Results 291 to 300 of about 127,473 (347)

Bispecific nanobody® as a new pharmacological drug for the selective inhibition of Trypsin‐3

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Proteolytic balance is dysregulated in many diseases, with proteases playing critical roles in pathological pathways. A high level of Trypsin‐3 expression has been implicated as a significant mediator of tumour progression and metastasis, and this protease is associated with poor prognosis for patients in various cancers.
Melissa David, Anaïs Faihy, Corinne Rolland, Anissa Edir, Astrid Canivet, Laetitia Ligat, Mireille Sebbag, Nathalie Vergnolle, Aurélien Olichon, Céline Deraison   +9 more
wiley   +1 more source

Convergent High O₂ Affinity but Distinct ATP-Mediated Allosteric Regulation of Hemoglobins in Oviparous and Viviparous Eremias Lizards from the Qinghai-Tibet Plateau. [PDF]

Animals (Basel)
Pu P, Niu Z, Ma M, Tang X, Chen Q.
europepmc   +1 more source

GPCR‐G protein signalling and its mutational landscape in cancer—Driver or passenger

British Journal of Pharmacology, EarlyView.
G protein‐coupled receptors (GPCRs) play a crucial role in cellular signalling, regulating various physiological processes. Abnormal expression and mutations of GPCRs have been implicated in several types of cancer, influencing tumour initiation, progression and immune response.
Chenlin Feng, Jasper F. Ooms, Erik H. J. Danen, Laura H. Heitman   +3 more
wiley   +1 more source

Pharmacological evaluation of non‐nucleotide purine derivatives as P2X7 antagonists for the treatment of neuroinflammation in traumatic brain injury

British Journal of Pharmacology, EarlyView.
Background and purpose Traumatic brain injury (TBI) is considered to be a leading cause of mortality and disability worldwide. After TBI, innate immunity is rapidly activated in response to damage‐associated molecular patterns, such as ATP release, recognised by P2X7 receptors.
Inés Valencia, Andrea Pastor‐Martínez, Céline Decouty‐Pérez, Ana Belen Lopez‐Rodriguez, María Álvarez‐Rubal, Eva Ramos, Francesco Calzaferri, Jorge Zamorano‐Fernández, Javier Giner‐García, Alexis J. Palpán‐Flores, Víctor Rodríguez‐Domínguez, Javier Rodríguez de Cía, Borja J. Hernández‐García, Alejandro Romero, Cristóbal de los Ríos, Javier Egea   +15 more
wiley   +1 more source

Structure–activity relationship of the allosteric effects of ivermectin at human P2X4 and GABAA receptors

British Journal of Pharmacology, EarlyView.
Abstract Background and purpose Positive allosteric modulation of the P2X4 receptor is a potential route to providing cardiovascular benefit through enhancing flow‐dependent arterial vasodilation and providing cardioprotection. However, ligands that selectively enhance P2X4 activity are absent.
Jessica L. Meades, Marcella Bassetto, Marius C. Staiculescu, Gayathri Swaminath, Samuel J. Fountain   +4 more
wiley   +1 more source

Treatment‐Free Remission in Chronic Myeloid Leukemia: Revisiting the “W” Questions

European Journal of Haematology, EarlyView.
ABSTRACT Chronic myeloid leukemia (CML) has undergone a transformation from a fatal disease to a chronic, manageable condition with the advent of tyrosine kinase inhibitors (TKIs), particularly imatinib. This shift has significantly improved survival rates, and for some patients, achieving deep molecular response (DMR) has made treatment‐free remission
Antonella Bruzzese, Ernesto Vigna, Enrica Antonia Martino, Nicola Amodio, Caterina Labanca, Francesco Mendicino, Eugenio Lucia, Virginia Olivito, Fortunato Morabito, Massimo Gentile   +9 more
wiley   +1 more source

Inhibition of tumor–microenvironment interaction and tumor invasion by small-molecule allosteric inhibitor of DDR2 extracellular domain [PDF]

, 2018
Grither, Whitney R., Longmore, Gregory D.   +1 more
core   +1 more source

Clioquinol as a new therapy in epilepsy: From preclinical evidence to a proof‐of‐concept clinical study

Epilepsia, EarlyView.
Abstract Objective Drug‐resistant epilepsy (DRE) affects >25 million people worldwide and is often associated with neuroinflammation. Increasing evidence links deficiency or malfunctioning of the enzyme phosphoglycerate dehydrogenase (PHGDH), which converts 3‐phosphoglycerate to generate serine and the neurotransmitter glycine, with (drug‐resistant ...
Karin Thevissen, Annelii Ny, Daniëlle Copmans, Jana Tits, Kenichi Kamata, Eva Gielis, Kevin Longin, Jo Sourbron, Peravina Thergarajan, Tracie Huey‐Lin Tan, Idrish Ali, Nigel C. Jones, Terence J. O'Brien, Mastura Monif, Bridgette D. Semple, Christine Germeys, Benedetta Frizzi, Virginia Minniti, Sebastian Perrone, Carole L. Linster, Ilaria Elia, Ludo Van Den Bosch, Bruno P. A. Cammue, Arnout Voet, Lieven Lagae, Peter de Witte   +25 more
wiley   +1 more source

PI5P4K inhibitors: promising opportunities and challenges

The FEBS Journal, EarlyView.
Developing inhibitors is like climbing a steep, challenging mountain. PI5P4K inhibitors hold significant promise for the treatment of cancer, immune disorders, and neurological diseases. However, the path to success is fraught with hurdles, and researchers are therefore required to apply their expertise to overcome critical “checkpoints.” While some ...
Koh Takeuchi, Lisa Nagase, Shun Kageyama, Hirotaka Kanoh, Masashi Oshima, Aki Ogawa‐Iio, Yoshiki Ikeda, Yuki Fujii, Sei Kondo, Natsuki Osaka, Takeshi Masuda, Tsukasa Ishihara, Yoshikazu Nakamura, Yoshihisa Hirota, Takehiko Sasaki, Toshiya Senda, Atsuo T. Sasaki   +16 more
wiley   +1 more source

Molecular mechanisms of hotspot variants in cytoskeletal β‐actin associated with Baraitser–Winter syndrome

The FEBS Journal, EarlyView.
Variants at position R196 in cytoskeletal β‐actin are the most common variants associated with Baraitser–Winter cerebrofrontofacial syndrome and result in craniofacial anomalies and neurodevelopmental disorders, most likely due to neuronal migration defects. This study explores the molecular mechanisms of p.R196 variants using purified proteins.
Johannes N. Greve, Dietmar J. Manstein
wiley   +1 more source