Results 221 to 230 of about 3,595,860 (302)

An intracellular recombinant single‐chain variable antibody fragment as a new class of phosphodiesterase type 5 inhibitors

British Journal of Pharmacology, EarlyView.
Background and Purpose Cyclic guanosine monophosphate (cGMP) is a ubiquitous second messenger involved in human (patho‐)physiology. Phosphodiesterase 5 (PDE5) is a major cGMP hydrolyzing enzyme in many cell types including vascular smooth muscle cells (VSMCs). Several highly selective PDE5 inhibitors are in clinical use. However, there are currently no
Kürsat Kirkgöz, Sophie Sprenger, Olga Schweigert, Sanika Mohagaonkar, Matti Walsdorff, Tanja Zeller, Filip Berisha, Viacheslav O. Nikolaev, Sergei D. Rybalkin   +8 more
wiley   +1 more source

Serine/Threonine-Protein Kinase mTOR [PDF]

, 2020
openaire   +1 more source

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

Functional phosphoproteomic analysis of SMG1 in nonsense-mediated mRNA decay and DNA damage repair in cancer. [PDF]

Front Syst Biol
Pai AKA, Dcunha L, Gopalakrishnan AP, Ummar S, Rajeev AC, Raju R.   +5 more
europepmc   +1 more source

Serine/Threonine-Protein Kinase Nek9 [PDF]

, 2020
openaire   +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

Genome-Wide Identification of CRK Family Members in Solanaceae Crops and Functional Characterization of <i>CaCRK10</i> and <i>SmCRK6</i> in Salt Stress Response. [PDF]

Curr Issues Mol Biol
Lyu J, Yu D, Zhang Y, Chen Q, Hu W, Xin Y, Yang F, Yang G, Ji T.   +8 more
europepmc   +1 more source

Cardiotoxicity of BRAF/MEK inhibitors

British Journal of Pharmacology, EarlyView.
Abstract Rapidly accelerated fibrosarcoma type B/B‐Raf proto‐oncogene, serine/threonine kinase (BRAF) and mitogen‐activated protein kinase (MEK) inhibitors have transformed outcomes in cancer therapy, particularly in melanoma. However, cardiovascular toxicities are increasingly recognized in real‐world clinical practice.
Katharina Seuthe, Valerie Lohner, Kevin Terre, Thomas Riffelmacher, Roman Pfister   +4 more
wiley   +1 more source

Phosphoproteomic Data Integration Reveals Paralog-Specific Co-Regulatory Networks of Rho-Associated Kinases ROCK1 and ROCK2. [PDF]

Int J Mol Sci
Vaz CE, Suresh M, Dcunha L, Raju R, Kanekar S.   +4 more
europepmc   +1 more source

Targeting KRAS for cancer therapy

British Journal of Pharmacology, EarlyView.
In recent years, therapeutics targeted against KRAS proto‐oncogene GTPase (KRAS)‐mutant cancers have seen significant progress. Herein we outline the biology and epidemiology of KRAS alterations at the lineage and allele levels, reviewing the clinical evidence for KRASG12C inhibition from the discovery of the recessive switch pocket to sotorasib ...
Jianlong Jia, Ruonan Liu, Tonia A. Adamide, Isis E. Fernandez, Georgios T. Stathopoulos   +4 more
wiley   +1 more source