Results 241 to 250 of about 209,848 (307)

Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt

British Journal of Pharmacology, EarlyView.
Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown, Alan Armstrong, David J. Mann   +2 more
wiley   +1 more source

Survival strategies of mycoplasmas: the critical role of post-translational modifications. [PDF]

Front Cell Infect Microbiol
Li T, Yuan H, Zhang W, Guo F.
europepmc   +1 more source

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

The stress-activated kinase p38 mediates non-canonical activation of Src and tyrosine phosphorylation of the adapter protein TAB1. [PDF]

J Biol Chem
Onuma I, Iwata Y, Zhou Y, Nakada M, Kondo A, Iwahara H, Natori K, Yokoyama S, Chihara K, Takeuchi K, Sada K, Ozawa T, Mizuguchi M, Yamagishi N, Kracht M, Sakurai H.   +15 more
europepmc   +1 more source

Thrombospondin‐4 is upregulated in abdominal aortic aneurysm: A vasoprotective response with potential therapeutic relevance

British Journal of Pharmacology, EarlyView.
TSP4 is upregulated in human and experimental AAA. TSP4 knockdown accelerated AAA formation and exacerbated both vascular inflammation and remodelling, emphasizing that TSP4 upregulation may represent a protective response against AAA. Our findings suggest that preserving TSP4 could be a useful strategy in the clinical management of AAA.
Laia Blanco‐Casoliva, Lidia Puertas‐Umbert, Judith Alonso, Rafael Almendra‐Pegueros, Saray Varona, Mercedes Camacho, Gemma Arderiu, Lluís Asmarats, Marta Alegret, Jose Martinez‐Gonzalez, Cristina Rodriguez   +10 more
wiley   +1 more source

Cellular phospho-signaling map of the enigmatic serine/threonine kinase MAST2. [PDF]

Biochem Biophys Rep
Fathima I, Mahin A, Priyanka P, Naurah Vattoth N, Nishana A, Perunelly Gopalakrishnan A, Soman S, Raju R.   +7 more
europepmc   +1 more source

The Overlooked Autoantibody Repertoire: Exploring the Biomarker Potential of Downregulated Autoantibodies in NSCLC

Cancer Science, EarlyView.
This study identifies downregulated autoantibodies in NSCLC and demonstrates their diagnostic and prognostic utility. Integrating proteome‐wide screening and large‐cohort validation, we highlight a novel biomarker class that enhances early detection and patient stratification.
Yihao Liang, Hanke Ma, Wenke Sun, Ying Chen, Fengqi Chen, Yutong Li, Songyun Ouyang, Liping Dai   +7 more
wiley   +1 more source

Revealing and Exploiting the Biochemistry of <i>O</i>-GlcNAc through Protein Semisynthesis. [PDF]

Biochemistry
Ampomah GB, Pratt MR.
europepmc   +1 more source

Reversal of MPPa‐PDT Resistance in Osteosarcoma by Targeting ROCK2‐Mediated Autophagy

Cell Proliferation, EarlyView.
ROCK2 competes with MST1 to bind to the aa 28‐198 region of SAV1 and then regulates the Hippo pathway to affect autophagy, resulting in the resistance of OS to MPPa‐PDT. Targeted inhibition of ROCK2 by screening for J059‐0149 increases the sensitivity of osteosarcoma to MPPa‐PDT. ABSTRACT Osteosarcoma (OS) is a primary bone tumour that occurs mostly in
Xuan Yi, Xueqiang Deng, Jianyong Deng, Chen Li, Hong Peng, Yunyan Du, Qing Li, Xiaohua Yan, Xin Hu, Yan Zheng, Shenliang Chen, Ting Xiong, Debin Xu, Leifeng Chen, Liang Hao   +14 more
wiley   +1 more source