JAK1 Inhibitor for the Treatment of Rheumatoid Arthritis.

Dual-target Janus kinase (JAK) inhibitors: Comprehensive review on the JAK-based strategies for treating solid or hematological malignancies and immune-related diseases.

Synergistic effects of type I PRMT and PARP inhibitors against non-small cell lung cancer cells.

Small molecule approaches to treat autoimmune and inflammatory diseases (Part I): Kinase inhibitors.

Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.

Discovery and Biological Evaluation of <i>N</i>-Methyl-pyrrolo[2,3-<i>b</i>]pyridine-5-carboxamide Derivatives as JAK1-Selective Inhibitors.

Discovery of triazolo [1,5-a] pyridine derivatives as novel JAK1/2 inhibitors.

Janus kinases (JAKs): The efficient therapeutic targets for autoimmune diseases and myeloproliferative disorders.

Development of selective inhibitors for the treatment of rheumatoid arthritis: (R)-3-(3-(Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)pyrrolidin-1-yl)-3-oxopropanenitrile as a JAK1-selective inhibitor.

Design, synthesis and evaluation of (<i>R</i>)-3-(7-(methyl(7<i>H</i>-pyrrolo[2,3-<i>d</i>]pyrimidin-4-yl)amino)-5-azaspiro[2.4]heptan-5-yl)-3-oxopropanenitrile as a JAK1-selective inhibitor.

The target landscape of clinical kinase drugs.

JAK2 JH2 Fluorescence Polarization Assay and Crystal Structures for Complexes with Three Small Molecules.

Benzimidazole Derivatives as Potent JAK1-Selective Inhibitors.

Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.

Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases.

Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases.