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 …
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 …
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 …
organocatalyst, catalytic ester reductions to alcohols with H2 as terminal reducing agent are …
The “C3aR antagonist” SB290157 is a partial C5aR2 agonist
Innate immune complement activation generates the C3 and C5 protein cleavage products
C3a and C5a, defined classically as anaphylatoxins. C3a activates C3aR, while C5a …
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 …
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 …
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
Complement system plays a dual role; physiological as well as pathophysiological. While
physiological role protects the host, pathophysiological role can substantially harm the host …
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
Abstract Complement activation and Rab GTPase trafficking are commonly observed in
inflammatory responses. Recruitment of innate immune cells to sites of infection or injury …
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 …
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 …
lead to severe brain damage. Inflammation is a crucial factor in CIRI pathogenesis, and the …