Cargando…

Controlling Ibrutinib’s Conformations about Its Heterobiaryl Axis to Increase BTK Selectivity

[Image: see text] Ibrutinib is a covalent BTK inhibitor that is approved for several indications in oncology. Ibrutinib possesses significant off-target activities toward many kinases, often leading to adverse events in patients. While there have been robust medicinal chemistry efforts leading to mo...

Descripción completa

Detalles Bibliográficos
Autores principales:	Toenjes, Sean T., Heydari, Bahar S., Albright, Samuel T., Hazin, Ramsey, Ortiz, Maria A., Piedrafita, F. Javier, Gustafson, Jeffrey L.
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	American Chemical Society 2023
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10009787/ https://www.ncbi.nlm.nih.gov/pubmed/36923918 http://dx.doi.org/10.1021/acsmedchemlett.2c00523

Ejemplares similares

Ibrutinib and novel BTK inhibitors in clinical development
por: Akinleye, Akintunde, et al.
Publicado: (2013)

Ibrutinib Inhibits Angiogenesis and Tumorigenesis in a BTK-Independent Manner
por: Liu, Jia, et al.
Publicado: (2022)

Pirtobrutinib targets BTK C481S in ibrutinib-resistant CLL but second-site BTK mutations lead to resistance
por: Naeem, Aishath, et al.
Publicado: (2022)

Ibrutinib directly reduces CD8+T cell exhaustion independent of BTK
por: Li, Ling, et al.
Publicado: (2023)

Inhibition of Btk by Btk-specific concentrations of ibrutinib and acalabrutinib delays but does not block platelet aggregation mediated by glycoprotein VI
por: Nicolson, Phillip L.R., et al.
Publicado: (2018)

Organocatalytic cycloaddition–elimination cascade for atroposelective construction of heterobiaryls
por: Xu, Wen-Lei, et al.
Publicado: (2021)

Identification of a structurally novel BTK mutation that drives ibrutinib resistance in CLL
por: Sharma, Shruti, et al.
Publicado: (2016)

The BTK/PI3K/BRD4 axis inhibitor SRX3262 overcomes Ibrutinib resistance in mantle cell lymphoma
por: Pal, Dhananjaya, et al.
Publicado: (2021)

Atroposelective Ir-Catalyzed C–H Borylation of Phthalazine Heterobiaryls
por: Stehrer, Paul, et al.
Publicado: (2023)

A Tec kinase BTK inhibitor ibrutinib promotes maturation and activation of dendritic cells
por: Natarajan, Gayathri, et al.
Publicado: (2016)

Bruton’s Tyrosine Kinase (BTK) Inhibitor (Ibrutinib)-Suppressed Migration and Invasion of Prostate Cancer
por: Zhu, Zhen, et al.
Publicado: (2020)

BTK and PLCG2 remain unmutated in one-third of patients with CLL relapsing on ibrutinib
por: Bonfiglio, Silvia, et al.
Publicado: (2023)

Differential impact of BTK active site inhibitors on the conformational state of full-length BTK
por: Joseph, Raji E, et al.
Publicado: (2020)

Advances in Atroposelectively De Novo Synthesis of Axially Chiral Heterobiaryl Scaffolds
por: Zhang, Xiaoke, et al.
Publicado: (2022)

Pd-Catalyzed Dynamic Kinetic Asymmetric Cross-Coupling of Heterobiaryl Bromides with N-Tosylhydrazones
por: Kattela, Shivashankar, et al.
Publicado: (2022)

Bruton's tyrosine kinase (Btk) inhibitor ibrutinib suppresses stem-like traits in ovarian cancer
por: Zucha, Muhammad Ary, et al.
Publicado: (2015)

Inhibition of BTK and ITK with Ibrutinib Is Effective in the Prevention of Chronic Graft-versus-Host Disease in Mice
por: Schutt, Steven D., et al.
Publicado: (2015)

Effect of the BTK inhibitor ibrutinib on macrophage- and γδ T cell-mediated response against Mycobacterium tuberculosis
por: Colado, Ana, et al.
Publicado: (2018)

The BTK inhibitor ibrutinib may protect against pulmonary injury in COVID-19–infected patients
por: Treon, Steven P., et al.
Publicado: (2020)

Clinical Trials of the BTK Inhibitors Ibrutinib and Acalabrutinib in Human Diseases Beyond B Cell Malignancies
por: Zhu, Sining, et al.
Publicado: (2021)

Ibrutinib facilitates the sensitivity of colorectal cancer cells to ferroptosis through BTK/NRF2 pathway
por: Zhu, Jin-Feng, et al.
Publicado: (2023)

Nucleophilic C4-selective (hetero) arylation of pyridines for facile synthesis of heterobiaryls
por: Kim, Kewon, et al.
Publicado: (2023)

Heightened BTK-dependent cell proliferation in unmutated chronic lymphocytic leukemia confers increased sensitivity to ibrutinib
por: Guo, Ailin, et al.
Publicado: (2015)

Btk inhibitor ibrutinib reduces inflammatory myeloid cell responses in the lung during murine pneumococcal pneumonia
por: de Porto, Alexander P., et al.
Publicado: (2019)

Effect and Mechanism of the Bruton Tyrosine Kinase (Btk) Inhibitor Ibrutinib on Rat Model of Diabetic Foot Ulcers
por: Yang, Xuedong, et al.
Publicado: (2019)

Ibrutinib Prevents Acute Lung Injury via Multi-Targeting BTK, FLT3 and EGFR in Mice
por: Rao, Huanan, et al.
Publicado: (2022)

High surface IgM levels associate with shorter response to ibrutinib and BTK bypass in patients with CLL
por: Chiodin, Giorgia, et al.
Publicado: (2022)

Multifaceted Immunomodulatory Effects of the BTK Inhibitors Ibrutinib and Acalabrutinib on Different Immune Cell Subsets – Beyond B Lymphocytes
por: Zhu, Sining, et al.
Publicado: (2021)

Cationic gold(I) axially chiral biaryl bisphosphine complex-catalyzed atropselective synthesis of heterobiaryls
por: Shibuya, Tetsuro, et al.
Publicado: (2011)

Nitrilium ion trapping as a strategy to access structurally diverse heterobiaryl-containing peptide macrocycles
por: Diamandas, Matthew, et al.
Publicado: (2023)

Preclinical investigation of ibrutinib, a Bruton's kinase tyrosine (Btk) inhibitor, in suppressing glioma tumorigenesis and stem cell phenotypes
por: Wei, Li, et al.
Publicado: (2016)

PB1874: BTK GENE MUTATIONS IN RUSSIAN PATIENTS TREATED WITH IBRUTINIB: AS-PCR VERSUS NGS FOR ALLELIC LOAD ASSESSMENT
por: Likold, E., et al.
Publicado: (2022)

Dynamic Kinetic Resolution of Indole-Based Sulfenylated Heterobiaryls by Rhodium-Catalyzed Atroposelective Reductive Aldol Reaction
por: Rodríguez-Franco, Carlos, et al.
Publicado: (2023)

Substitution scanning identifies a novel, catalytically active ibrutinib-resistant BTK cysteine 481 to threonine (C481T) variant
por: Hamasy, A, et al.
Publicado: (2017)

BTK gatekeeper residue variation combined with cysteine 481 substitution causes super-resistance to irreversible inhibitors acalabrutinib, ibrutinib and zanubrutinib
por: Estupiñán, H. Yesid, et al.
Publicado: (2021)

Proteolysis Targeting Chimeras for BTK Efficiently Inhibit B-Cell Receptor Signaling and Can Overcome Ibrutinib Resistance in CLL Cells
por: Shorer Arbel, Yamit, et al.
Publicado: (2021)

Catalytic atroposelective synthesis of heterobiaryls with vicinal C−C and N−N diaxes via dynamic kinetic resolution
por: Han, Tian-Jiao, et al.
Publicado: (2023)

Ibrutinib synergizes with poly(ADP-ribose) glycohydrolase inhibitors to induce cell death in AML cells via a BTK-independent mechanism
por: Rotin, Lianne E., et al.
Publicado: (2015)

Synthesis and Structure-Activity Relationship Analysis of 5-HT(7) Receptor Antagonists: Piperazin-1-yl Substituted Unfused Heterobiaryls
por: Strekowski, Lucjan, et al.
Publicado: (2016)

Ibrutinib Inhibits BTK Signaling in Tumor-Infiltrated B Cells and Amplifies Antitumor Immunity by PD-1 Checkpoint Blockade for Metastatic Prostate Cancer
por: Deng, Gengguo, et al.
Publicado: (2023)

Cannot write session to /tmp/vufind_sessions/sess_r3k3f5ec9seqbbo31nc9upasc1