Discovery of novel BTK PROTACs for B-Cell lymphomas

Targeting Bruton tyrosine kinase using non-covalent inhibitors in B cell malignancies

(2021) Danling Gu et al.   Journal of Hematology & Oncology

BTK gatekeeper residue variation combined with cysteine 481 substitution causes super-resistance to irreversible inhibitors acalabrutinib, ibrutinib and zanubrutinib

(2021) H. Yesid Estupiñán et al.   LEUKEMIA

Efficient Targeted Degradation via Reversible and Irreversible Covalent PROTACs

(2020) Ronen Gabizon et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Unifying principles of bifunctional, proximity-inducing small molecules

(2020) Christopher J. Gerry et al.   Nature Chemical Biology

Ibrutinib Resistance Mechanisms and Treatment Strategies for B-Cell Lymphomas

(2020) Bhawana George et al.   Cancers

Understanding and Improving the Membrane Permeability of VH032-Based PROTACs

(2020) Victoria G. Klein et al.   ACS Medicinal Chemistry Letters

Enhancing intracellular accumulation and target engagement of PROTACs with reversible covalent chemistry

(2020) Wen-Hao Guo et al.   Nature Communications

Degradation of Bruton’s tyrosine kinase mutants by PROTACs for potential treatment of ibrutinib-resistant non-Hodgkin lymphomas

(2019) Yonghui Sun et al.   LEUKEMIA

PROTAC-Mediated Degradation of Bruton’s Tyrosine Kinase Is Inhibited by Covalent Binding

(2019) Christopher P. Tinworth et al.   ACS Chemical Biology

Proteolysis targeting chimeras (PROTACs) in ‘beyond rule-of-five’ chemical space: Recent progress and future challenges

(2019) Scott D. Edmondson et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase

(2019) Yunhang Guo et al.   JOURNAL OF MEDICINAL CHEMISTRY

Development of targeted protein degradation therapeutics

(2019) Philip P. Chamberlain et al.   Nature Chemical Biology

Design, synthesis and biological evaluation of Proteolysis Targeting Chimeras (PROTACs) as a BTK degraders with improved pharmacokinetic properties

(2019) Saul Jaime-Figueroa et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Targeting the C481S Ibrutinib-Resistance Mutation in Bruton’s Tyrosine Kinase Using PROTAC-Mediated Degradation

(2018) Alexandru D. Buhimschi et al.   BIOCHEMISTRY

Role of Bruton’s tyrosine kinase in B cells and malignancies

(2018) Simar Pal Singh et al.   Molecular Cancer

Delineating the role of cooperativity in the design of potent PROTACs for BTK

(2018) Adelajda Zorba et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The BTK Inhibitor ARQ 531 Targets Ibrutinib-Resistant CLL and Richter Transformation

(2018) Sean D. Reiff et al.   Cancer Discovery

Targeting Bruton’s Tyrosine Kinase Across B-Cell Malignancies

(2018) Caspar da Cunha-Bang et al.   DRUGS

The 2016 revision of the World Health Organization classification of lymphoid neoplasms

(2016) S. H. Swerdlow et al.   BLOOD

Induced protein degradation: an emerging drug discovery paradigm

(2016) Ashton C. Lai et al.   NATURE REVIEWS DRUG DISCOVERY

Targeting B cell receptor signaling with ibrutinib in diffuse large B cell lymphoma

(2015) Wyndham H Wilson et al.   NATURE MEDICINE

Resistance Mechanisms for the Bruton's Tyrosine Kinase Inhibitor Ibrutinib

(2014) Jennifer A. Woyach et al.   NEW ENGLAND JOURNAL OF MEDICINE

The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy

(2010) L. A. Honigberg et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA