Results 71 to 80 of about 7,702 (129)

Agonist‐specific conformational dynamics at the β2‐adrenoceptor dictate allosteric modulation of Gαs signalling and bronchodilation

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose β2‐adrenoceptor (β2AR) agonists are the cornerstone of asthma therapy and promote bronchodilation through Gαs signalling in airway smooth muscle (ASM), but their efficacy is limited by β‐arrestin‐mediated β2AR desensitization.
Sushrut D. Shah, Joshua Richard, Suvankar Ghosh, Jillian Jerwick, Joice T. Gavali, Raymond B. Penn, Alexander D. MacKerell Jr, Deepak A. Deshpande   +7 more
wiley   +1 more source

Red fluorescent protein-aequorin fusions as improved bioluminescent Ca2+ reporters in single cells and mice.

PLoS ONE, 2011
Bioluminescence recording of Ca(2+) signals with the photoprotein aequorin does not require radiative energy input and can be measured with a low background and good temporal resolution.
Adil Bakayan, Cecilia F Vaquero, Fernando Picazo, Juan Llopis   +3 more
doaj   +1 more source

The selective degradation of PDE4B shortform, using a PROTAC, leads to inhibition of several hallmarks of cancer in HCT116 cells

British Journal of Pharmacology, EarlyView.
Background and Purpose Colorectal cancer is one of the most prevalent cancers worldwide, and novel precision medicine approaches are rapidly improving patient outcomes. Phosphodiesterase 4B (PDE4B) is a member of an enzyme family (PDE4) that hydrolyses intracellular cAMP to control spatial and temporal signalling cues.
Alina Zorn, John Daniel Pediani, Madihah Hussain, Jiayue Ling, Elaine Brown, Igor Belka, Eduardo Torres, Cathy Swindlehurst, Kyle Chan, David Stirling, George S. Baillie, Yuan Yan Sin   +11 more
wiley   +1 more source

Targeting KRAS for cancer therapy

British Journal of Pharmacology, EarlyView.
In recent years, therapeutics targeted against KRAS proto‐oncogene GTPase (KRAS)‐mutant cancers have seen significant progress. Herein we outline the biology and epidemiology of KRAS alterations at the lineage and allele levels, reviewing the clinical evidence for KRASG12C inhibition from the discovery of the recessive switch pocket to sotorasib ...
Jianlong Jia, Ruonan Liu, Tonia A. Adamide, Isis E. Fernandez, Georgios T. Stathopoulos   +4 more
wiley   +1 more source

Genetically encoded fluorogenic RNA-based bioluminescence resonance energy transfer (BRET) sensors for cellular imaging and target detection

SLAS Discovery
Fluorescence- and bioluminescence-based probes are valuable tools for understanding cell functions in health and disease. Bioluminescence offers an ideal complementary readout to fluorescence due to its minimal background interference and self ...
Lan Mi, Mingxu You
doaj   +1 more source

The Natural Quassinoid Brusatol Enhances Venetoclax Efficacy and Overcomes Resistance in Myeloid Leukemias

Cancer Science, EarlyView.
Schematic illustration of the mechanisms by which the natural quassinoid brusatol induces apoptosis in myeloid leukemias and enhances venetoclax efficacy via p53‐dependent apoptosis and mitochondrial dysfunction. ABSTRACT While venetoclax‐based combinations have shown promising results in acute myeloid leukemia (AML), the remission duration is ...
Shin‐ichiro Kawaguchi, Kazuya Sato, Junko Izawa, Norihito Takayama, Hiroko Hayakawa, Ken Suzaki, Susumu Goyama, Chiyoko Kato, Eiji Sakashita, Kaoru Tominaga, Hitoshi Endo, Yoshinobu Kanda   +11 more
wiley   +1 more source

In Vivo Biosensing Using Resonance Energy Transfer

Biosensors, 2019
Solution-phase and intracellular biosensing has substantially enhanced our understanding of molecular processes foundational to biology and pathology. Optical methods are favored because of the low cost of probes and instrumentation.
Shashi Bhuckory, Joshua C. Kays, Allison M. Dennis   +2 more
doaj   +1 more source

Ratiometric Zinc Biosensor Based on Bioluminescence Resonance Energy Transfer: Trace Metal Ion Determination with Tunable Response. [PDF]

Int J Mol Sci, 2022
Matveeva EG, Stoddard AK, Zeng HH, Franke G, Bourne L, Fierke CA, Thompson RB.   +6 more
europepmc   +1 more source

A Constellation of Fluorescent Biosensors to Illuminate the Galaxy of Protein Kinases

ChemBioChem, Volume 27, Issue 11, 15 June 2026.
Protein kinases (PKs) are enzymes that catalyze phosphorylation of protein substrates involved in a wide variety of biological signalling pathways. This review describes the different families and mechanisms of action and regulation of protein kinases, together with the different classes of fluorescent biosensors that have been engineered and ...
Timothe Abbura, May C. Morris
wiley   +1 more source

Applications of bioluminescence-mediated photodynamic therapy (BL-PDT) for the treatment of deep-seated tumours

Discover Oncology
Bioluminescence, the light generated through biochemical reactions involving luciferases in living organisms, has been the focus of extensive research due to its diverse applications.
Mpho Mohlongo, Blassan P. George, Heidi Abrahamse   +2 more
doaj   +1 more source