Results 161 to 170 of about 7,774 (200)

KRAS Mutations in Cancers: From Undruggable Dilemma to Precision Medicine

MedComm, Volume 7, Issue 10, October 2026.
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, Yimin Wu, Xing Jia, Li Yang, Wenjun Yang, Weishan Lu, Zhiye Huang, Yang Pan, Zixuan Fei, Junnan Ru, Jiazheng Zhao, Jue Shen, Taobo Luo, Da Chen, Haihong Yu, Haihan Deng, Jian Zeng, Wenmei Jiang, Leilei Wu   +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]

J Med Chem
Deng Z, Catlett J, Lee Y, Wu Q, Xu Z, Xie L, Chen X, Xiong Y, Kaniskan HÜ, Jin J.   +9 more
europepmc   +1 more source

Ineffectiveness of immune checkpoint inhibitors in prostate cancer: is it just a question of ‘‐mabs’?

The Journal of Pathology, Volume 270, Issue 2, Page 139-162, October 2026.
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, Irene Torresan, Emilio Francesco Giunta, Sara Bleve, Nicole Brighi, Elisa Tassinari, Sofia Zanuccoli, Maria Concetta Cursano, Cristian Lolli   +8 more
wiley   +1 more source

Discovery of the First Potent DYRK2 Proteolysis Targeting Chimera Degraders. [PDF]

ACS Med Chem Lett
Chen J, Zhu W, Zhang W, Tong Y, Xu F, Pang J.   +5 more
europepmc   +1 more source

RheoScale 2.0: Revealing the hidden roles of protein positions via substitution patterns

Protein Science, Volume 35, Issue 10, October 2026.
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, Shwetha Sreenivasan, Carter J. Gray, Hannah C. Cleveland, Liskin Swint‐Kruse   +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]

RSC Med Chem
Weldert AC, Frey AF, Krone MW, Krähe F, Kuhn H, Kersten C, Barthels F.   +6 more
europepmc   +1 more source

Structural Insights Into the Function of Leishmania major Adenylosuccinate Lyase

Proteins: Structure, Function, and Bioinformatics, Volume 94, Issue 10, Page 1686-1701, October 2026.
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, Monique Mantovani, Maria E. S. D. Lino, Aline O. Albuquerque, João H. M. da Silva, Ronaldo A. P. Nagem, Adriana L. Rojas, Geraldo R. Sartori, Eduardo Horjales, David Campbell, Otavio H. Thiemann   +10 more
wiley   +1 more source

Chemoproteomics-Enabled <i>De Novo</i> Proteolysis Targeting Chimera Discovery Platform Identifies a Metallothionein Degrader to Probe Its Role in Cancer. [PDF]

J Am Chem Soc
Racioppo B, Pechalrieu D, Abegg D, Dwyer B, Ramseier NT, Hu YS, Adibekian A.   +6 more
europepmc   +1 more source

Thiazolidine‐2,4‐dione and Thiazole Derivatives as Privileged Structures for Dengue Virus: A Review of Medicinal Chemistry Aspects

ChemistrySelect, Volume 11, Issue 37, 6 October 2026.
This graphical abstract summarizes thiazole, thiazolidine‐2,4‐dione, and hybrid compounds investigated as antiviral candidates against dengue virus. Representative structures and reported potencies are presented in the context of DENV serotypes. Proposed molecular targets include NS2B–NS3 protease and NS5.
Pedro César de Souza, Thaynara Paula Warren Bezerra, Matheus Vinicius Guimarães de Melo, Thayná da Silva Barros, Matheus Italo da Conceição, Michelle Melgarejo da Rosa, Moacyr Jesus Barreto de Melo Rêgo   +6 more
wiley   +1 more source

Leveraging Dual-Ligase Recruitment to Enhance Protein Degradation via a Heterotrivalent Proteolysis Targeting Chimera. [PDF]

J Am Chem Soc
Bond AG, Muñoz I Ordoño M, Bisbach CM, Craigon C, Makukhin N, Caine EA, Nagala M, Urh M, Winter GE, Riching KM, Ciulli A.   +10 more
europepmc   +1 more source