Results 51 to 60 of about 10,651,893 (289)

Discovery and Biological Evaluation of a Series of Pyrrolo[2,3-b]pyrazines as Novel FGFR Inhibitors

Molecules, 2017
Abnormality of fibroblast growth factor receptor (FGFR)-mediated signaling pathways were frequently found in various human malignancies, making FGFRs hot targets for cancer treatment. To address the consistent need for a new chemotype of FGFR inhibitors,
Yan Zhang, Hongchun Liu, Zhen Zhang, Ruifeng Wang, Tongchao Liu, Chaoyun Wang, Yuchi Ma, Jing Ai, Dongmei Zhao, Jingkang Shen, Bing Xiong   +10 more
doaj   +1 more source

Potent, Selective Inhibitors of Fibroblast Growth Factor Receptor Define Fibroblast Growth Factor Dependence in Preclinical Cancer Models [PDF]

Molecular Cancer Therapeutics, 2011
Abstract We describe here the identification and characterization of 2 novel inhibitors of the fibroblast growth factor receptor (FGFR) family of receptor tyrosine kinases. The compounds exhibit selective inhibition of FGFR over the closely related VEGFR2 receptor in cell lines and in vivo.
Matthew Squires, George Ward, Gordan Saxty, Valerio Berdini, Anne Cleasby, Peter King, Patrick Angibaud, Tim Perera, Lynsey Fazal, Douglas Ross, Charlotte Griffiths Jones, Andrew Madin, Rajdeep K. Benning, Emma Vickerstaffe, Alistair O'Brien, Martyn Frederickson, Michael Reader, Christopher Hamlett, Michael A. Batey, Sharna Rich, Maria Carr, Darcey Miller, Ruth Feltell, Abarna Thiru, Susanne Bethell, Lindsay A. Devine, Brent L. Graham, Andrew Pike, Jose Cosme, Edward J. Lewis, Eddy Freyne, John Lyons, Julie Irving, Christopher Murray, David Newell, Neil T. Thompson   +35 more
openaire   +3 more sources

Fibroblast Growth Factor 22 is not essential for skin development and repair but plays a role in tumorigenesis [PDF]

, 2012
Fibroblast Growth Factors play critical roles during development, tissue homeostasis and repair by controlling cell proliferation, survival, migration and differentiation.
Robbez-Masson, L, Ian Rosewell, Grose Richard, Cross, B, Rosewell, I, Athina-Myrto Chioni (156542), Robbez-Masson, Luisa, Rosewell Ian, Chioni Athina-Myrto, Jarosz, Monika, Barbara Cross (156544), Barbara Cross, Grose, Richard, Chioni, A-M, Rosewell, Ian, Cross Barbara, Richard Grose (156552), Chioni, Athina-Myrto, Cross, Barbara, Jarosz, M, Luisa Robbez-Masson (156539), Grose, R, Luisa Robbez-Masson, Jarosz Monika, Ian Rosewell (156548), Monika Jarosz, Richard Grose, Robbez-Masson Luisa, Monika Jarosz (156537), Athina-Myrto Chioni   +29 more
core   +2 more sources

Engineering peptides into antibodies—opportunities and strategies for therapeutic innovation

FEBS Letters, EarlyView.
Peptides and antibodies occupy complementary therapeutic niches. Peptides recognize difficult targets in a compact format, while antibodies add specificity, long half‐life, and effector functions. This review examines strategies that merge both modalities—peptide grafting into loops, terminal and Fc fusions, and bioconjugation—highlighting how ...
Jinling Wang, Ruslana Romaniuk, Hristo L. Svilenov   +2 more
wiley   +1 more source

Skeletal overgrowth in a pre-pubescent child treated with pan-FGFR inhibitor

Heliyon
Fibroblast growth factors and their receptors (FGFR) have major roles in both human growth and oncogenesis. In adults, therapeutic FGFR inhibitors have been successful against tumors that carry somatic FGFR mutations.
Fataneh Majlessipour, Gaohui Zhu, Nicole Baca, Meenasri Kumbaji, Vivian Hwa, Moise Danielpour   +5 more
doaj   +1 more source

Discovery of a series of dimethoxybenzene FGFR inhibitors with 5H-pyrrolo[2,3-b]pyrazine scaffold: structure–activity relationship, crystal structural characterization and in vivo study

Acta Pharmaceutica Sinica B, 2019
Genomic alterations are commonly found in the signaling pathways of fibroblast growth factor receptors (FGFRs). Although there is no selective FGFR inhibitors in market, several promising inhibitors have been investigated in clinical trials, and showed ...
Peng Wei, Bo Liu, Ruifeng Wang, Yinglei Gao, Lanlan Li, Yuchi Ma, Zhiwei Qian, Yuelei Chen, Maosheng Cheng, Meiyu Geng, Jingkang Shen, Dongmei Zhao, Jing Ai, Bing Xiong   +13 more
doaj   +1 more source

Liver organoids: modelling complexity in homeostasis and disease

FEBS Letters, EarlyView.
Studying liver in vitro has been challenging because simple 2D cell cultures fail to capture liver's cellular and architectural complexity. To bridge this gap, scientists increasingly use organoids, 3D liver models which better mimic liver composition and function. This review examines recent advances in liver organoid complexity and realism, discusses
Anna M. Dowbaj, Meritxell Huch
wiley   +1 more source

Novel insights into the cardio-protective effects of FGF21 in lean and obese rat hearts [PDF]

, 2014
Aims: Fibroblast growth factor 21 (FGF21) is a hepatic metabolic regulator with pleotropic actions. Its plasma concentrations are increased in obesity and diabetes; states associated with an increased incidence of cardiovascular disease.
Muhammad F Bari, Bari Muhammad F., Jing Chen, Edward W. Hillhouse (519261), Bari, Muhammad F., Raghu Adya (519258), Patel Vanlata, Bhudia, Sunil K., Edward W Hillhouse, Harpal S Randeva, Vanlata Patel, Raghu Adya, Chen Jing, Manjunath Ramanjaneya, Bee K. Tan (417731), Ramanjaneya, Manjunath, Jing Chen (4762), Patel, Vanlata H., Ramanjaneya Manjunath, Harpal S. Randeva (417734), Randeva Harpal S., Muhammad F. Bari (417733), Tan, Bee K., Adya Raghu, Adya, Raghu, Tan Bee K., Bhudia Sunil K., Randeva, Harpal S., Bee K Tan, Manjunath Ramanjaneya (519259), Sunil K Bhudia, Sunil K. Bhudia (519260), Hillhouse Edward W., Vanlata Patel (519257), Hillhouse, Edward W., Chen, Jing   +35 more
core   +1 more source

The microbiome in human skin aging

FEBS Letters, EarlyView.
Age‐related skin changes encompass the well‐known visible phenotypic alterations, together with microbiome dysbiosis and a series of molecular aging hallmarks. These hallmarks characterize not only a fully stablished aged phenotype but also the skin aging process itself.
Manuel Huerta Arana, Cornelia Wiegand, Omid Omrani, Mario Fabri   +3 more
wiley   +1 more source

Ligand‐dependent transcriptional heterogeneity in cell cycle gene expression delays G1/S entry

FEBS Letters, EarlyView.
EGF and HRG induce distinct G1/S progression programs in ErbB2‐amplified BT474 breast cancer cells. Despite activating the potent ErbB2–ErbB3 heterodimer, HRG does not accelerate cell‐cycle entry. Instead, EGF promotes earlier restriction‐point passage via ERK–FOS signaling, whereas HRG activates the AKT–MYC axis, driving transcriptional heterogeneity ...
Ririn Rahmala Febri, Ayaka Nagasato‐Ichikawa, Keita Iida, Shuhei Kimura, Akira Imamoto, Mariko Okada   +5 more
wiley   +1 more source