Results 161 to 170 of about 11,341 (256)

Targeting Tumor Stroma: Current Challenges and Future Directions

MedComm, Volume 7, Issue 5, May 2026.
Figure 1. Mechanism of ECM reprogramming. Cancer‐associated fibroblasts (CAFs), cancer‐associated macrophages (CAMs), and other mesenchymal cells alter the ECM composition and increase its stiffness by depositing matrix components such as collagen and hyaluronic acid, and secreting cross‐linking agents like lysyl oxidase homolog 2 (LOXL2).
Siwei Wang, Haofan Hu, Weifeng Zeng, Lu Qin, Xiaoping Chen, Zhibin Liao, Furong Liu, Zhanguo Zhang   +7 more
wiley   +1 more source

Property-based optimisation of PROTACs

RSC Medicinal Chemistry
PROTACs are an emerging therapeutic approach towards targeted protein degradation. This article examines the leading examples of this modality that are in clinical development through the prism of their physicochemical properties.
James S. Scott, Iacovos N. Michaelides, Markus Schade   +2 more
openaire   +3 more sources

Fusion Molecules Between the STAT5b Inhibitor Stafib‐2‐CR and a Cereblon Ligand

ChemistryOpen, Volume 15, Issue 5, May 2026.
The design and synthesis of fusion molecules between the selective STAT5b inhibitor Stafib‐2‐CR and a ligand of the E3 ubiquitin ligase cereblon is reported. Activity analysis in fluorescence polarization assays and isothermal titration calorimetry indicated that the chosen attachment point for the linker is well‐suited to retain activity of the fusion
Theresa Münzel, Karl Christian Seidenstücker, Christoph Protzel, Angela Berg, Thorsten Berg   +4 more
wiley   +1 more source

Structural and functional insights into TBC1D17 highlight the importance of the previously uncharacterized Rab‐binding domain

Protein Science, Volume 35, Issue 5, May 2026.
Abstract TBC (Tre2/Bub2/Cdc16) domain‐containing proteins constitute the widespread family of GTPase‐activating proteins (GAPs). They interact with the Rab superfamily of small GTPases, stimulate GTP hydrolysis, and regulate vesicle trafficking. TBC1D17, involved in Shiga toxin trafficking, autophagy and glucose metabolism regulation, constitutes an ...
Dominika Nielipińska, Marta Orlikowska, Maciej Nielipiński, Bartosz Sekuła, Katarzyna M. Błażewska, Edyta Gendaszewska‐Darmach, Agnieszka J. Pietrzyk‐Brzezińska   +6 more
wiley   +1 more source

Clearance of Senescent Cells by BCL_XL-PROTAC: A Novel Approach to Treat COPD? [PDF]

Aging Cell
Devulder JV, Fenwick PS, Kolosionek E, Al-Sahaf M, Viola P, Lemaire R, Razdan N, Kudo H, Sinadinos A, Odqvist L, Donnelly LE, Barnes PJ.   +11 more
europepmc   +1 more source

PROTACs in cancer therapy: targeted degradation of GPX4, PARP and epigenetic regulators. [PDF]

J Enzyme Inhib Med Chem
Periyasamy S, Jarrett T, Truong J, Skouta R.   +3 more
europepmc   +1 more source

Bumped pomalidomide-based PROTACs

Communications Chemistry
Pomalidomide is an E3 ligase recruiter exploited by PROTACs to degrade target proteins, but its application is hampered by the off-target degradation of other vital endogenous zinc finger (ZF) proteins. Now, the off-target ZF binding of pomalidomide-based PROTACs is evaluated by a high-throughput imaging screening platform, and minimization of off ...
openaire   +3 more sources

Peripheral RIPK2 degradation improves neurological outcomes after experimental ischemic stroke. [PDF]

J Cereb Blood Flow Metab
Howell JA, Larochelle J, Strawser M, De La Vega Mulet S, Tishko R, Gunraj R, Liu L, Candelario-Jalil E.   +7 more
europepmc   +1 more source

Preliminary Anti-Melanoma Activity of a Chlorogenic Acid-Based PROTAC Targeting MDM4, a Candidate Protein Identified by Proteomics. [PDF]

Foods
Mei Z, Sun J, Zhao P, Luo Y, Niu J, Huang D.   +5 more
europepmc   +1 more source

Revolutionizing protein degradation: Harnessing nanoparticles for PROTAC delivery. [PDF]

Mater Today Bio
Fan Y, Su J, Yang J, Guan X, Gong Y, Yang D, Qin A, Zhang L.   +7 more
europepmc   +1 more source