Cited by 394Rheumatoid Arthritis Research and TherapiesNatural Compounds in Disease TreatmentProtein Kinase Regulation and GTPase Signaling

The DOI matches its Crossref record; 50 of the 50 references it cites were found in a registry or an index.

Specific Btk inhibition suppresses B cell- and myeloid cell-mediated arthritis

Open access

Di Paolo, Julie A, Huang, Tao, Balazs, Mercedesz, Barbosa, James, Barck, Kai H, Bravo, Brandon J, Carano, Richard A D, Darrow, James, Davies, Douglas R, DeForge, Laura E, Diehl, Lauri, Ferrando, Ronald, Gallion, Steven L, Giannetti, Anthony M, Gribling, Peter, Hurez, Vincent, Hymowitz, Sarah G, Jones, Randall, Kropf, Jeffrey E, Lee, Wyne P, Maciejewski, Patricia M, Mitchell, Scott A, Rong, Hong, Staker, Bart L, Whitney, J Andrew, Yeh, Sherry, Young, Wendy B, Yu, Christine, Zhang, Juan, Reif, Karin, Currie, Kevin S·2011·Nature Chemical Biology

DOI 10.1038/nchembio.481

Open this paper in CoChat — free account Open PDF

Abstract

Bruton's tyrosine kinase (Btk) is a therapeutic target for rheumatoid arthritis, but the cellular and molecular mechanisms by which Btk mediates inflammation are poorly understood. Here we describe the discovery of CGI1746, a small-molecule Btk inhibitor chemotype with a new binding mode that stabilizes an inactive nonphosphorylated enzyme conformation. CGI1746 has exquisite selectivity for Btk and inhibits both auto- and transphosphorylation steps necessary for enzyme activation. Using CGI1746, we demonstrate that Btk regulates inflammatory arthritis by two distinct mechanisms. CGI1746 blocks B cell receptor-dependent B cell proliferation and in prophylactic regimens reduces autoantibody levels in collagen-induced arthritis. In macrophages, Btk inhibition abolishes FcγRIII-induced TNFα, IL-1β and IL-6 production. Accordingly, in myeloid- and FcγR-dependent autoantibody-induced arthritis, CGI1746 decreases cytokine levels within joints and ameliorates disease. These results provide new understanding of the function of Btk in both B cell- or myeloid cell-driven disease processes and provide a compelling rationale for targeting Btk in rheumatoid arthritis.

The claims and statistics of this paper haven’t been checked yet.

Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.

Integrity signals

Registry

Crossref · 10.1038/nchembio.481

Cites

50 of 50 references verified0 citation errors · 0 not checkable

Statistics

Claims the paper makes

The claims and statistics of this paper haven’t been checked yet.

Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.

Claims other papers make about this one

Each is checked against this paper’s own text: does it say what the citing paper says it does?

Self-check

Percentages, sums and reported differences re-computed from the paper’s own numbers.

The self-check needs the paper’s full text.

Fcγ receptors as regulators of immune responses
Nimmerjahn, F., & Ravetch, J. V. (2008) · Nature Reviews Immunology · doi:10.1038/nri2206 · Cited by 2,947
A quantitative analysis of kinase inhibitor selectivity
Karaman, M. W., Herrgard, S., Treiber, D. K., Gallant, P., Atteridge, C. E., Campbell, B. T., Chan, K. W., Ciceri, P., Davis, M. I., Edeen, P. T., et al. (2008) · Nature Biotechnology · doi:10.1038/nbt1358 · Cited by 2,466
A Unique Structure for Epidermal Growth Factor Receptor Bound to GW572016 (Lapatinib)
Wood, E. R., Truesdale, A. T., McDonald, O. B., Yuan, D. Y., Hassell, A. M., Dickerson, S. H., Ellis, B., Pennisi, C., Horne, E., Lackey, K. E., et al. (2004) · Cancer Research · doi:10.1158/0008-5472.can-04-1168 · Cited by 1,125
Rational design of inhibitors that bind to inactive kinase conformations
Liu, Y., & Gray, N. S. (2006) · Nature Chemical Biology · doi:10.1038/nchembio799 · Cited by 1,096
Roles of Fc receptors in autoimmunity
Takai, T. (2002) · Nature reviews. Immunology · doi:10.1038/nri856 · Cited by 627
Crystal Structure of Hck in Complex with a Src Family–Selective Tyrosine Kinase Inhibitor
Schindler, T. H., Sicheri, F., Pico, A. R., Gazit, A., Levitzki, A., & Kuriyan, J. (1999) · Molecular Cell · doi:10.1016/s1097-2765(00)80357-3 · Cited by 433
Autoantibody profiling as early diagnostic and prognostic tool for rheumatoid arthritis
Nell, V. P. K., Machold, K. P., Stamm, T. A., Eberl, G., Heinzl, H., Uffmann, M., Smolen, J. S., & Steiner, G. E. (2005) · Annals of the Rheumatic Diseases · doi:10.1136/ard.2005.035691 · Cited by 354
Tyrosine Kinases Btk and Tec Regulate Osteoclast Differentiation by Linking RANK and ITAM Signals
Shinohara, M., Koga, T., Okamoto, K., Sakaguchi, S., Arai, K., Yasuda, H., Takai, T., Kodama, T., Morio, T., Geha, R. S., et al. (2008) · Cell · doi:10.1016/j.cell.2007.12.037 · Cited by 327
B‐lymphocyte contributions to human autoimmune disease
Yanaba, K., Bouaziz, J., Matsushita, T., MAGRO, C. M. J., Clair, E. W. S., & Tedder, T. F. (2008) · Immunological Reviews · doi:10.1111/j.1600-065x.2008.00646.x · Cited by 326
Therapeutic B cell depletion impairs adaptive and autoreactive CD4 + T cell activation in mice
Bouaziz, J., Yanaba, K., Venturi, G. M., Wang, Y., Tisch, R., Poe, J. C., & Tedder, T. F. (2007) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0709205105 · Cited by 315

Flagged first, then by citations

Show all 50 references

Research works printed but not linked: 1

Currie, K.S., DeSimone, R.W., Mitchell, S.A. & Pippin, D.A. Certain heterocyclic substituted imidazo[1,2-a]pyrazin-8-yl compounds and methods of inhibition of Bruton's tyrosine kinase by such compounds. US Patent 7,393,848 (2008).

Sorted by citations

Items 101–200 of 394

Rational Design of Highly Selective Spleen Tyrosine Kinase Inhibitors
Lucas, M. C., GOLDSTEIN, D. M., Hermann, J. C., Kuglstatter, A., Liu, W., Luk, K. C., Padilla, F., Slade, M., Villaseñor, A. G., Wanner, J., et al. (2012) · Journal of Medicinal Chemistry · doi:10.1021/jm301367c · Cited by 52
Bruton’s Tyrosine Kinase Inhibitors: The Next Frontier of B-Cell-Targeted Therapies for Cancer, Autoimmune Disorders, and Multiple Sclerosis
Garg, N., Padron, E., Rammohan, K. W., & Goodman, C. F. (2022) · Journal of Clinical Medicine · doi:10.3390/jcm11206139 · Cited by 54
Investigational Bruton’s tyrosine kinase inhibitors for the treatment of rheumatoid arthritis
Norman, P. (2016) · Expert Opinion on Investigational Drugs · doi:10.1080/13543784.2016.1182499 · Cited by 50
Novel irreversible covalent BTK inhibitors discovered using DNA-encoded chemistry
Guilinger, J. P., Archna, A., Augustin, M., Bergmann, A., Centrella, P. A., Clark, M. A., Cuozzo, J. W., Däther, M., Guié, M.-A., Habeshian, S., et al. (2021) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2021.116223 · Cited by 49
T cells mediate autoantibody-induced cutaneous inflammation and blistering in epidermolysis bullosa acquisita
Bieber, K., Witte, M., Sun, S., Hundt, J. E., Kalies, K., Dräger, S., Kasprick, A., Twelkmeyer, T., Manz, R. A., König, P., et al. (2016) · Scientific Reports · doi:10.1038/srep38357 · Cited by 49
Discovery and Preclinical Characterization of BIIB091, a Reversible, Selective BTK Inhibitor for the Treatment of Multiple Sclerosis
Hopkins, B. T., Bame, E., Bajrami, B., Black, C., Bohnert, T., Boiselle, C., Burdette, D., Burns, J. C., Delva, L., Donaldson, D., et al. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c00926 · Cited by 48
Bruton’s Tyrosine Kinase and Its Isoforms in Cancer
Wang, X., Kokabee, L., Kokabee, M., & Conklin, D. S. (2021) · Frontiers in Cell and Developmental Biology · doi:10.3389/fcell.2021.668996 · Cited by 48
Potential therapies for immune-related adverse events associated with immune checkpoint inhibition: from monoclonal antibodies to kinase inhibition
Berg, M. H., Rincon, S. V. D., & Miller, W. H. (2022) · Journal for ImmunoTherapy of Cancer · doi:10.1136/jitc-2021-003551 · Cited by 53
The therapeutic potential of PROTACs
Benowitz, A. B., Jones, K. L., & Harling, J. D. (2020) · Expert Opinion on Therapeutic Patents · doi:10.1080/13543776.2021.1840553 · Cited by 47
Bruton’s Tyrosine Kinase Inhibition for the Treatment of Rheumatoid Arthritis
Arneson, L. C., Carroll, K., & Ruderman, E. (2021) · ImmunoTargets and Therapy · doi:10.2147/itt.s288550 · Cited by 47
BMX and Its Role in Inflammation, Cardiovascular Disease, and Cancer
Cenni, B., Gutmann, S., & Gottar, M. (2012) · International Reviews of Immunology · doi:10.3109/08830185.2012.663838 · Cited by 47
Nanoparticle-delivered siRNA targeting Bruton's tyrosine kinase for rheumatoid arthritis therapy
Zhao, G., Liu, A., Zhang, Y., Zuo, Z.-Q., Cao, Z., Zhang, H., Xu, C., & Wang, J. (2019) · Biomaterials Science · doi:10.1039/c9bm01025d · Cited by 46
Btk inhibition suppresses agonist-induced human macrophage activation and inflammatory gene expression in RA synovial tissue explants
Hartkamp, L. M., Fine, J. S., van Es, I. E., Tang, M. W., Smith, M. H., Woods, J., Narula, S. K., DeMartino, J. A., Tak, P. P., & Reedquist, K. A. (2014) · Annals of the Rheumatic Diseases · doi:10.1136/annrheumdis-2013-204143 · Cited by 45
Bruton’s tyrosine kinase inhibition attenuates oxidative stress in systemic immune cells and renal compartment during sepsis-induced acute kidney injury in mice
Nadeem, A., Ahmad, S. F., Al-Harbi, N. O., Ibrahim, K. E., Alqahtani, F., Alanazi, W. A., Mahmood, H. M., Alsanea, S., & Attia, S. M. (2020) · International Immunopharmacology · doi:10.1016/j.intimp.2020.107123 · Cited by 45
Differential impact of BTK active site inhibitors on the conformational state of full-length BTK
Joseph, R. E., Amatya, N., Fulton, D. B., Engen, J. R., Wales, T. E., & Andreotti, A. H. (2020) · eLife · doi:10.7554/elife.60470 · Cited by 47
Novel small molecule therapeutics in rheumatoid arthritis
Kelly, V., & Genovese, M. C. (2013) · Rheumatology · doi:10.1093/rheumatology/kes367 · Cited by 44
Bruton's tyrosine kinase is a potential therapeutic target in prostate cancer
Kokabee, L., Wang, X., Sevinsky, C. J., Wang, W. L. W., Cheu, L. A., Chittur, S. V., Karimipoor, M., Tenniswood, M., & Conklin, D. S. (2015) · Cancer Biology & Therapy · doi:10.1080/15384047.2015.1078023 · Cited by 43
Discovery of highly potent and selective Bruton’s tyrosine kinase inhibitors: Pyridazinone analogs with improved metabolic stability
Young, W. B., Barbosa, J., Blomgren, P., Bremer, M. C. D., Crawford, J. J., Dambach, D. M., Eigenbrot, C. W., Gallion, S., Johnson, A. R., Kropf, J. E., et al. (2015) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2015.11.076 · Cited by 43
Self-citation
The Exploration of Chirality for Improved Druggability within the Human Kinome
Saha, D., Kharbanda, A., Yan, W., Lakkaniga, N. R., Frett, B., & Li, H. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b00640 · Cited by 43
Purine derivatives as potent Bruton’s tyrosine kinase (BTK) inhibitors for autoimmune diseases
Shi, Q., Tebben, A. J., Dyckman, A. J., Li, H., Liu, C., Lin, J., Spergel, S. H., Burke, J. R., McIntyre, K. W., Olini, G. C., et al. (2014) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2014.02.075 · Cited by 42
Optimized nanoparticle-mediated delivery of CRISPR-Cas9 system for B cell intervention
Li, M., Fan, Y.-N., Chen, Z., Luo, Y., Wang, Y., Lian, Z., Xu, C., & Wang, J. (2018) · Nano Research · doi:10.1007/s12274-018-2150-5 · Cited by 43
Inflammasome activation controlled by the interplay between post-translational modifications: emerging drug target opportunities
Liang, Z., Damianou, A., Daniel, E. D., & Kessler, B. M. (2021) · Cell Communication and Signaling · doi:10.1186/s12964-020-00688-6 · Cited by 42
Safety, pharmacokinetics, and pharmacodynamics of BMS-986142, a novel reversible BTK inhibitor, in healthy participants
Lee, S. K., Xing, J. W., Catlett, I. M., Adamczyk, R., Griffies, A., Liu, A., Murthy, B., & Nowak, M. (2017) · European Journal of Clinical Pharmacology · doi:10.1007/s00228-017-2226-2 · Cited by 41
A quantitative mechanistic PK/PD model directly connects Btk target engagement and in vivo efficacy
Daryaee, F., Zhang, Z., Gogarty, K. R., Li, Y., Merino, J., Fisher, S. L., & Tonge, P. J. (2017) · Chemical Science · doi:10.1039/c6sc03306g · Cited by 41
The kinase IRAK4 promotes endosomal TLR and immune complex signaling in B cells and plasmacytoid dendritic cells
Corzo, C. A., Varfolomeev, E. E., Setiadi, A., Francis, R., Klabunde, S., Senger, K., Sujatha-Bhaskar, S., Drobnick, J., Do, S., Suto, E., et al. (2020) · Science Signaling · doi:10.1126/scisignal.aaz1053 · Cited by 41
Self-citation
Placement of Water Molecules in Protein Structures: From Large-Scale Evaluations to Single-Case Examples
Nittinger, E., Flachsenberg, F., Bietz, S., Lange, G., Klein, R., & Rarey, M. (2018) · Journal of Chemical Information and Modeling · doi:10.1021/acs.jcim.8b00271 · Cited by 41
Discovery of BIIB068: A Selective, Potent, Reversible Bruton’s Tyrosine Kinase Inhibitor as an Orally Efficacious Agent for Autoimmune Diseases
Ma, B., Bohnert, T., Otipoby, K. L., Tien, E. S., Arefayene, M., Bai, J., Bajrami, B., Bame, E., Chan, T. R., Humora, M. J., et al. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c00702 · Cited by 40
From mechanism to therapies in systemic lupus erythematosus
Paley, M., Strand, V., & Kim, A. H. J. (2017) · Current Opinion in Rheumatology · doi:10.1097/bor.0000000000000369 · Cited by 38
Pharmacokinetic/Pharmacodynamic Modeling in Inflammation
Lon, H., Liu, D., & Jusko, W. J. (2012) · Critical Reviews in Biomedical Engineering · doi:10.1615/critrevbiomedeng.v40.i4.50 · Cited by 38
Discovery of Potent and Selective Tricyclic Inhibitors of Bruton?s Tyrosine Kinase with Improved Druglike Properties
Wang, X., Barbosa, J., Blomgren, P., Bremer, M. C. D., Chen, J., Crawford, J. J., Deng, W., Dong, L., Eigenbrot, C. W., Gallion, S., et al. (2017) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.7b00103 · Cited by 38
Self-citation
Wnt5a causes ROR1 to complex and activate cortactin to enhance migration of chronic lymphocytic leukemia cells
Hasan, M. K., Rassenti, L. Z., Widhopf, G. F., Yu, J., & Kipps, T. J. (2018) · Leukemia · doi:10.1038/s41375-018-0306-7 · Cited by 37
Water molecules in protein–ligand interfaces. Evaluation of software tools and SAR comparison
Nittinger, E., Gibbons, P., Eigenbrot, C. W., Davies, D. R., Maurer, B., Yu, C., Kiefer, J. R., Kuglstatter, A., Murray, J. M., Ortwine, D. F., et al. (2019) · Journal of Computer-Aided Molecular Design · doi:10.1007/s10822-019-00187-y · Cited by 38
Self-citation
Ibrutinib selectively targets FLT3-ITD in mutant FLT3-positive AML
Wu, H., Hu, C., Wang, A., Weisberg, E., Wang, W., Chen, C., Zhao, Z., Yu, K., Liu, J., Wu, J., et al. (2015) · Leukemia · doi:10.1038/leu.2015.175 · Cited by 37
Bruton's tyrosine kinase regulates TLR9 but not TLR7 signaling in human plasmacytoid dendritic cells
Wang, J., Lau, K., Jung, J., Ravindran, P., & Barrat, F. J. (2013) · European Journal of Immunology · doi:10.1002/eji.201344030 · Cited by 39
Aberrant B Cell Selection and Activation in Systemic Lupus Erythematosus
Kil, L. P., & Hendriks, R. W. (2013) · International Reviews of Immunology · doi:10.3109/08830185.2013.786712 · Cited by 38
Ibrutinib
Charalambous, A., Schwarzbich, M., & Witzens‐Harig, M. (2018) · Recent results in cancer research/Recent Results in Cancer Research · doi:10.1007/978-3-319-91439-8_7 · Cited by 36
Exploration of Novel Inhibitors for Bruton’s Tyrosine Kinase by 3D QSAR Modeling and Molecular Dynamics Simulation
Bavi, R., Kumar, R., Choi, L., & Lee, K. W. (2016) · PLoS ONE · doi:10.1371/journal.pone.0147190 · Cited by 36
Successful use of Bruton's kinase inhibitor, ibrutinib, to control paraneoplastic pemphigus in a patient with paraneoplastic autoimmune multiorgan syndrome and chronic lymphocytic leukaemia
Lee, A., Sandhu, S., Imlay‐Gillespie, L., Mulligan, S. P., & Shumack, S. P. (2017) · Australasian Journal of Dermatology · doi:10.1111/ajd.12615 · Cited by 35
Design and Synthesis of Novel Amino-triazine Analogues as Selective Bruton’s Tyrosine Kinase Inhibitors for Treatment of Rheumatoid Arthritis
Kawahata, W., Asami, T., Kiyoi, T., Irie, T., Taniguchi, H., Asamitsu, Y., Inoue, T., Miyake, T., & Sawa, M. (2018) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.8b01147 · Cited by 36
Insulin-like Growth Factor-2 Enhances Functions of Antigen (Ag)-specific Regulatory B Cells
Geng, X., Yang, G., Li, M., Song, J., Liu, Z., Liu, Z., Liu, Z., & Yang, P. (2014) · Journal of Biological Chemistry · doi:10.1074/jbc.m113.515262 · Cited by 33
Noncovalent inhibitors reveal BTK gatekeeper and auto-inhibitory residues that control its transforming activity
Wang, S., Mondal, S., Zhao, C., Berishaj, M., Ghanakota, P., Batlevi, C. L., Doǧan, A., Seshan, V., Abel, R., Green, M. R., et al. (2019) · JCI Insight · doi:10.1172/jci.insight.127566 · Cited by 33
Discovery of novel Bruton’s tyrosine kinase (BTK) inhibitors bearing a pyrrolo[2,3-d]pyrimidine scaffold
Zhao, X., Huang, W., Wang, Y., Xin, M., Qiu, J. J., Cai, J., Tang, F. S., Zhao, Y., & Xiang, H. (2014) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2014.10.043 · Cited by 32
A novel tricyclic BTK inhibitor suppresses B cell responses and osteoclastic bone erosion in rheumatoid arthritis
Liu, Y.-T., Ding, H., Lin, Z., Wang, Q., Chen, L., Liu, S., Yang, X., Zhu, F., Huang, Y.-T., Cao, S., et al. (2021) · Acta Pharmacologica Sinica · doi:10.1038/s41401-020-00578-0 · Cited by 32
Kinase inhibitors: A new tool for the treatment of rheumatoid arthritis
Chakravarty, S. D., Poulikakos, P. I., Ivashkiv, L. B., Salmon, J. E., & Kalliolias, G. D. (2013) · Clinical Immunology · doi:10.1016/j.clim.2013.04.007 · Cited by 32
Design and synthesis of carbazole carboxamides as promising inhibitors of Bruton’s tyrosine kinase (BTK) and Janus kinase 2 (JAK2)
Liu, Q., Batt, D. G., Lippy, J., Surti, N., Tebben, A. J., Muckelbauer, J. K., Chen, L., An, Y., Chang, C., Pokross, M. E., et al. (2015) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2015.07.102 · Cited by 31
The Complement Anaphylatoxins C5a and C3a Suppress IFN-β Production in Response to Listeria monocytogenes by Inhibition of the Cyclic Dinucleotide–Activated Cytosolic Surveillance Pathway
Mueller‐Ortiz, S. L., Calame, D. G., Shenoi, N., Li, Y.-D., & Wetsel, R. A. (2017) · The Journal of Immunology · doi:10.4049/jimmunol.1601420 · Cited by 30
Targeting Bruton's tyrosine kinase for the treatment of B cell associated malignancies and autoimmune diseases: Preclinical and clinical developments of small molecule inhibitors
Zhang, Z., Zhang, D., Liu, Y., Yang, D., Ran, F., Wang, M. L., & Zhao, G. (2018) · Archiv der Pharmazie · doi:10.1002/ardp.201700369 · Cited by 33
Design, synthesis and evaluation of novel 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as potent, selective and reversible Bruton's tyrosine kinase (BTK) inhibitors for the treatment of rheumatoid arthritis
Zhang, C., Pei, H., He, J., Zhu, J., Li, W., Niu, T., Xiang, M., & Chen, L. (2019) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2019.02.077 · Cited by 30
Discovery of 4-Aminoquinoline-3-carboxamide Derivatives as Potent Reversible Bruton’s Tyrosine Kinase Inhibitors for the Treatment of Rheumatoid Arthritis
Yao, X. Y., Sun, X., Jin, S., Yang, L. L., Xu, H., & Rao, Y. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b00329 · Cited by 30
Safety, pharmacokinetics and pharmacodynamics of branebrutinib (BMS‐986195), a covalent, irreversible inhibitor of Bruton's tyrosine kinase: Randomised phase I, placebo‐controlled trial in healthy participants
Catlett, I. M., Nowak, M., Kundu, S., Zheng, N., Liu, A., He, B., Girgis, I. G., & Grasela, D. M. (2020) · British Journal of Clinical Pharmacology · doi:10.1111/bcp.14290 · Cited by 30
Next‐generation Bruton's tyrosine kinase inhibitor BIIB091 selectively and potently inhibits B cell and Fc receptor signaling and downstream functions in B cells and myeloid cells
Bame, E., Tang, H., Burns, J. C., Arefayene, M., Michelsen, K., Ma, B., Marx, I. E., Prince, R. J., Roach, A. M., Poreci, U., et al. (2021) · Clinical & Translational Immunology · doi:10.1002/cti2.1295 · Cited by 31
Progress of small molecules for targeted protein degradation: PROTACs and other technologies
Zhao, H., Xin, M., & Zhang, S. (2023) · Drug Development Research · doi:10.1002/ddr.22026 · Cited by 31
Nonreceptor tyrosine kinases ITK and BTK negatively regulate mast cell proinflammatory responses to lipopolysaccharide
Huang, W., Morales, J. L., Gazivoda, V. P., & August, A. (2015) · Journal of Allergy and Clinical Immunology · doi:10.1016/j.jaci.2015.08.056 · Cited by 31
Bruton's Tyrosine Kinase Inhibition in the Treatment of Preclinical Models and Multiple Sclerosis
Steinmaurer, A., Wimmer, I., Berger, T., Rommer, P. S., & Sellner, J. (2021) · Current Pharmaceutical Design · doi:10.2174/1381612827666210701152934 · Cited by 29
Relevance of lymphocyte subsets to B cell‐targeted therapy in systemic lupus erythematosus
Nakayamada, S., Iwata, S., & Tanaka, Y. (2015) · International Journal of Rheumatic Diseases · doi:10.1111/1756-185x.12534 · Cited by 29
X‐Ray Crystal Structure of Bone Marrow Kinase in the X Chromosome: A Tec Family Kinase
Muckelbauer, J. K., Sack, J. S., Ahmed, N., Burke, J. R., Chang, C. Y., Gao, M., Tino, J. A., Xie, D., & Tebben, A. J. (2011) · Chemical Biology & Drug Design · doi:10.1111/j.1747-0285.2011.01230.x · Cited by 29
Heterogeneity of Toll-like receptor 9 signaling in B cell malignancies and its potential therapeutic application
Bai, L., Chen, W., Chen, J., Li, W., Zhou, L., Niu, C. S., Han, W., & Cui, J. (2017) · Journal of Translational Medicine · doi:10.1186/s12967-017-1152-5 · Cited by 29
Dried plum alleviates symptoms of inflammatory arthritis in TNF transgenic mice
Mirza, F., Lorenzo, J., Drissi, H., Lee, F. Y., & Soung, D. Y. (2017) · The Journal of Nutritional Biochemistry · doi:10.1016/j.jnutbio.2017.10.002 · Cited by 29
Bruton's tyrosine kinase inhibitors in B‐cell non‐Hodgkin's lymphomas
Alinari, L., Quinion, C. D., & Blum, K. (2015) · Clinical Pharmacology & Therapeutics · doi:10.1002/cpt.65 · Cited by 28
A Unique Role for ITK in Survival of Invariant NKT Cells Associated with the p53-Dependent Pathway in Mice
Qi, Q., Huang, W., Bai, Y., Balmus, G., Weiss, R. S., & August, A. (2012) · The Journal of Immunology · doi:10.4049/jimmunol.1102475 · Cited by 28
Bruton's Tyrosine Kinase Deficiency Inhibits Autoimmune Arthritis in Mice but Fails to Block Immune Complex–Mediated Inflammatory Arthritis
Nyhoff, L. E., Barron, B. L., Johnson, E., Bonami, R. H., Maseda, D., Fensterheim, B. A., Han, W., Blackwell, T. S., Crofford, L. J., & Kendall, P. L. (2016) · Arthritis & Rheumatology · doi:10.1002/art.39657 · Cited by 29
Ibrutinib-A double-edge sword in cancer and autoimmune disorders
Kokhaei, P., Jadidi‐Niaragh, F., Jahromi, A. S., Österborg, A., Mellstedt, H., & Hojjat‐Farsangi, M. (2015) · Journal of drug targeting · doi:10.3109/1061186x.2015.1086357 · Cited by 27
Recent advances in targeting protein kinases and pseudokinases in cancer biology
Riegel, K., Vijayarangakannan, P., Kechagioglou, P., Bogucka, K., & Rajalingam, K. (2022) · Frontiers in Cell and Developmental Biology · doi:10.3389/fcell.2022.942500 · Cited by 26
Design, synthesis and evaluation of novel 5-phenylpyridin-2(1H)-one derivatives as potent reversible Bruton’s tyrosine kinase inhibitors
Zhao, X., Xin, M., Huang, W., Ren, Y., Qiu, J. J., Tang, F. S., Jiang, H., Wang, Y., Yang, J., Mo, S., et al. (2014) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2014.11.006 · Cited by 26
Structure–Activity Relationship Study of QL47: A Broad-Spectrum Antiviral Agent
Liang, Y., de Wispelaere, M., Carocci, M., Liu, Q., Wang, J., Yang, P. L., & Gray, N. S. (2017) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.7b00008 · Cited by 28
Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit
Qiu, H., Liu‐Bujalski, L., Caldwell, R. D., Follis, A. V., Gardberg, A. S., Goutopoulos, A., Grenningloh, R., Head, J. C., Johnson, T. L., Jones, R. C., et al. (2018) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2018.07.008 · Cited by 25
Self-citation
Bruton's tyrosine kinase (Btk) inhibitor tirabrutinib suppresses osteoclastic bone resorption
Ariza, Y., Murata, M., Ueda, Y., & Yoshizawa, T. (2019) · Bone Reports · doi:10.1016/j.bonr.2019.100201 · Cited by 26
Discovery and structure-activity relationship of novel diphenylthiazole derivatives as BTK inhibitor with potent activity against B cell lymphoma cell lines
Guo, X., Yang, D., Fan, Z., Zhang, N., Zhao, B., Huang, C., Wang, F., Ma, R., Meng, M., & Deng, Y. (2019) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2019.06.035 · Cited by 24
Design of Potent and Selective Covalent Inhibitors of Bruton’s Tyrosine Kinase Targeting an Inactive Conformation
Pulz, R., Angst, D., Dawson, J., Gessier, F., Gutmann, S., Hersperger, R., Hinniger, A., Janser, P., Koch, G., Révész, L., et al. (2019) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.9b00317 · Cited by 24
A multicenter, open-label, uncontrolled, single-arm phase 2 study of tirabrutinib, an oral Bruton’s tyrosine kinase inhibitor, in pemphigus
Yamagami, J., Ujiie, H., Aoyama, Y., Ishii, N., Tateishi, C., Ishiko, A., Ichijima, T., Hagihara, S., Hashimoto, K., & Amagai, M. (2021) · Journal of Dermatological Science · doi:10.1016/j.jdermsci.2021.07.002 · Cited by 24
Bruton's TK regulates myeloid cell recruitment during acute inflammation
Purvis, G. S. D., Aranda-Tavío, H., Channon, K. M., & Greaves, D. R. (2021) · British Journal of Pharmacology · doi:10.1111/bph.15778 · Cited by 23
Regulation of B lymphocytes and plasma cells by innate immune mechanisms and stromal cells in rheumatoid arthritis
Maseda, D., Bonami, R. H., & Crofford, L. J. (2014) · Expert Review of Clinical Immunology · doi:10.1586/1744666x.2014.907744 · Cited by 24
Safety and Efficacy of Poseltinib, Bruton’s Tyrosine Kinase Inhibitor, in Patients With Rheumatoid Arthritis: A Randomized, Double-blind, Placebo-controlled, 2-part Phase II Study
Genovese, M. C., Spindler, A. J., Sagawa, A., Park, W., Dudek, A., Kivitz, A., Chao, J., Chan, L. S., Witcher, J. W., Barchuk, W., et al. (2020) · The Journal of Rheumatology · doi:10.3899/jrheum.200893 · Cited by 24
Next-generation Bruton’s Tyrosine Kinase (BTK) Inhibitors Potentially Targeting BTK C481S Mutation- Recent Developments and Perspectives
Das, D., Wang, J., & Hong, J. (2022) · Current Topics in Medicinal Chemistry · doi:10.2174/1568026622666220801101706 · Cited by 23
Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4-b]pyrrolizines as Novel Bruton’s Tyrosine Kinase Inhibitors
Xue, Y., Song, P., Song, Z., Wang, A., Tong, L., Geng, M., Ding, J., Liu, Q., Sun, L., Xie, H., et al. (2018) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.8b00441 · Cited by 23
QSAR modelling, molecular docking, molecular dynamic and ADMET prediction of pyrrolopyrimidine derivatives as novel Bruton’s tyrosine kinase (BTK) inhibitors
Aloui, M., Er-rajy, M., Imtara, H., Goudzal, A., Zarougui, S., fadili, M. E., Arthur, D. E., Mothana, R. A., Noman, O. M., Tarayrah, M., et al. (2023) · Saudi Pharmaceutical Journal · doi:10.1016/j.jsps.2023.101911 · Cited by 24
From development to clinical success: the journey of established and next-generation BTK inhibitors
Gupta, S., Sharma, A., Shukla, A. K., Mishra, A., & Singh, A. K. (2025) · Investigational New Drugs · doi:10.1007/s10637-025-01513-y · Cited by 25
Anti-tumor efficacy study of the Bruton’s tyrosine kinase (BTK) inhibitor, ONO/GS-4059, in combination with the glycoengineered type II anti-CD20 monoclonal antibody obinutuzumab (GA101) demonstrates superiorin vivoefficacy compared to ONO/GS-4059 in combination with rituximab
Yasuhiro, T., Sawada, W., Klein, C., Kozaki, R., Hotta, S., & Yoshizawa, T. (2016) · Leukemia & lymphoma/Leukemia and lymphoma · doi:10.1080/10428194.2016.1201567 · Cited by 22
Discovery of N-(3-(5-((3-acrylamido-4-(morpholine-4-carbonyl)phenyl)amino)-1-methyl-6-oxo-1,6-dihydropyridin-3-yl)-2-methylphenyl)-4-(tert-butyl)benzamide (CHMFL-BTK-01) as a highly selective irreversible Bruton's tyrosine kinase (BTK) inhibitor
Liang, Q., Chen, Y., Yu, K., Chen, C., Zhang, S., Wang, A., Wang, W., Wu, H., Liu, X., Wang, B., et al. (2017) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2017.03.001 · Cited by 22
Combined pharmacophore, virtual screening and molecular dynamics studies to identify Bruton’s tyrosine kinase inhibitors
Sakthivel, S., & Mohideen, H. S. (2018) · Journal of Biomolecular Structure and Dynamics · doi:10.1080/07391102.2017.1415821 · Cited by 22
A non‐covalent inhibitor XMU‐MP‐3 overrides ibrutinib‐resistant BtkC481S mutation in B‐cell malignancies
Gui, F., Jiang, J., He, Z., Li, L., Li, Y., Deng, Z., Lu, Y., Wu, X., Chen, G., Su, J., et al. (2019) · British Journal of Pharmacology · doi:10.1111/bph.14809 · Cited by 20
Self-citation
Discovery and Evaluation of Pyrazolo[3,4-d]pyridazinone as a Potent and Orally Active Irreversible BTK Inhibitor
Zhang, X., Sheng, X., Shen, J., Zhang, S., Sun, W., Shen, C., Li, Y., Wang, J., Lv, H., Cui, M., et al. (2019) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.9b00395 · Cited by 23
Emerging immunotherapies for rheumatoid arthritis
Reynolds, G., Cooles, F. A. H., Isaacs, J. D., & Hilkens, C. M. U. (2014) · Human Vaccines & Immunotherapeutics · doi:10.4161/hv.27910 · Cited by 21
Reining in BTK: Interdomain Interactions and Their Importance in the Regulatory Control of BTK
Kueffer, L. E., Joseph, R. E., & Andreotti, A. H. (2021) · Frontiers in Cell and Developmental Biology · doi:10.3389/fcell.2021.655489 · Cited by 22
Preclinical Mechanisms of Topical PRN473, a Bruton Tyrosine Kinase Inhibitor, in Immune-Mediated Skin Disease Models
Xing, Y., Chu, K. A., Wadhwa, J., Chen, W., Zhu, J., Bradshaw, J. M., Shu, J., Foulke, M. C., Loewenstein, N., Nunn, P. A., et al. (2021) · ImmunoHorizons · doi:10.4049/immunohorizons.2100063 · Cited by 20
Rilzabrutinib, a reversible covalent Bruton's tyrosine kinase inhibitor: Absorption, metabolism, excretion, and absolute bioavailability in healthy participants
Ucpinar, S., Smith, P. F., Li, L., Li, F., Yan, H., Wadhwa, J., Chu, K. A., Shu, J., Nunn, P. A., & Li, M. (2023) · Clinical and Translational Science · doi:10.1111/cts.13524 · Cited by 20
Breaking good: the inexorable rise of BTK inhibitors in the treatment of chronic lymphocytic leukaemia
Hutchinson, C. V., & Dyer, M. J. S. (2014) · British Journal of Haematology · doi:10.1111/bjh.12895 · Cited by 21
The Immunomodulatory Mechanisms of BTK Inhibition in CLL and Beyond
Jiang, Q., Peng, Y., Herling, C., & Herling, M. (2024) · Cancers · doi:10.3390/cancers16213574 · Cited by 19
Inhibition of BTK protects lungs from trauma-hemorrhagic shock-induced injury in rats
Liu, X., Zhang, J., Han, W., Wang, Y., Liu, Y., Zhang, Y., Zhou, D., & Xiang, L. (2017) · Molecular Medicine Reports · doi:10.3892/mmr.2017.6553 · Cited by 19
Self-citation
Discovery of thieno[3,2-c]pyridin-4-amines as novel Bruton’s tyrosine kinase (BTK) inhibitors
Zhao, X., Xin, M., Wang, Y., Huang, W., Qiu, J. J., Tang, F. S., Wu, G., Zhao, Y., & Xiang, H. (2015) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2015.05.043 · Cited by 19
The Role of the Tec Kinase Bruton's Tyrosine Kinase (Btk) in Leukocyte Recruitment
Block, H., & Zarbock, A. (2012) · International Reviews of Immunology · doi:10.3109/08830185.2012.668982 · Cited by 20
Advances in kinase inhibition
Gadina, M. (2014) · Current Opinion in Rheumatology · doi:10.1097/bor.0000000000000023 · Cited by 19
Targeting rheumatoid arthritis: a molecular perspective on biologic therapies and clinical progress
Jain, A., Bishnoi, M., Prajapati, S. K., Acharya, S., Kapre, S., Singhvi, G., & Palakurthi, S. (2025) · Journal of Biological Engineering · doi:10.1186/s13036-025-00534-8 · Cited by 19
Current Perspectives: Evidence to Date on BTK Inhibitors in the Management of Multiple Sclerosis
Contentti, E. C., & Correale, J. D. (2022) · Drug Design Development and Therapy · doi:10.2147/dddt.s348129 · Cited by 18
Discovery of novel BTK inhibitors with carboxylic acids
Gao, X., Wang, J., Liu, J., Guiadeen, D., Krikorian, A. D., Boga, S. B., Alhassan, A., Selyutin, O., Yu, W., Yu, Y., et al. (2016) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2016.11.079 · Cited by 18
Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk
Caldwell, R. D., Liu‐Bujalski, L., Qiu, H., Mochalkin, I., Jones, R. C., Neagu, C., Goutopoulos, A., Grenningloh, R., Johnson, T. L., Sherer, B., et al. (2018) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2018.09.033 · Cited by 18
Self-citation
Population Pharmacokinetics, Efficacy Exposure-response Analysis, and Model-based Meta-analysis of Fenebrutinib in Subjects with Rheumatoid Arthritis
Chan, P., Yu, J., Chinn, L. W., Prohn, M., Huisman, J., Matzuka, B., Hanley, W. D., Tuckwell, K., & Quartino, A. L. (2020) · Pharmaceutical Research · doi:10.1007/s11095-019-2752-y · Cited by 18
Stereochemical Differences in Fluorocyclopropyl Amides Enable Tuning of Btk Inhibition and Off-Target Activity
Crawford, J. J., Lee, W., Johnson, A. R., Delatorre, K. J., Chen, J., Eigenbrot, C. W., Heidmann, J. D., Kakiuchi-Kiyota, S., Katewa, A., Kiefer, J. R., et al. (2020) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.0c00249 · Cited by 18
Self-citation
Discovery of potent and selective reversible Bruton’s tyrosine kinase inhibitors
Qiu, H., Ali, Z., Bender, A. T., Caldwell, R. D., Chen, Y.-Y., Fang, Z., Gardberg, A. S., Glaser, N., Goettsche, A., Goutopoulos, A., et al. (2021) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2021.116163 · Cited by 18
Self-citation
Proteolysis-targeting chimeras in biotherapeutics: Current trends and future applications
Li, Q., Zhou, L., Qin, S., Huang, Z., Li, B., Li, B., Yang, M., Nice, E. C., Zhu, H., & Huang, C. (2023) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2023.115447 · Cited by 17

Authors: Di Paolo, J. A., Huang, T., Balazs, M., Barbosa, J., Barck, K. H., Bravo, B. J., Carano, R. A. D., Darrow, J., Davies, D. R., DeForge, L. E., Diehl, L., Ferrando, R., Gallion, S. L., Giannetti, A. M., Gribling, P., Hurez, V., Hymowitz, S. G., Jones, R., Kropf, J. E., Lee, W. P., Maciejewski, P. M., Mitchell, S. A., Rong, H., Staker, B. L., Whitney, J. A., Yeh, S., Young, W. B., Yu, C., Zhang, J., Reif, K., & Currie, K. S.
Affiliations: Genentech (US)
The University of Texas at San Antonio Health Science Center (US)
Corresponding author: Reif, Karin
Currie, Kevin S
ORCID: Huang, Tao
Barck, Kai H
Carano, Richard A D
Davies, Douglas R
Diehl, Lauri
Hurez, Vincent
Hymowitz, Sarah G
Lee, Wyne P
Maciejewski, Patricia M
Mitchell, Scott A
Rong, Hong
Staker, Bart L
Whitney, J Andrew
Yeh, Sherry
Yu, Christine
Zhang, Juan
Reif, Karin
Currie, Kevin S
Venue: Nature Chemical Biology
Publisher: Springer Science and Business Media LLC
Published: 2010-11-28
Volume: 7
Issue: 1
Pages: 41-50
ISSN: 1552-4450 (ISSN-L)
1552-4469
DOI: 10.1038/nchembio.481
OpenAlex: W2093522627
Cited by: 340
References: 50
Citations by year: 2026: 15 · 2025: 16 · 2024: 13 · 2023: 14 · 2022: 26 · 2021: 35 · 2020: 29 · 2019: 25 · 2018: 22 · 2017: 33 · 2016: 22 · 2015: 26 · 2014: 23 · 2013: 16 · 2012: 15
FWCI: 9.81
Type: journal article
Language: en
Open access: bronze
doi.org
Licence: www.springernature.com/gp/researchers/text-and-data-mining (tdm)
www.springernature.com/gp/researchers/text-and-data-mining (vor)
Locations: Nature Chemical Biology (publishedVersion)
PubMed (publishedVersion)
Funders: Genentech
Topics: Health Sciences › Medicine › Rheumatology › Rheumatoid Arthritis Research and Therapies
Health Sciences › Medicine › Complementary and alternative medicine › Natural Compounds in Disease Treatment
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Kinase Regulation and GTPase Signaling
Keywords: Bruton's tyrosine kinase, BTK inhibition, rheumatoid arthritis, inflammatory arthritis, B cell receptor signaling, FcγRIII, macrophage cytokine production, TNF-α, IL-1β, interleukin-6, B cell proliferation, collagen-induced arthritis
MeSH terms: Agammaglobulinaemia Tyrosine Kinase, Animals, Arthritis, Experimental, Arthritis, Rheumatoid, Autoantibodies, B-Lymphocytes, Benzamides, Enzyme Activation, Phosphorylation, Protein-Tyrosine Kinases, Tumor Necrosis Factor-alpha, Interleukin-6, Bridged Bicyclo Compounds, Heterocyclic, Myeloid Cells, Protein Kinase Inhibitors, Cell Proliferation, Mice, Interleukin-1beta

About these checks

Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.

Statistics and arithmetic are recomputed, not judged.

Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.

What counts as a claim ›How we measure confidence ›How we check this ›

Are you an author, or do you see a problem with this page? Request a review

Specific Btk inhibition suppresses B cell- and myeloid cell-mediated arthritis

Abstract

Overview

Integrity signals

Verification

Claims the paper makes

Claims other papers make about this one

Self-check

Citations

Cites

Cited by

Related

Metadata

Record

About these checks