Kinase inhibitors: the road ahead

FM Ferguson, NS Gray - Nature reviews Drug discovery, 2018 - nature.com
Receptor tyrosine kinase signalling pathways have been successfully targeted to inhibit
proliferation and angiogenesis for cancer therapy. However, kinase deregulation has been …

Mechanism-based criteria to improve therapeutic outcomes in progressive multiple sclerosis

HYF Yong, VW Yong - Nature Reviews Neurology, 2022 - nature.com
In contrast to the multiple disease-modifying therapies that are available for relapsing–
remitting multiple sclerosis (MS), the therapeutic options for progressive MS (PMS) are …

Rilzabrutinib, an oral BTK inhibitor, in immune thrombocytopenia

DJ Kuter, M Efraim, J Mayer, M Trněný… - … England Journal of …, 2022 - Mass Medical Soc
Background Rilzabrutinib, an oral, reversible covalent inhibitor of Bruton's tyrosine kinase,
may increase platelet counts in patients with immune thrombocytopenia by means of dual …

Pemphigus: current and future therapeutic strategies

D Didona, R Maglie, R Eming, M Hertl - Frontiers in immunology, 2019 - frontiersin.org
Pemphigus encompasses a heterogeneous group of autoimmune blistering diseases, which
affect both mucous membranes and the skin. The disease usually runs a chronic-relapsing …

The role of Bruton's tyrosine kinase in the immune system and disease

C McDonald, C Xanthopoulos, E Kostareli - Immunology, 2021 - Wiley Online Library
Bruton's tyrosine kinase (BTK) is a TEC kinase with a multifaceted role in B‐cell biology and
function, highlighted by its position as a critical component of the B‐cell receptor signalling …

Bruton tyrosine kinase degradation as a therapeutic strategy for cancer

D Dobrovolsky, ES Wang, S Morrow… - Blood, The Journal …, 2019 - ashpublications.org
The covalent Bruton tyrosine kinase (BTK) inhibitor ibrutinib is highly efficacious against
multiple B-cell malignancies. However, it is not selective for BTK, and multiple mechanisms …

[HTML][HTML] Preclinical efficacy and anti-inflammatory mechanisms of action of the Bruton tyrosine kinase inhibitor rilzabrutinib for immune-mediated disease

CL Langrish, JM Bradshaw, MR Francesco… - The Journal of …, 2021 - journals.aai.org
Bruton tyrosine kinase (BTK) is expressed in B cells and innate immune cells, acting as an
essential signaling element in multiple immune cell pathways. Selective BTK inhibition has …

The role of B cells and antibodies in multiple sclerosis, neuromyelitis optica, and related disorders

S Häusser-Kinzel, MS Weber - Frontiers in immunology, 2019 - frontiersin.org
Our pathophysiological concept of the most common central nervous system demyelinating
disease, multiple sclerosis, strikingly evolved by recent discoveries suggesting that B …

Bruton's tyrosine kinase inhibition—An emerging therapeutic strategy in immune‐mediated dermatological conditions

P Mendes‐Bastos, A Brasileiro, P Kolkhir… - Allergy, 2022 - Wiley Online Library
Bruton's tyrosine kinase (BTK), a member of the Tec kinase family, is critically involved in a
range of immunological pathways. The clinical application of BTK inhibitors for B‐cell …

Discovery of reversible covalent Bruton's tyrosine kinase inhibitors PRN473 and PRN1008 (rilzabrutinib)

TD Owens, KA Brameld, EJ Verner, T Ton… - Journal of medicinal …, 2022 - ACS Publications
Bruton's tyrosine kinase (BTK), a Tec family tyrosine kinase, is critical in immune pathways
as an essential intracellular signaling element, participating in both adaptive and immune …