The proposed mechanism of action for the CDK12/13 inhibitor and cyclin K degrader, CT7439. CDK12/13 inhibition interrupts transcription elongation, leading to increased DNA damage that results in cell death. This agent is a potentially novel treatment option for patients with colorectal cancer. Created in BioRender. Cyclin‐dependent kinase (CDK) 12 and
Wylie K. Watlington +10 more
wiley +1 more source
Drug resistance limits treatment success in a subset of lung cancers driven by ROS1 gene alterations. Using patient‐derived cells and computer simulations, we studied three key mutations and how they affect five targeted drugs. The mutations reduced drug effectiveness in different ways by altering protein structure and behavior.
Farhan Ul Haq +8 more
wiley +1 more source
Sulfonamide-Based 2-Amino-1,3,4-Oxadiazole Derivatives as Dual Cholinesterase and Carbonic Anhydrase Inhibitors: Design, Synthesis, Kinetic Characterization, Molecular Modeling, and ADMET Evaluation. [PDF]
Arslan Karahan G +4 more
europepmc +1 more source
Recent Progress in Urea-Containing Compounds as Tyrosine Kinase Inhibitors. [PDF]
Sroor FM.
europepmc +1 more source
Gut microbiome-derived indoles differentially suppress type III secretion system-associated virulence in <i>Escherichia coli</i> and <i>Salmonella enterica</i>. [PDF]
Shvarthburg M +4 more
europepmc +1 more source
Heterocyclic-Based Fungicides: Emerging Strategies for Viable Plant Disease Control. [PDF]
Tahlan S +4 more
europepmc +1 more source
Rational Design of Multifunctional Tacrine Derivatives as Candidates for the Treatment of Alzheimer and Parkinson Diseases. [PDF]
Dzib E +3 more
europepmc +1 more source
An investigation of 2-hydrazinyl-1,3-benzothiazole, 4-amino-4H-1,2,4-triazole and 2-hydrazinyl-1H-benzimidazole applicability as derivatization reagents for HPLC-HRMS determination of steroid hormones in urine. [PDF]
Zorina M +7 more
europepmc +1 more source

