Results 171 to 180 of about 14,786 (290)

Tissue distribution and retention drives efficacy of rapidly clearing VHL-based PROTACs

Communications Medicine
Proteolysis-targeting chimeras (PROTACs) are being developed for therapeutic use. However, they have poor pharmacokinetic profiles and their tissue distribution kinetics are not known.
Donglu Zhang, Bin Ma, P. Dragovich, Li Ma, Shu Chen, E. Chen, Xiaofen Ye, Joyce Liu, Jennifer Pizzano, E. Bortolon, E. Chan, Xing Zhang, Yi-Chen Chen, Elizabeth S. Levy, R. Yauch, S. C. Khojasteh, C. E. Hop   +16 more
semanticscholar   +1 more source

Contemporary Applications of Chemical Libraries for Drug Discovery and Methods for Their Synthesis

ChemistryEurope, Volume 4, Issue 5, May 2026.
Screening of chemical libraries has over the past decades become a cornerstone of drug discovery. Today, a broad range of chemical libraries exist but they are often not well described in terms of diversity. This review describes current efforts which aim to visualize chemical diversity in compound collections and discuss current trends in synthetic ...
Tobias N. Hansen, Nils J. V. Hansen
wiley   +1 more source

PROTACs improve selectivity for targeted proteins

Acta Materia Medica
Proteolysis targeting chimera (PROTAC) technology has emerged as a powerful tool in drug discovery that enables targeted protein degradation through a unique bifunctional approach.
Lihua Liu, Xian Guan, Jiezhen Zhuo, Xifeng Wu, Xin Han   +4 more
doaj   +1 more source

CDK6 inactivation counteracts CALR‐mutant‐induced MPN evolution and sensitizes MPN stem cells to interferon‐α treatment

HemaSphere, Volume 10, Issue 5, May 2026.
Abstract Interferon‐α (IFNα) remains a potent therapeutic option for myeloproliferative neoplasms (MPNs) with an activated JAK/STAT signaling axis. However, variable patient responses highlight the need for optimized combination strategies. Recent studies suggest a link between cyclin‐dependent kinase 6 (CDK6) and IFN signaling.
Brian Ringhofer, Wolfram Polzer, Michaela Prchal‐Murphy, Eszter Doma, Sebastian Kollmann, Elisabeth Gamper, Jonatan Kendler, Belinda S. Maw, Eva Zebedin‐Brandl, Juan Li, Anthony R. Green, Maria‐Theresa Krauth, Emir Hadzijusufovic, Daniel Ivanov, Peter Valent, Gregor Hoermann, Thorsten Klampfl, Veronika Sexl, Karoline Kollmann   +18 more
wiley   +1 more source

CRBN‐PROTACs in Cancer Therapy: From Mechanistic Insights to Clinical Applications

Chemical Biology and Drug Design
Cereblon (CRBN), a member of the E3 ubiquitin ligase complex, has gained significant attention as a therapeutic target in cancer. CRBN regulates the degradation of various proteins in cancer progression, including transcription factors and signaling ...
Riya Thapa, A. Bhat, Gaurav Gupta, S. Renuka Jyothi, Irwanjot Kaur, Sachin Kumar, Naveen Sharma, G. V. S. Prasad, Atreyi Pramanik, Haider Ali   +9 more
semanticscholar   +1 more source

From Platelet Toxicity to Precision Targeting: Evolving Strategies to Overcome Thrombocytopenia in BCL‐2/BCL‐XL Inhibition

Health Science Reports, Volume 9, Issue 5, May 2026.
ABSTRACT Background Simultaneous blockade of the anti‐apoptotic proteins BCL‐2 and BCL‐XL has been shown to be efficacious in preclinical and clinical trials for tumors that are co‐dependent on their survival pathways, although clinical development has been limited owing to dose‐limiting thrombocytopenia associated with BCL‐XL inhibition.
Md Mohiuddin
wiley   +1 more source

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

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

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

Evaluation of Oral PROTAC Guidelines: Efflux Ratio Outweighs Chameleonicity Descriptors. [PDF]

ACS Med Chem Lett
Le Manach C, Viklund J, Kwapień K, Winiwarter S.   +3 more
europepmc   +1 more source