Preclinical Evaluation of Bavdegalutamide (ARV-110), a Novel PROteolysis TArgeting Chimera Androgen Receptor Degrader. [PDF]
Snyder LB +13 more
europepmc +1 more source
The Hippo–YAP/TAZ–TEAD pathway integrates mechanical and biochemical cues to govern organ growth, regeneration, cancer, and fibrosis. This review dissects pathway physiology, TEAD structural pharmacology and ligandable pockets, and therapeutic strategies spanning palmitoylation‐pocket inhibitors, PROTAC degraders, and gene/RNA therapies, highlighting ...
Xiaodan Qu, Zhan‐you Wang
wiley +1 more source
Preparation and Characterization of Ternary Complexes to Improve the Solubility and Dissolution Performance of a Proteolysis-Targeting Chimera Drug. [PDF]
Zhang H +8 more
europepmc +1 more source
Colorectal cancer is a heterogeneous, adaptive disease shaped by population‐level risk, genomic and epigenetic alterations, tumor ecosystem evolution, and treatment pressure. This review integrates epidemiology, risk factors, signaling networks, clinical presentation, screening, molecular diagnosis, and stage‐ and biomarker‐guided management while ...
Kairui Wan +6 more
wiley +1 more source
KRAS Mutations in Cancers: From Undruggable Dilemma to Precision Medicine
KRAS‐mutant cancers are therapeutically shaped by both allele identity and tumor context. Direct KRAS inhibition has achieved the greatest clinical success in KRAS G12C‐mutant NSCLC, whereas colorectal cancer often requires EGFR cotargeting and pancreatic cancer remains constrained by stromal and metabolic barriers. Shared resistance mechanisms include
Jiaying Cai +18 more
wiley +1 more source
Harnessing the SPOP E3 Ubiquitin Ligase via a Bridged Proteolysis Targeting Chimera (PROTAC) Strategy for Targeted Protein Degradation. [PDF]
Deng Z +9 more
europepmc +1 more source
Abstract Prostate cancer (PCa) is the second most common type of neoplasm, currently treated with a variety of therapeutic agents. Although advances in treatment over the past decade have improved overall survival, patients with advanced PCa eventually progress from hormone‐sensitive PCa to metastatic castration‐resistant PCa.
Giuseppe Schepisi +8 more
wiley +1 more source
RheoScale 2.0: Revealing the hidden roles of protein positions via substitution patterns
Abstract A central challenge in molecular biology is understanding how amino acid substitutions modulate various features of protein function and stability. To illuminate the complexities of this relationship, high‐throughput (HTP) assays are increasingly used to assess site‐saturating mutagenesis libraries.
David H. Liu +4 more
wiley +1 more source
Structure-guided design of a methyltransferase-like 3 (METTL3) proteolysis targeting chimera (PROTAC) incorporating an indole-nicotinamide chemotype. [PDF]
Weldert AC +6 more
europepmc +1 more source
Structural Insights Into the Function of Leishmania major Adenylosuccinate Lyase
ABSTRACT One of several intriguing aspects of kinetoplastid biochemistry is the complete dependence on host purines and purine recycling due to the lack of a de novo purine biosynthesis pathway. Adenylosuccinate lyase (ASL, EC 4.3.2.2) is a key enzyme in the purine synthesis pathway responsible for the conversion of adenylosuccinate into adenosine ...
Ivan R. e Silva +10 more
wiley +1 more source

