Results 101 to 110 of about 6,610 (202)

Artificial intelligence empowers targeted protein degradation: Core technological innovations, multi‐scenario applications, and translational prospects

Smart Molecules, EarlyView.
AI is transforming TPD by improving the design, prediction, and optimization of degraders such as PROTACs, molecular glues, and LYTACs. This review summarizes key AI‐driven advances, highlights applications across drug discovery stages, and discusses remaining challenges and future directions for accelerating the development of therapies against ...
Shuanglin Qin, Rui Peng, Guangshuai Zhang, Si Yan, Jin Xiao, Zishu Liu, Ziyu Tan, Qingqing Xie, Shangjie Li, Wei Luo, Xiaohe Xiao   +10 more
wiley   +1 more source

Ponatinib as targeted therapy for FGFR1 fusions associated with the 8p11 myeloproliferative syndrome

Haematologica, 2013
The 8p11 myeloproliferative syndrome is a rare, aggressive myeloproliferative neoplasm characterized by constitutively active FGFR1 fusion proteins that arise from specific chromosomal translocations and which drive aberrant proliferation. Although FGFR1
Andrew Chase, Catherine Bryant, Joannah Score, Nicholas C.P. Cross   +3 more
doaj   +1 more source

Defective FGFR1 Signaling Disrupts Glucose Regulation: Evidence From Humans With FGFR1 Mutations

Journal of the Endocrine Society
Abstract Context Activation of fibroblast growth factor receptor 1 (FGFR1) signaling improves the metabolic health of animals and humans, while inactivation leads to diabetes in mice. Direct human genetic evidence for the role of FGFR1 signaling in human metabolic health has not been fully established.
Maria I Stamou, Crystal J Chiu, Shreya V Jadhav, Vanessa Ferreira Lopes, Kathryn B Salnikov, Lacey Plummer, Margaret F Lippincott, Hang Lee, Stephanie B Seminara, Ravikumar Balasubramanian   +9 more
openaire   +2 more sources

PPM1G‒MET axis sustains AKT signaling to drive Twist‐associated EMT and drug resistance in hepatocellular carcinoma

VIEW, EarlyView.
Hepatocellular carcinoma (HCC) is frequently resistant to targeted therapies. We identify protein phosphatase Mg2+/Mn2+‐dependent 1G (PPM1G) as a key phosphatase that stabilizes mesenchymal‐epithelial transition factor (MET) by inhibiting its ubiquitination, thereby sustaining protein kinase B (AKT) signaling and promoting Twist‐mediated epithelial ...
Weixun Wu, Songbin Lin, Cong Zhou, Jinwu Hu, Kun Liu, Yongfeng Xu, Zhenbin Ding, Mengting Luo, Bo Hu   +8 more
wiley   +1 more source

The diverse dependence of galectin-1 and -8 on multivalency for the modulation of FGFR1 endocytosis

Cell Communication and Signaling
Fibroblast growth factor receptor 1 (FGFR1) is a N-glycosylated cell surface receptor tyrosine kinase, which upon recognition of specific extracellular ligands, fibroblast growth factors (FGFs), initiates an intracellular signaling.
Dominika Żukowska, Aleksandra Chorążewska, Krzysztof Ciura, Aleksandra Gędaj, Marta Kalka, Marta Poźniak, Natalia Porębska, Łukasz Opaliński   +7 more
doaj   +1 more source

The kinase inhibitor TKI258 is active against the novel CUX1-FGFR1 fusion detected in a patient with T-lymphoblastic leukemia/lymphoma and t(7;8)(q22;p11)

Haematologica, 2011
We report a patient with T-lymphoblastic leukemia/lymphoma and a t(7;8)(q22;p11). CUX1 was identified as the fusion partner of FGFR1 by fluorescence in situ hybridization and 5′ RACE-PCR.
Bartosz Wasag, Els Lierman, Peter Meeus, Jan Cools, Peter Vandenberghe   +4 more
doaj   +1 more source

Pathways of Epithelial Barrier Breakdown and Remodeling in Esophageal Organoids by Commonly Used Surfactants

Allergy, EarlyView.
This study shows that SDS and CAPB directly impair esophageal epithelial barrier integrity in primary EoE‐derived models. SDS induces stronger inflammatory, oxidative stress, and keratinization responses than CAPB. Both surfactants promote epithelial remodeling and partial epithelial‐mesenchymal transition (EMT), with CAPB showing a distinct ...
Ozge Ardicli, Duygu Yazici, Huseyn Babayev, Yagiz Pat, Manal Bel Imam, Hang Du, Hassan Melhem, Carina Beha, Laura Buergi, Anja Heider, Juan‐Felipe López, Sena Ardicli, Can Zeyneloğlu, Andrea Kreienbühl, Nino Stocker, Patrick Westermann, Christoph B. Messner, Mübeccel Akdis, Jan Hendrik Niess, Alain Schoepfer, Luc Biedermann, Cezmi A. Akdis, Swiss EoE Cohort Study Group, Patrick Aepli, Luc Biedermann, Ruggero Biral, Carine Blanchard, Lorenzo Botteselle, Simon Buetikofer, Emanuel Burri, Joachim Diebold, Annika Eckhold, Annett Franke, Michèle Frei, Thomas Greuter, Chantal Hasler, Wolfram Jochum, Tanja Kilchmann, Seraina Koller, Andrea Kreienbühl, Fritz Murray, Peter Netzer, Gabrielle Reichhart, Elodie Ristorcelli, Gerhard Rogler, Jean‐Benoit Rossel, Ekaterina Safroneeva, Catherine Saner, Christoph Schlag, Jon‐Duri Senn, Alain Schoepfer, Philipp Schreiner, Christine Sempoux, Dagmar Simon, Hans‐Uwe Simon, Alex Straumann, Sven Trelle, Achim Weber, Niels Willi, Marcel Zwahlen, Willem van de Veen   +60 more
wiley   +1 more source

A Spotlight on Yolk‐sac Tumors: Molecular Pathology, Current Diagnostics, and Novel Therapeutics

Andrology, EarlyView.
ABSTRACT Background Yolk‐sac tumors are an aggressive subtype of testicular cancer that significantly contribute to disease progression and therapy resistance, especially in adults. While testicular cancer generally has high cure rates with cisplatin‐based treatment, adult yolk‐sac tumors often appear as components of mixed tumors with poor response to
Evangelos Prokakis, Lisa Schneider, Felix Bremmer, Daniel Nettersheim   +3 more
wiley   +1 more source

Distinct stem cell myeloproliferative/T lymphoma syndromes induced by ZNF198-FGFR1 and BCR-FGFR1 fusion genes from 8p11 translocations [PDF]

, 2004
8p11 myeloproliferative syndrome (EMS) is a hematopoietic stem cell disorder characterized by myeloid hyperplasia and non-Hodgkin's lymphoma with chromosomal translocations fusing several genes, most commonly ZNF198, to fibroblast growth factor receptor ...
Krause, Daniela S., Cross, Nicholas CP, Asiedu, Frances, Neumann, Carola A, Dimitri, Christopher A, Dimitri, Christopher A., Cross, Nicholas C.P., Cross, Nicholas C.P, Van Etten, Richard A., Neumann, Carola A., Krause, Daniela S, Van Etten, Richard A, Roumiantsev, Sergei   +12 more
core   +1 more source

Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt

British Journal of Pharmacology, EarlyView.
Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown, Alan Armstrong, David J. Mann   +2 more
wiley   +1 more source