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

Skepinone-L, a Novel Potent and Highly Selective Inhibitor of p38 MAP Kinase, Effectively Impairs Platelet Activation and Thrombus Formation
Borst, O., Walker, B., Münzer, P., Russo, A., Schmid, E., Faggio, C., Bigalke, B., Laufer, S., Gawaz, M., & Lang, F. J. W. (2013) · Cellular Physiology and Biochemistry · doi:10.1159/000350110 · Cited by 1,867
Pathogenetic insights from the treatment of rheumatoid arthritis
McInnes, I. B., & Schett, G. A. (2017) · The Lancet · doi:10.1016/s0140-6736(17)31472-1 · Cited by 1,420
PROTACs: past, present and future
Li, K., & Crews, C. M. (2022) · Chemical Society Reviews · doi:10.1039/d2cs00193d · Cited by 869
B cell depletion therapies in autoimmune disease: advances and mechanistic insights
Lee, D. S. W., Rojas, O. L., & Gommerman, J. L. (2020) · Nature Reviews Drug Discovery · doi:10.1038/s41573-020-00092-2 · Cited by 684
Targeting Bruton's tyrosine kinase in B cell malignancies
Hendriks, R. W., Yuvaraj, S., & Kil, L. P. (2014) · Nature reviews. Cancer · doi:10.1038/nrc3702 · Cited by 580
Prolonged and tunable residence time using reversible covalent kinase inhibitors
Bradshaw, J. M., McFarland, J. M., Paavilainen, V. O., Bisconte, A. R., Tam, D., Phan, V. T., Romanov, S., Finkle, D., Shu, J., Patel, V. P., et al. (2015) · Nature Chemical Biology · doi:10.1038/nchembio.1817 · Cited by 437
Kinase inhibition in autoimmunity and inflammation
Zarrin, A. A., Bao, K., Lupardus, P., & Vucic, D. (2021) · Nature Reviews Drug Discovery · doi:10.1038/s41573-020-0082-8 · Cited by 431
Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase
Guo, Y., Liu, Y., Hu, N., Yu, D., Zhou, C., Shi, G., Zhang, B., Wei, M., Liu, J., Luo, L., et al. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b00687 · Cited by 376
Chemistries of bifunctional PROTAC degraders
Cao, C., He, M., Wang, L., He, Y., & Rao, Y. (2022) · Chemical Society Reviews · doi:10.1039/d2cs00220e · Cited by 313
Drug–Target Kinetics in Drug Discovery
Tonge, P. J. (2017) · ACS Chemical Neuroscience · doi:10.1021/acschemneuro.7b00185 · Cited by 304
The ins and outs of selective kinase inhibitor development
Müller, S., Chaikuad, A., Gray, N. S., & Knapp, S. (2015) · Nature Chemical Biology · doi:10.1038/nchembio.1938 · Cited by 276
Bruton’s Tyrosine Kinase: An Emerging Key Player in Innate Immunity
Weber, A. N. R., Bittner, Z., Liu, X., Dang, T., Radsak, M. P., & Brunner, C. (2017) · Frontiers in Immunology · doi:10.3389/fimmu.2017.01454 · Cited by 271
A phase 1 clinical trial of the selective BTK inhibitor ONO/GS-4059 in relapsed and refractory mature B-cell malignancies
Walter, H. S., Rule, S. A., Dyer, M. J. S., Karlin, L., Jones, C. H., Cazin, B., Quittet, P., Shah, N., Hutchinson, C. V., Honda, H., et al. (2015) · Blood · doi:10.1182/blood-2015-08-664086 · Cited by 274
Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton’s Tyrosine Kinase Inhibitor in Early Clinical Development
Crawford, J. J., Johnson, A. R., Misner, D., Belmont, L. D., Castanedo, G. M., Choy, R., Coraggio, M., Dong, L., Eigenbrot, C. W., Erickson, R., et al. (2018) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.7b01712 · Cited by 264
Self-citation
Ibrutinib and novel BTK inhibitors in clinical development
Akinleye, A., Chen, Y., Mukhi, N., Song, Y., & Liu, D. (2013) · Journal of Hematology & Oncology · doi:10.1186/1756-8722-6-59 · Cited by 234
Inhibition of Btk with CC-292 Provides Early Pharmacodynamic Assessment of Activity in Mice and Humans
Evans, E. K., Tester, R. W., Aslanian, S., Karp, R., Sheets, M. P., Labenski, M., Witowski, S. R., Lounsbury, H. A., Chaturvedi, P., Mazdiyasni, H., et al. (2013) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.113.203489 · Cited by 226
Ibrutinib antagonizes rituximab-dependent NK cell–mediated cytotoxicity
Kohrt, H. E. K., Sagiv-Barfi, I., Rafiq, S., Herman, S. E. M., Butchar, J. P., Cheney, C. M., Zhang, X., Buggy, J. J., Muthusamy, N., Levy, R., et al. (2014) · Blood · doi:10.1182/blood-2014-01-547869 · Cited by 218
Bruton tyrosine kinase inhibitors for multiple sclerosis
Krämer, J., Bar-Or, A., Turner, T. J., & Wiendl, H. (2023) · Nature Reviews Neurology · doi:10.1038/s41582-023-00800-7 · Cited by 206
Ability of Bruton’s Tyrosine Kinase Inhibitors to Sequester Y551 and Prevent Phosphorylation Determines Potency for Inhibition of Fc Receptor but not B-Cell Receptor Signaling
Bender, A. T., Gardberg, A. S., Pereira, A., Johnson, T. L., Wu, Y., Grenningloh, R., Head, J. C., Morandi, F., Haselmayer, P., & Liu‐Bujalski, L. (2017) · Molecular Pharmacology · doi:10.1124/mol.116.107037 · Cited by 198
Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase
Angst, D., Gessier, F., Janser, P., Vulpetti, A., Wälchli, R., Beerli, C., Littlewood-Evans, A. J., Dawson, J., Nuesslein‐Hildesheim, B., Wieczorek, G., et al. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b01916 · Cited by 181
The development of Bruton's tyrosine kinase (BTK) inhibitors from 2012 to 2017: A mini-review
Liang, C., Tian, D., Ren, X., Ding, S., Jia, M., Xin, M., & Thareja, S. (2018) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2018.03.062 · Cited by 178
Bruton tyrosine kinase degradation as a therapeutic strategy for cancer
Dobrovolsky, D., Wang, E. S., Morrow, S., Leahy, C., Faust, T., Nowak, R. P., Donovan, K. A., Yang, G., Li, Z., Fischer, E. S., et al. (2019) · Blood · doi:10.1182/blood-2018-07-862953 · Cited by 169
Bruton tyrosine kinase inhibition is a novel therapeutic strategy targeting tumor in the bone marrow microenvironment in multiple myeloma
Tai, Y., Chang, B. Y., Kong, S., Fulciniti, M., Yang, G., Calle, Y., Hu, Y., Lin, J., Zhao, J., Cagnetta, A., et al. (2012) · Blood · doi:10.1182/blood-2011-12-396853 · Cited by 168
BTK inhibitors in the treatment of hematological malignancies and inflammatory diseases: mechanisms and clinical studies
Alu, A., Lei, H., Han, X., Wei, Y., & Wei, X. (2022) · Journal of Hematology & Oncology · doi:10.1186/s13045-022-01353-w · Cited by 159
Bruton tyrosine kinase inhibitor ibrutinib (PCI-32765)
Burger, J. A., & Buggy, J. J. (2013) · Leukemia & lymphoma/Leukemia and lymphoma · doi:10.3109/10428194.2013.777837 · Cited by 156
Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton’s Tyrosine Kinase (BTK) Conformationally Constrained by Two Locked Atropisomers
Watterson, S. H., Lucca, G. V. D., Shi, Q., Langevine, C. M., Liu, Q., Batt, D. G., Bertrand, M. B., Gong, H., Dai, J., Yip, S. H., et al. (2016) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b01088 · Cited by 153
Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton’s Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases
Caldwell, R. D., Qiu, H., Askew, B. C., Bender, A. T., Brügger, N., Camps, M., Dhanabal, M., Dutt, V., Eichhorn, T., Gardberg, A. S., et al. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b00794 · Cited by 152
Self-citation
Efficacy and Pharmacodynamic Modeling of the BTK Inhibitor Evobrutinib in Autoimmune Disease Models
Haselmayer, P., Camps, M., Liu‐Bujalski, L., Nguyen, N. T. K., Morandi, F., Head, J. C., O’Mahony, A., Zimmerli, S. C., Bruns, L., Bender, A. T., et al. (2019) · The Journal of Immunology · doi:10.4049/jimmunol.1800583 · Cited by 143
The role of Bruton’s tyrosine kinase in autoimmunity and implications for therapy
Crofford, L. J., Nyhoff, L. E., Sheehan, J. H., & Kendall, P. L. (2016) · Expert Review of Clinical Immunology · doi:10.1586/1744666x.2016.1152888 · Cited by 142
RN486, a Selective Bruton's Tyrosine Kinase Inhibitor, Abrogates Immune Hypersensitivity Responses and Arthritis in Rodents
Xu, D., Kim, Y. D., Postelnek, J., Vu, M. D., Hu, D., Liao, C., Bradshaw, M., Hsu, J., Zhang, J., Pashine, A., et al. (2012) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.111.187740 · Cited by 142
Self-citation
A public-private partnership to unlock the untargeted kinome
Knapp, S., Arruda, P., Blagg, J., Burley, S. K., Drewry, D. H., Edwards, A. M., Fabbro, D., Gillespie, P., Gray, N. S., Küster, B., et al. (2012) · Nature Chemical Biology · doi:10.1038/nchembio.1113 · Cited by 139
BTK Signaling in B Cell Differentiation and Autoimmunity
Corneth, O. B. J., Wolterink, R. G. J. K., & Hendriks, R. W. (2015) · Current topics in microbiology and immunology · doi:10.1007/82_2015_478 · Cited by 145
Battling Btk mutants with noncovalent inhibitors that overcome Cys481 and Thr474 mutations
Johnson, A. R., Kohli, P. B., Katewa, A., Gogol, E., Belmont, L. D., Choy, R., Penuel, E., Burton, L., Eigenbrot, C., Yu, C., et al. (2016) · ACS Chemical Biology · doi:10.1021/acschembio.6b00480 · Cited by 137
Self-citation
Human NACHT, LRR, and PYD domain–containing protein 3 (NLRP3) inflammasome activity is regulated by and potentially targetable through Bruton tyrosine kinase
Liu, X., Pichulik, T., Wolz, O., Dang, T., Stutz, A., Dillen, C. A., Garcia, M. D., Kraus, H., Dickhöfer, S., Daiber, E., et al. (2017) · Journal of Allergy and Clinical Immunology · doi:10.1016/j.jaci.2017.01.017 · Cited by 137
Applications of organocatalysed visible-light photoredox reactions for medicinal chemistry
Bogdos, M. K., Pinard, E., & Murphy, J. A. (2018) · Beilstein Journal of Organic Chemistry · doi:10.3762/bjoc.14.179 · Cited by 129
Bruton's Tyrosine Kinase: From X-Linked Agammaglobulinemia Toward Targeted Therapy for B-Cell Malignancies
Ponader, S., & Burger, J. A. (2014) · Journal of Clinical Oncology · doi:10.1200/jco.2013.53.1046 · Cited by 126
Autoinhibition of Bruton's tyrosine kinase (Btk) and activation by soluble inositol hexakisphosphate
Wang, Q., Vogan, E. M., Nocka, L. M., Rosen, C. E., Zorn, J. A., Harrison, S. C., & Kuriyan, J. (2015) · eLife · doi:10.7554/elife.06074 · Cited by 127
Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton’s Tyrosine Kinase (BTK)
Watterson, S. H., Liu, Q., Bertrand, M. B., Batt, D. G., Li, L., Pattoli, M. A., Skala, S., Cheng, L., Obermeier, M. T., Moore, R., et al. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b00167 · Cited by 120
Phenazinium Salt-Catalyzed Aerobic Oxidative Amidation of Aromatic Aldehydes
Leow, D. (2014) · Organic Letters · doi:10.1021/ol5029354 · Cited by 119
CGI1746 targets σ1R to modulate ferroptosis through mitochondria-associated membranes
Zhang, Z., Zhou, H., Gu, W., Wei, Y., Mou, S., Wang, Y., Zhang, J., & Zhong, Q. (2024) · Nature Chemical Biology · doi:10.1038/s41589-023-01512-1 · Cited by 126
Self-citation
Selective inhibition of BTK prevents murine lupus and antibody-mediated glomerulonephritis
Rankin, A. L., Seth, N., Keegan, S., Andreyeva, T., Cook, T. A., Edmonds, J., Mathialagan, N., Benson, M. J., Syed, J., Zhan, Y., et al. (2013) · The Journal of Immunology · doi:10.4049/jimmunol.1301553 · Cited by 113
Structure-Based Drug Design of RN486, a Potent and Selective Bruton’s Tyrosine Kinase (BTK) Inhibitor, for the Treatment of Rheumatoid Arthritis
Lou, Y. C., Han, X., Kuglstatter, A., Kondru, R. K., Sweeney, Z. K., Soth, M., McIntosh, J. E., Litman, R., Suh, J. M., Koçer, B., et al. (2014) · Journal of Medicinal Chemistry · doi:10.1021/jm500305p · Cited by 114
A phase I trial of PRN1008, a novel reversible covalent inhibitor of Bruton's tyrosine kinase, in healthy volunteers
Smith, P. F., Krishnarajah, J., Nunn, P. A., Hill, R. J., Karr, D. E., Tam, D., Masjedizadeh, M. R., Funk, J. O., & Gourlay, S. G. (2017) · British Journal of Clinical Pharmacology · doi:10.1111/bcp.13351 · Cited by 108
Enhanced Bruton's Tyrosine Kinase Activity in Peripheral Blood B Lymphocytes From Patients With Autoimmune Disease
Corneth, O. B. J., Verstappen, G. M. P. J., Paulissen, S. M. J., de Bruijn, M. J. W., Rip, J., Lukkes, M. M., van Hamburg, J. P., Lubberts, E., Bootsma, H., Kroese, F. G. M., et al. (2017) · Arthritis & Rheumatology · doi:10.1002/art.40059 · Cited by 112
The NLRP3 inflammasome and bruton's tyrosine kinase in platelets co-regulate platelet activation, aggregation, and in vitro thrombus formation
Murthy, P., Durco, F., Miller-Ocuin, J. L., Takedai, T., Shankar, S., Liang, X., Liu, X., Cui, X. D., Sachdev, U., Rath, D., et al. (2016) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2016.12.161 · Cited by 110
The PD-1/PD-L1 axis contributes to immune metabolic dysfunctions of monocytes in chronic lymphocytic leukemia
Qorraj, M., Bruns, H., Böttcher, M., Weigand, L., Saul, D., Mackensen, A., Jitschin, R., & Mougiakakos, D. (2016) · Leukemia · doi:10.1038/leu.2016.214 · Cited by 108
Bruton’s Tyrosine Kinase (BTK) Inhibitors in Clinical Trials
Burger, J. A. (2013) · Current Hematologic Malignancy Reports · doi:10.1007/s11899-013-0188-8 · Cited by 103
Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases
Xie, Z., Yang, X., Duan, Y., Han, J., & Liao, C. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c01511 · Cited by 102
Bleeding by Bruton Tyrosine Kinase-Inhibitors: Dependency on Drug Type and Disease
von Hundelshausen, P., & Siess, W. (2021) · Cancers · doi:10.3390/cancers13051103 · Cited by 100
Targeting Bruton tyrosine kinase using non-covalent inhibitors in B cell malignancies
Gu, D., Tang, H., Wu, J., Li, J., & Miao, Y. (2021) · Journal of Hematology & Oncology · doi:10.1186/s13045-021-01049-7 · Cited by 100
Biochemical characterization of tirabrutinib and other irreversible inhibitors of Bruton's tyrosine kinase reveals differences in on - and off - target inhibition
Liclican, A. C., Serafini, L., Xing, W., Czerwieniec, G. A., Steiner, B. H., Wang, T., Brendza, K. M., Lutz, J. D., Keegan, K. S., Ray, A. S., et al. (2020) · Biochimica et Biophysica Acta (BBA) - General Subjects · doi:10.1016/j.bbagen.2020.129531 · Cited by 101
Modulating proximal cell signaling by targeting Btk ameliorates humoral autoimmunity and end-organ disease in murine lupus
Hutcheson, J., Vanarsa, K., Bashmakov, A., Grewal, S., Sajitharan, D., Chang, B. Y., Buggy, J. J., Zhou, X. J., Du, Y., Satterthwaite, A. B., et al. (2012) · Arthritis Research & Therapy · doi:10.1186/ar4086 · Cited by 96
Bruton's tyrosine kinase inhibitors for the treatment of rheumatoid arthritis
Whang, J. A., & Chang, B. Y. (2014) · Drug Discovery Today · doi:10.1016/j.drudis.2014.03.028 · Cited by 95
Exploring the target scope of KEAP1 E3 ligase-based PROTACs
Du, G., Jiang, J., Henning, N. J., Safaee, N., Koide, E., Nowak, R. P., Donovan, K. A., Yoon, H., You, I., Yue, H., et al. (2022) · Cell chemical biology · doi:10.1016/j.chembiol.2022.08.003 · Cited by 97
Antiarthritis Effect of a Novel Bruton’s Tyrosine Kinase (BTK) Inhibitor in Rat Collagen-Induced Arthritis and Mechanism-Based Pharmacokinetic/Pharmacodynamic Modeling: Relationships between Inhibition of BTK Phosphorylation and Efficacy
Liu, L., Paolo, J. A. D., Barbosa, J., Rong, H., Reif, K., & Wong, H. (2011) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.111.181545 · Cited by 89
Self-citation
Bruton’s Tyrosine Kinase Inhibitors: Approaches to Potent and Selective Inhibition, Preclinical and Clinical Evaluation for Inflammatory Diseases and B Cell Malignancies
Lou, Y. C., Owens, T. D., Kuglstatter, A., Kondru, R. K., & GOLDSTEIN, D. M. (2012) · Journal of Medicinal Chemistry · doi:10.1021/jm300035p · Cited by 88
Cirmtuzumab inhibits Wnt5a-induced Rac1 activation in chronic lymphocytic leukemia treated with ibrutinib
Yu, J., Chen, L., Cui, B., Wu, C. C. N., Choi, M. Y., Chen, Y., Zhang, L., Rassenti, L. Z., Widhopf, G. F., & Kipps, T. J. (2016) · Leukemia · doi:10.1038/leu.2016.368 · Cited by 88
7-Azaindole: A Versatile Scaffold for Developing Kinase Inhibitors
Irie, T., & Sawa, M. (2017) · Chemical and Pharmaceutical Bulletin · doi:10.1248/cpb.c17-00380 · Cited by 85
Discovery of a Potent BTK Inhibitor with a Novel Binding Mode by Using Parallel Selections with a DNA‐Encoded Chemical Library
Cuozzo, J. W., Gikunju, D., Habeshian, S., Hupp, C. D., Keefe, A. D., Sigel, E. A., Soutter, H. H., Thomson, H. A., Zhang, Y., & Clark, M. (2017) · ChemBioChem · doi:10.1002/cbic.201600573 · Cited by 81
BTK gatekeeper residue variation combined with cysteine 481 substitution causes super-resistance to irreversible inhibitors acalabrutinib, ibrutinib and zanubrutinib
Estupiñán, H. Y., Wang, Q., Berglöf, A., Schaafsma, G. C. P., Shi, Y., Zhou, L., Mohammad, D. K., Yu, L., Vihinen, M., Zain, R., et al. (2021) · Leukemia · doi:10.1038/s41375-021-01123-6 · Cited by 80
Targeting Bruton’s Tyrosine Kinase in Inflammatory and Autoimmune Pathologies
Neys, S. F. H., Hendriks, R. W., & Corneth, O. B. J. (2021) · Frontiers in Cell and Developmental Biology · doi:10.3389/fcell.2021.668131 · Cited by 80
BTK Modulates p53 Activity to Enhance Apoptotic and Senescent Responses
Althubiti, M., Rada, M., Samuel, J., Escorsa, J. M., Najeeb, H., Lee, K.-G., Lam, K., Jones, G. D. D., Barlev, N. A., & Macip, S. (2016) · Cancer Research · doi:10.1158/0008-5472.can-16-0690 · Cited by 76
Discovery of a Potent, Covalent BTK Inhibitor for B-Cell Lymphoma
Wu, H., Wang, W., Liu, F., Weisberg, E., Tian, B., Chen, Y., Li, B., Wang, A., Wang, B., Zhao, Z., et al. (2014) · ACS Chemical Biology · doi:10.1021/cb4008524 · Cited by 77
Review of the development of BTK inhibitors in overcoming the clinical limitations of ibrutinib
Ran, F., Liu, Y., Wang, C., Xu, Z., Zhang, Y., Liu, Y., Zhao, G., & Ling, Y. (2021) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2021.114009 · Cited by 76
Bruton’s Kinase Inhibitors for the Treatment of Immunological Diseases: Current Status and Perspectives
Robak, E., & Robak, T. (2022) · Journal of Clinical Medicine · doi:10.3390/jcm11102807 · Cited by 75
Bruton Tyrosine Kinase Is a Therapeutic Target in Stem-like Cells from Multiple Myeloma
Yang, Y., Shi, J., Gu, Z., Salama, M. E., Das, S., Wendlandt, E. B., Xu, H., Huang, J., Yi, T., Hao, M., et al. (2015) · Cancer Research · doi:10.1158/0008-5472.can-14-2362 · Cited by 76
Fragment-Based Discovery of a Small Molecule Inhibitor of Bruton’s Tyrosine Kinase
Smith, C. R., Dougan, D. R., Komandla, M., Kanouni, T., Knight, B., Lawson, J. D., Sabat, M. P., Taylor, E. R., Vu, P. H., & Wyrick, C. (2015) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5b00734 · Cited by 75
Significant Species Difference in Amide Hydrolysis of GDC-0834, a Novel Potent and Selective Bruton’s Tyrosine Kinase Inhibitor
Liu, L., Halladay, J. S., Shin, Y. G., Wong, S., Coraggio, M., La, H., Baumgardner, M., Le, H. T., Gopaul, S. V., Boggs, J. W., et al. (2011) · Drug Metabolism and Disposition · doi:10.1124/dmd.111.040840 · Cited by 74
Self-citation
Recent Advances in BTK Inhibitors for the Treatment of Inflammatory and Autoimmune Diseases
Zhang, D., He, G., & Meng, F. (2021) · Molecules · doi:10.3390/molecules26164907 · Cited by 74
The Development of BTK Inhibitors: A Five-Year Update
Tasso, B., Spallarossa, A., Russo, E., & Brullo, C. (2021) · Molecules · doi:10.3390/molecules26237411 · Cited by 72
Tec Family Kinases in Inflammation and Disease
Horwood, N. J., Urbaniak, A. M., & Danks, L. (2012) · International Reviews of Immunology · doi:10.3109/08830185.2012.670334 · Cited by 74
Tyrosine Kinase Btk Is Required for NK Cell Activation
Bao, Y., Zheng, J. H., Han, C., Jin, J., Han, H., Liu, Y., Lau, Y., Tu, W., & Cao, X. (2012) · Journal of Biological Chemistry · doi:10.1074/jbc.m112.372425 · Cited by 73
Btk-specific inhibition blocks pathogenic plasma cell signatures and myeloid cell–associated damage in IFNα-driven lupus nephritis
Katewa, A., Wang, Y., Hackney, J. A., Huang, T., Suto, E., Ramamoorthi, N., Austin, C. D., Bremer, M. C. D., Chen, J. Z., Crawford, J. J., et al. (2017) · JCI Insight · doi:10.1172/jci.insight.90111 · Cited by 72
Self-citation
Structural mechanism for Bruton’s tyrosine kinase activation at the cell membrane
Wang, Q., Pechersky, Y., Sagawa, S., Pan, A. C., & Shaw, D. E. (2019) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1819301116 · Cited by 73
Emerging small-molecule inhibitors of the Bruton’s tyrosine kinase (BTK): Current development
Liu, J., Chen, C., Wang, D., Zhang, J., & Zhang, T. (2021) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2021.113329 · Cited by 71
Self-citation
BODIPY catalyzed amide synthesis promoted by BHT and air under visible light
Wang, X., Yu, S.-S., Wang, C., Xue, D. Q., & Xiao, J. (2016) · Organic & Biomolecular Chemistry · doi:10.1039/c6ob00736h · Cited by 71
B-Cell Receptor Signaling Inhibitors for Treatment of Autoimmune Inflammatory Diseases and B-Cell Malignancies
Puri, K. D., Paolo, J. A. D., & Gold, M. R. (2013) · International Reviews of Immunology · doi:10.3109/08830185.2013.818140 · Cited by 69
Analysis of the Effects of the Bruton's tyrosine kinase (Btk) Inhibitor Ibrutinib on Monocyte Fcγ Receptor (FcγR) Function
Ren, L., Campbell, A. R., Fang, H., Gautam, S., Elavazhagan, S., Fatehchand, K., Mehta, P., Stiff, A. R., Reader, B. F., Mo, X. M., et al. (2015) · Journal of Biological Chemistry · doi:10.1074/jbc.m115.687251 · Cited by 69
Potent and selective Bruton’s tyrosine kinase inhibitors: Discovery of GDC-0834
Young, W. B., Barbosa, J., Blomgren, P., Bremer, M. C. D., Crawford, J. J., Dambach, D. M., Gallion, S., Hymowitz, S. G., Kropf, J. E., Lee, S., et al. (2015) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2015.01.032 · Cited by 68
Self-citation
HM71224, a novel Bruton’s tyrosine kinase inhibitor, suppresses B cell and monocyte activation and ameliorates arthritis in a mouse model: a potential drug for rheumatoid arthritis
Park, J. K., Byun, J., Park, J. A., Kim, Y.-Y., Lee, Y. J., Oh, J. I., Jang, S. Y., Kim, Y., Song, Y. W., Son, J., et al. (2016) · Arthritis Research & Therapy · doi:10.1186/s13075-016-0988-z · Cited by 68
Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations
Lu, X., Smaill, J. B., & Ding, K. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c00507 · Cited by 67
Targeting the SYK–BTK axis for the treatment of immunological and hematological disorders
Tan, S., Liao, C., Lucas, M. C., Stevenson, C. S., & DeMartino, J. A. (2013) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2013.02.001 · Cited by 65
Discovery of a Series of 2,5-Diaminopyrimidine Covalent Irreversible Inhibitors of Bruton’s Tyrosine Kinase with in Vivo Antitumor Activity
Li, X., Zuo, Y., Tang, G., Wang, Y., Zhou, Y., Wang, X., Guo, T., Xia, M., Ding, N., & Pan, Z. (2014) · Journal of Medicinal Chemistry · doi:10.1021/jm4017762 · Cited by 65
Cinnoline Scaffold—A Molecular Heart of Medicinal Chemistry?
Szumilak, M., & Stańczak, A. (2019) · Molecules · doi:10.3390/molecules24122271 · Cited by 63
Bruton’s tyrosine kinase inhibitor suppresses imiquimod-induced psoriasis-like inflammation in mice through regulation of IL-23/IL-17A in innate immune cells
Nadeem, A., Ahmad, S. F., Al-Harbi, N. O., El‐Sherbeeny, A. M., Alasmari, A. F., Alanazi, W. A., Alasmari, F. F., Ibrahim, K. E., Al‐Harbi, M. M., Bakheet, S. A., et al. (2020) · International Immunopharmacology · doi:10.1016/j.intimp.2020.106215 · Cited by 63
Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis
Kim, K., Maderna, A., Schnute, M. E., Hegen, M., Mohan, S., Miyashiro, J. S., Lin, L., Li, E., Keegan, S., Lussier, J., et al. (2011) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2011.09.008 · Cited by 63
Targeting B cells in treatment of autoimmunity
Franks, S. E., Getahun, A., Hogarth, P. M., & Cambier, J. C. (2016) · Current Opinion in Immunology · doi:10.1016/j.coi.2016.09.003 · Cited by 61
Role of Bruton's tyrosine kinase in myeloma cell migration and induction of bone disease
Bam, R., Ling, W., Khan, S., Pennisi, A., Venkateshaiah, S. U., Li, X., van Rhee, F., Usmani, S. Z., Barlogie, B., Shaughnessy, J. D., et al. (2013) · American Journal of Hematology · doi:10.1002/ajh.23433 · Cited by 61
Ibrutinib in previously treated chronic lymphocytic leukemia patients with autoimmune cytopenias in the RESONATE study
Montillo, M., O'Brien, S. M., Tedeschi, A., Byrd, J. C., Dearden, C. E., Gill, D. S., Brown, J. R., Barrientos, J. C., Mulligan, S. P., Furman, R. R., et al. (2017) · Blood Cancer Journal · doi:10.1038/bcj.2017.5 · Cited by 61
Therapeutic treatment with Ibrutinib attenuates imiquimod-induced psoriasis-like inflammation in mice through downregulation of oxidative and inflammatory mediators in neutrophils and dendritic cells
Al-Harbi, N. O., Nadeem, A., Ahmad, S. F., Bakheet, S. A., El‐Sherbeeny, A. M., Ibrahim, K. E., Alzahrani, K. S., Al‐Harbi, M. M., Mahmood, H. M., Alqahtani, F., et al. (2020) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2020.173088 · Cited by 60
Wnt5a induces ROR1 to complex with HS1 to enhance migration of chronic lymphocytic leukemia cells
Hasan, M. K., Yu, J., Chen, L., Cui, B., Widhopf, G. F., Rassenti, L. Z., Shen, Z., Briggs, S. P., & Kipps, T. J. (2017) · Leukemia · doi:10.1038/leu.2017.133 · Cited by 60
Bruton's tyrosine kinase inhibitor BMS-986142 in experimental models of rheumatoid arthritis enhances efficacy of agents representing clinical standard-of-care
Gillooly, K. M., Pulicicchio, C. M., Pattoli, M. A., Cheng, L., Skala, S., Heimrich, E., McIntyre, K. W., Taylor, T. L., Kukral, D. W., Dudhgaonkar, S. P., et al. (2017) · PLoS ONE · doi:10.1371/journal.pone.0181782 · Cited by 59
Inhibition of Bruton´s tyrosine kinase as a novel therapeutic approach in multiple sclerosis
Torke, S., & Weber, M. S. (2020) · Expert Opinion on Investigational Drugs · doi:10.1080/13543784.2020.1807934 · Cited by 58
A Fast and Clean BTK Inhibitor
Gabizon, R., & London, N. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c00597 · Cited by 56
Bruton’s Tyrosine Kinase Inhibition as an Emerging Therapy in Systemic Autoimmune Disease
Neys, S. F. H., Rip, J., Hendriks, R. W., & Corneth, O. B. J. (2021) · Drugs · doi:10.1007/s40265-021-01592-0 · Cited by 58
Bruton's Tyrosine Kinase Inhibitors Prevent Therapeutic Escape in Breast Cancer Cells
Wang, X., Wong, J., Sevinsky, C. J., Kokabee, L., Khan, F., Sun, Y., & Conklin, D. S. (2016) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-15-0813 · Cited by 56
Emerging nanotherapeutics alleviating rheumatoid arthritis by readjusting the seeds and soils
Zhang, W., Chen, Y., Liu, Q., Zhou, M. L., Wang, K., Wang, Y., Nie, J., Gui, S., Peng, D., He, Z., et al. (2022) · Journal of Controlled Release · doi:10.1016/j.jconrel.2022.04.001 · Cited by 54
New Btk inhibitor holds promise
Hendriks, R. W. (2010) · Nature Chemical Biology · doi:10.1038/nchembio.502 · Cited by 54
Enhanced Expression of Bruton’s Tyrosine Kinase in B Cells Drives Systemic Autoimmunity by Disrupting T Cell Homeostasis
Corneth, O. B. J., de Bruijn, M. J. W., Rip, J., Asmawidjaja, P. S., Kil, L. P., & Hendriks, R. W. (2016) · The Journal of Immunology · doi:10.4049/jimmunol.1600208 · Cited by 53
Toll-like receptor 4–, 7–, and 8–activated myeloid cells from patients with X-linked agammaglobulinemia produce enhanced inflammatory cytokines
Marron, T. U., Martínez‐Gallo, M., Yu, J. E., & Cunningham‐Rundles, C. (2011) · Journal of Allergy and Clinical Immunology · doi:10.1016/j.jaci.2011.10.009 · Cited by 52

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