Results 121 to 130 of about 90,202 (264)

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

open access: yesBritish 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   +2 more
wiley   +1 more source

Hypericin Suppresses Liver Cancer Through Autophagic Degradation of AKT and Eliciting Antitumor Immune Response

open access: yesCancer Science, EarlyView.
Hypericin induces autophagic AKT degradation by promoting AKT‐HSPA5 interaction in an S473 phosphorylation‐dependent manner, suppressing HCC growth. It enhances CD8+ T cell‐mediated antitumor immunity and synergizes with anti‐PD‐L1 therapy, showing favorable safety for HCC treatment. ABSTRACT Hepatocellular carcinoma (HCC) is the most prevalent primary
Sien Ma   +12 more
wiley   +1 more source

Proteomic Analysis Reveals AMPKα‐Mediated Antiandrogen Resistance via Ferroptosis Suppression in Prostate Cancer

open access: yesCancer Science, EarlyView.
Antiandrogen‐resistant prostate cancer cells acquire ferroptosis resistance through AMPKα activation and upregulation of ferroptosis suppressor pathways. This adaptive state creates a therapeutic vulnerability, as GPX4 inhibition, particularly in combination with AMPKα inhibition, effectively suppresses the growth of resistant cells.
Masaki Shiota   +8 more
wiley   +1 more source

The antitumor promise of furo[2,3-<i>d</i>]pyrimidine: a 2016-2025 review. [PDF]

open access: yesRSC Adv
Mansour MA   +10 more
europepmc   +1 more source

New Treatment Strategy and Future Research Direction for BRAF‐Mutated Cancer

open access: yesCancer Science, EarlyView.
Treatment with BRAF inhibitor plus MEK inhibitor is currently used in BRAF‐mutated various malignancies except colorectal cancer, and treatments with BRAF and/or MEK inhibitors and anti‐EGFR antibody are used in BRAF‐mutated colorectal cancer. Despite recent advances in BRAF‐targeted therapies, their efficacy is still limited.
Masanobu Takahashi   +2 more
wiley   +1 more source

Evidence of Antiproliferative Activity in the Liverwort <i>Isotachis serrulata</i> from Southern Ecuador. [PDF]

open access: yesMolecules
Andrade JM   +6 more
europepmc   +1 more source

Daraxonrasib and Beyond: Pan‐RAS Inhibition, Resistance, and Next‐Generation Strategies

open access: yesCancer Science, EarlyView.
ABSTRACT RAS proteins have long been considered difficult therapeutic targets, but allele‐selective inhibitors established the clinical tractability of mutant RAS. Daraxonrasib (RMC‐6236), an oral pan‐RAS inhibitor, has now extended this concept by targeting multiple mutant and wild‐type RAS proteins.
Ryo Honda
wiley   +1 more source

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