Results 141 to 150 of about 18,386 (273)

Targeting protein–protein interactions with reversible covalent modalities: Non‐cysteine chemistries

British Journal of Pharmacology, EarlyView.
Abstract Protein–protein interactions (PPIs) are central to diverse cellular functions, and represent a rapidly expanding class of therapeutic targets. Advancements in covalent drug design have enabled small‐molecule drugs to overcome challenges associated with engaging these targets, such as limited durations of action and difficult‐to‐drug (expansive,
Ruchira Basu, Steven Fletcher
wiley   +1 more source

Renal‐vascular axis: unmasking its role in vascular endothelial growth factor‐inhibitor vascular toxicity in cancer patients

British Journal of Pharmacology, EarlyView.
Abstract Vascular toxicity is a growing concern in cancer patients receiving vascular endothelial growth factor inhibitor (VEGFi) therapy, posing a significant threat to patient prognosis. While the primary mechanism of VEGFi‐induced vascular toxicity is linked to redox‐sensitive reactions that disrupt vascular tone, leading to hypertension and ...
Grace Whelan, Karla B. Neves
wiley   +1 more source

Investigating the Residue-Level Dynamics of the Thrombin-Thrombomodulin Interaction [PDF]

Biophysical Journal, 2020
Riley B. Peacock, Taylor McGrann, Elizabeth A. Komives   +2 more
openaire   +1 more source

Haemostatic changes and bleeding with anti‐IL‐6 directed therapy in autoimmune diseases

British Journal of Pharmacology, EarlyView.
Abstract Anti‐IL‐6 directed therapy, especially tocilizumab (TCZ), is widely used for the treatment of autoimmune diseases such as rheumatoid arthritis, giant cell arteritis and systemic juvenile idiopathic arthritis. Next to being a master regulator of inflammation, IL‐6 also is an important regulator of haemostasis. Although generally well tolerated,
Charlotte D. C. C. van der Heijden, Loes C. Oskam, Lenny van Bon, Chantal P. Rovers   +3 more
wiley   +1 more source

Interactions between small leucine‐rich proteoglycans and proteases: implications for tissue homeostasis and pathology

The FEBS Journal, EarlyView.
Small leucine‐rich proteoglycans (SLRPs) are key modulators of extracellular matrix structure and signaling. Their proteolytic processing by MMPs (Matrix Metalloproteinases), ADAMTS (disintegrin and metalloprotease with thrombospondin motifs), and serine proteases generates bioactive fragments that regulate collagen remodeling, inflammation, and ...
Maria Konstantaraki, Lydia‐Nefeli Thrapsanioti, Aikaterini Berdiaki, Ioanna Spyridaki, Dragana Nikitovic   +4 more
wiley   +1 more source

Investigating transthyretin variants H88R and I107V in amyloid priming: From destabilization to complete dissociation

The FEBS Journal, EarlyView.
Investigated mutations in transthyretin (TTR) disrupt the F87‐centered hydrophobic core that stabilizes its tetrameric structure. The mild I107V mutation weakens inter‐chain packing, while H88R fully abolishes tetramer formation, yielding a monomeric, aggregation‐prone form. Structural, biophysical, and computational analyses reveal that both mutations
István L. Bódy, Zsolt Fazekas, Nóra Wágner, Anna J. Kiss‐Szemán, Veronika Harmat, Zoltán Pozsonyi, Dóra K. Menyhárd, András Perczel   +7 more
wiley   +1 more source

Mechanistic insights into HapC: A key enzyme in prodiginine biosynthesis in Hahella chejuensis

The FEBS Journal, EarlyView.
HapC catalyzes prodiginine biosynthesis through coordinated movements of its ATP‐binding, substrate‐binding, and catalytic‐swivel domains. The enzyme shows tolerance toward short‐chain MAP analogs, and docking analyses reveal key residues and structural features underlying its substrate flexibility.
Yueh‐Te Chan, Aden Dhana Rizkita, Hsin‐Ju Hsieh, Shu‐Fang Hsu, Tony Eight Lin, Wei‐Jan Huang, Kai‐Cheng Hsu, Sheila Nathan, Peiching Chang, Andrew H.‐J. Wang, Cheng‐Chung Lee   +10 more
wiley   +1 more source

UNDERSTANDING GENERALIZED ALLOSTERY IN THROMBIN

, 2018
Thrombin is a critical drug target for chemotherapeutic and antithrombotic therapy development. Although many experiments have demonstrated that thrombin is a multifunctional allosteric enzyme, the exact mechanism of thrombin's allostery is still unclear
Xiao, Jiajie
core  

Solution Biophysical Characterization of the Thrombin- Thrombomodulin Interation [PDF]

, 2013
The final step of the blood coagulation cascade is the activation of thrombin. Active thrombin cleaves fibrinogen to create fibrin which polymerizes into clots. Regulation of thrombin is imperative to maintaining normal hemostasis.
Treuheit, Nicholas Adam
core  

Proteolytic remodelling of the extracellular matrix by pericytes

The FEBS Journal, EarlyView.
Pericytes are specialised perivascular cells intimately connected with endothelial cells and essential for the maintenance of vascular beds. They contribute to the formation and remodelling of the extracellular matrix by actively secreting proteases and protease inhibitors.
Tina Burkhard, Ella Milne, Kate Qian, Paola Campagnolo, Salvatore Santamaria   +4 more
wiley   +1 more source