Oxadiazole: A highly versatile scaffold in drug discovery

N Desai, J Monapara, A Jethawa… - Archiv der …, 2022 - Wiley Online Library
As a pharmacologically important heterocycle, oxadiazole paved the way to combat the
problem associated with the confluence of many commercially available drugs with different …

Tackling COVID‐19 infection through complement‐targeted immunotherapy

S Jodele, J Köhl - British Journal of Pharmacology, 2021 - Wiley Online Library
The complement system is an ancient part of innate immunity sensing highly pathogenic
coronaviruses by mannan‐binding lectin (MBL) resulting in lectin pathway activation and …

A Bifunctional Copper Catalyst Enables Ester Reduction with H2: Expanding the Reactivity Space of Nucleophilic Copper Hydrides

BM Zimmermann, TT Ngoc, DI Tzaras… - Journal of the …, 2021 - ACS Publications
Employing a bifunctional catalyst based on a copper (I)/NHC complex and a guanidine
organocatalyst, catalytic ester reductions to alcohols with H2 as terminal reducing agent are …

The “C3aR antagonist” SB290157 is a partial C5aR2 agonist

XX Li, V Kumar, RJ Clark, JD Lee… - Frontiers in …, 2021 - frontiersin.org
Innate immune complement activation generates the C3 and C5 protein cleavage products
C3a and C5a, defined classically as anaphylatoxins. C3a activates C3aR, while C5a …

Functional profiling of the G protein-coupled receptor C3aR1 reveals ligand-mediated biased agonism

P Rodriguez, LJ Laskowski, JP Pallais, HA Bock… - Journal of Biological …, 2024 - ASBMB
G protein-coupled receptors (GPCRs) are leading druggable targets for several medicines,
but many GPCRs are still untapped for their therapeutic potential due to poor understanding …

Nonacidic thiophene‐based derivatives as potential analgesic and design, synthesis, biological evaluation, and metabolic stability study

DS Mikhail, HB El‐Nassan… - Drug Development …, 2022 - Wiley Online Library
Nonsteroidal anti‐inflammatory drugs represent one of the most popularly used classes of
drugs. However, their long‐term administration is associated with various side effects …

The role of human C5a as a non-genomic target in corticosteroid therapy for management of severe COVID19

A Das, S Rana - Computational Biology and Chemistry, 2021 - Elsevier
Complement system plays a dual role; physiological as well as pathophysiological. While
physiological role protects the host, pathophysiological role can substantially harm the host …

Ras-Related Protein Rab5a Regulates Complement C5a Receptor Trafficking, Chemotaxis, and Chemokine Secretion in Human Macrophages

KC Wu, ND Condon, TA Hill, RC Reid… - Journal of Innate …, 2023 - karger.com
Abstract Complement activation and Rab GTPase trafficking are commonly observed in
inflammatory responses. Recruitment of innate immune cells to sites of infection or injury …

[HTML][HTML] Protocol for cell-based screening assay to measure ERK1/2 phosphorylation as a readout for complement receptor activation

XX Li, TM Woodruff - STAR protocols, 2023 - Elsevier
The complement receptors C3aR and C5aR1 are promising therapeutic targets. Here, we
present a protocol to screen the effects of different agonists and antagonists on these …

[HTML][HTML] JR14a: A Novel Antagonist of C3aR Attenuates Neuroinflammation in Cerebral Ischemia-Reperfusion Injury

J Tang, N Maihemuti, Y Fang, J Tan, M Jia, Q Mu… - Brain Research …, 2024 - Elsevier
Cerebral ischemia-reperfusion injury (CIRI), a prevalent stroke-related complication, can
lead to severe brain damage. Inflammation is a crucial factor in CIRI pathogenesis, and the …