Covalent Proximity Inducers
N London - Chemical Reviews, 2024 - ACS Publications
Molecules that are able to induce proximity between two proteins are finding ever increasing
applications in chemical biology and drug discovery. The ability to introduce an electrophile …
applications in chemical biology and drug discovery. The ability to introduce an electrophile …
PROTACting the kinome with covalent warheads
The dawn of targeted degradation using proteolysis-targeting chimeras (PROTACs) against
recalcitrant proteins has prompted numerous efforts to develop complementary drugs …
recalcitrant proteins has prompted numerous efforts to develop complementary drugs …
Development of a Novel Amplifiable System to Quantify Hydrogen Peroxide in Living Cells
Although many redox signaling molecules are present at low concentrations, typically
ranging from micromolar to submicromolar levels, they often play essential roles in a wide …
ranging from micromolar to submicromolar levels, they often play essential roles in a wide …
Development of a RIPK1 degrader to enhance antitumor immunity
The scaffolding function of receptor interacting protein kinase 1 (RIPK1) confers intrinsic and
extrinsic resistance to immune checkpoint blockades (ICBs) and emerges as a promising …
extrinsic resistance to immune checkpoint blockades (ICBs) and emerges as a promising …
Comprehensive detection of CRLF2 alterations in acute lymphoblastic leukemia: a rapid and accurate novel approach
JV Gil, A Miralles, S de Las Heras, E Such… - Frontiers in Molecular …, 2024 - frontiersin.org
Introduction: Acute lymphoblastic leukemia (ALL) is a prevalent childhood cancer with high
cure rate, but poses a significant medical challenge in adults and relapsed patients …
cure rate, but poses a significant medical challenge in adults and relapsed patients …
Bruton Tyrosine Kinase Degraders in B-Cell Malignancies
T Huynh, S Rodriguez-Rodriguez, AV Danilov - Molecular Cancer …, 2024 - AACR
Bruton tyrosine kinase (BTK) belongs to the TEC family of nonreceptor kinases and is
expressed in various hematopoietic cells, including B cells, myeloid cells, and platelets (1) …
expressed in various hematopoietic cells, including B cells, myeloid cells, and platelets (1) …
A Kinetic Scout Approach Accelerates Targeted Protein Degrader Development
AT Fan, GE Gadbois, HT Huang… - Angewandte …, 2024 - Wiley Online Library
Bifunctional molecules such as targeted protein degraders induce proximity to promote gain‐
of‐function pharmacology. These powerful approaches have gained broad traction across …
of‐function pharmacology. These powerful approaches have gained broad traction across …
Quantitative measurement of PROTAC intracellular accumulation
Abstract In recent years, Proteolysis Targeting Chimera (PROTAC) technology has emerged
as one of the most promising approaches to remove disease-associated proteins by utilizing …
as one of the most promising approaches to remove disease-associated proteins by utilizing …
[HTML][HTML] The role of noncovalent BTK inhibitors in the era of covalent BTK inhibitors.
Despite significantly improving outcomes in patients with B-cell malignancies, covalent
Bruton tyrosine kinase (BTK) inhibitors are limited by toxicities and the development of …
Bruton tyrosine kinase (BTK) inhibitors are limited by toxicities and the development of …
[PDF][PDF] Investigating Resistance Mechanisms to Non-Covalent Bruton's Tyrosine Kinase Inhibitors and Using Degraders to Overcome Resistance for Patients with B …
S Montoya - 2024 - scholarship.miami.edu
Chronic lymphocytic leukemia (CLL) is a clinically heterogeneous disease that originates
from dysfunctional B lymphocytes. Abnormal B cell receptor (BCR) signaling has been …
from dysfunctional B lymphocytes. Abnormal B cell receptor (BCR) signaling has been …