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A Model for Decoding Resistance in Precision Oncology: Acquired Resistance to FGFR inhibitors in Cholangiocarcinoma.
Ann Oncol
December 2024
Department of Medicine, Massachusetts General Hospital Cancer Center, Harvard Medical School, Boston, MA.
Article Synopsis
- FGFR inhibitors have shown promise in treating FGFR-altered cholangiocarcinoma, but acquired resistance poses a challenge to their effectiveness.
- The study utilized diverse investigative methods, including DNA analysis and tissue biopsies, to explore resistance mechanisms in a cohort of patients.
- Results indicated that a significant number of patients with clinical benefits had specific FGFR2 mutations, but polyclonal resistance was influenced by low drug concentrations and specific mutation types affecting drug efficacy.
Novel deoxyhypusine synthase (DHPS) inhibitors target hypusination-induced vasculogenic mimicry (VM) against malignant melanoma.
Pharmacol Res
November 2024
Department of Pharmacy, Shengjing Hospital of China Medical University, Shenyang 110004, China. Electronic address:
Article Synopsis
- This study focuses on developing inhibitors for deoxyhypusine synthase (DHPS), which is crucial for targeting vasculogenic mimicry (VM) in malignant melanoma, a factor linked to poor patient outcomes.
- A new compound, 7k, was identified as effective in inhibiting DHPS activity and was shown to affect the expression of specific genes involved in VM, contributing to its anti-melanoma properties.
- Testing in zebrafish and various models shows that 7k not only impacts melanoma cell behavior but also demonstrates significant effectiveness against melanoma growth, revealing DHPS as a vital target for treatment.
Isoform-specific inhibition of FGFR signaling achieved by a de-novo-designed mini-protein.
Cell Rep
October 2022
Department of Pharmacology, Yale University School of Medicine, New Haven, CT 06520, USA. Electronic address:
Article Synopsis
- - The study focuses on fibroblast growth factor receptors (FGFRs) and their regulated signaling processes, particularly the interaction between specific FGF ligands and two FGFR isoforms (b- and c-isoforms).
- - Researchers have developed a mini-protein called mb7, designed to bind to the ligand-binding region of FGFR2, which shows high affinity for the c-isoform and inhibits its signaling from certain FGFs.
- - Mb7 also blocks interactions between FGFRs and Klotho proteins, acting as an antagonist to metabolic hormones FGF19 and FGF21, which could lead to new therapeutic approaches for diseases linked to faulty FGFR activation.
Peptide ligands targeting FGF receptors promote recovery from dorsal root crush injury via AKT/mTOR signaling.
Theranostics
February 2022
Institute of Biomedicine & Department of Cell Biology, College of Life Science and Technology, Jinan University; Guangdong Province Key Laboratory of Bioengineering Medicine; Guangdong Provincial biotechnology drug & Engineering Technology Research Center; National Engineering Research Center of Genetic Medicine, Guangzhou, Guangdong, 510632, P. R. China.
Fibroblast growth factor receptors (FGFRs) are key targets for nerve regeneration and repair. The therapeutic effect of exogenous recombinant FGFs is limited due to their high molecular weight. Small peptides with low molecular weight, easy diffusion, low immunogenicity, and nontoxic metabolite formation are potential candidates.
View Article and Find Full Text PDFAcute and chronic effects of a light-activated FGF receptor in keratinocytes in vitro and in mice.
Life Sci Alliance
November 2021
Department of Biology, Institute of Molecular Health Sciences, Eidgenössische Technische Hochschule (ETH) Zurich, Zurich, Switzerland
FGFs and their high-affinity receptors (FGFRs) play key roles in development, tissue repair, and disease. Because FGFRs bind overlapping sets of ligands, their individual functions cannot be determined using ligand stimulation. Here, we generated a light-activated FGFR2 variant (OptoR2) to selectively activate signaling by the major FGFR in keratinocytes.
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