Results 151 to 160 of about 14,319 (272)

Design and Evaluation of Bivalent K‐Ras Inhibitors That Target the CAAX Binding Site and the Acidic Surface of Farnesyltransferase and Geranylgeranyltransferase I

open access: yesChemistry – A European Journal, EarlyView.
Chemical inhibition of K‐Ras posttranslational prenylation represents a promising strategy against aggressive cancers. A structure‐based design produces piperidine‐based peptidomimetics conjugated to cationic modules, effectively inhibiting FTase and GGTase I at single‐digit nanomolar concentrations.
Naomi Horiuchi   +8 more
wiley   +1 more source

Peptide‐based covalent inhibitors of protein–protein interactions

open access: yesJournal of Peptide Science, Volume 29, Issue 1, January 2023., 2023
Peptide interaction motifs derived from a protein–protein interaction interface can serve as starting points for the development of inhibitors. However, for certain proteins when applying competitive inhibitors, peptide‐based ligands with an irreversible binding mode may be more active. This review summarizes examples of covalent inhibitors that employ
Felix M. Paulussen, Tom N. Grossmann
wiley   +1 more source

A truncation mutant of adenomatous polyposis coli impairs apical cell extrusion through elevated epithelial tissue tension

open access: yesCytoskeleton, EarlyView.
Abstract Tissue tension encompasses the mechanical forces exerted on solid tissues within animal bodies, originating from various sources such as cellular contractility, interactions with neighboring cells and the extracellular matrix. Emerging evidence indicates that an imbalance in such forces can influence structural organization, homeostasis, and ...
Wan J. Gan   +7 more
wiley   +1 more source

Disruption of salt bridge interactions in the inter‐domain cleft of the tubulin‐like protein FtsZ of Escherichia coli makes cells sensitive to the cell division inhibitor PC190723

open access: yesCytoskeleton, EarlyView.
Abstract FtsZ forms a ring‐like assembly at the site of division in bacteria. It is the first protein involved in the formation of the divisome complex to split the cell into two halves, indicating its importance in bacterial cell division. FtsZ is an attractive target for developing new anti‐microbial drugs to overcome the challenges of antibiotic ...
Sakshi Mahesh Poddar   +3 more
wiley   +1 more source

Tumor Suppression of Ras GTPase-Activating Protein RASA5 through Antagonizing Ras Signaling Perturbation in Carcinomas

open access: yesiScience, 2019
Summary: Aberrant RAS signaling activation is common in cancers with even few Ras mutations, indicating alternative dysregulation other than genetic mutations.
Lili Li   +13 more
doaj  

Whole‐genome CRISPR‐Cas9 knockout screens identify SHOC2 as a genetic dependency in NRAS‐mutant melanoma

open access: yes
Cancer Communications, EarlyView.
Andrea Y. Gu   +6 more
wiley   +1 more source

Tristetraprolin affects invasion‐associated genes expression and cell motility in triple‐negative breast cancer model

open access: yesCytoskeleton, EarlyView.
Abstract Tristetraprolin (TTP) is an RNA‐binding protein that negatively regulates its target mRNAs and has been shown to inhibit tumor progression and invasion. Tumor invasion requires precise regulation of cytoskeletal components, and dysregulation of cytoskeleton‐associated genes can significantly alter cell motility and invasive capability. Several
Anastasiia Hubiernatorova   +5 more
wiley   +1 more source

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