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Background: SUVN-I7016031 is a novel and selective positive allosteric modulator (PAM) of the M1 subtype of the muscarinic acetylcholine receptors (mAChRs). The proposed primary indication for SUVN-I7016031 is in the treatment of dementia such as Alzheimer's disease dementia (ADD) and Parkinson's disease dementia (PDD). In the current research, the pharmacological properties of SUVN-I7016031 in various types of dementia were investigated.
View Article and Find Full Text PDFDefining ortholog-specific UHRF1 inhibition by STELLA for cancer therapy.
Nat Commun
January 2025
Guangdong Provincial Key Laboratory of Stem Cell and Regenerative Medicine, CAS Key Laboratory of Regenerative Biology, China-New Zealand Joint Laboratory on Biomedicine and Health, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou, 510530, China.
UHRF1 maintains DNA methylation by recruiting DNA methyltransferases to chromatin. In mouse, these dynamics are potently antagonized by a natural UHRF1 inhibitory protein STELLA, while the comparable effects of its human ortholog are insufficiently characterized, especially in cancer cells. Herein, we demonstrate that human STELLA (hSTELLA) is inadequate, while mouse STELLA (mSTELLA) is fully proficient in inhibiting the abnormal DNA methylation and oncogenic functions of UHRF1 in human cancer cells.
View Article and Find Full Text PDFAn Azomethine Derivative, BCS3, Targets XIAP and cIAP1/2 to Arrest Breast Cancer Progression Through MDM2-p53 and Bcl-2-Caspase Signaling Modulation.
Pharmaceuticals (Basel)
December 2024
Department of Biochemistry, School of Medicine, Case Western Reserve University, Woods Building, W437, 2109 Adelbert Road, Cleaveland, OH 44106, USA.
: Breast cancer influences more than 2 million women worldwide annually. Since apoptotic dysregulation is a cancer hallmark, targeting apoptotic regulators encompasses strategic drug development for cancer therapy. One such class of apoptotic regulators is inhibitors of apoptosis proteins (IAP) which are a class of E3 ubiquitin ligases that actively function to support cancer growth and survival.
View Article and Find Full Text PDFAntagonistic interactions between spinosad and macrocyclic lactones in combination against larvae of the sheep blowfly, Lucilia cuprina, in vitro.
Vet Parasitol
January 2025
Virbac Australia Pty Ltd, Milperra, NSW 2214, Australia.
Control of the sheep blowfly relies on insecticides, however resistance is currently impacting on their efficacy. The use of insecticides in combination (mixtures) is considered to be a useful strategy to delay resistance under some circumstances. The present study aimed to examine the combination of spinosad with macrocyclic lactones in order to determine if the two drug classes showed any interactions that would impact on the usefulness of a combination product for flystrike control.
View Article and Find Full Text PDFSubtle Structural Modifications Spanning from EP4 Antagonism to EP2/EP4 Dual Antagonism: A Novel Class of Thienocyclic-Based Derivatives.
J Med Chem
January 2025
Shanghai Key Laboratory of Regulatory Biology, Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, Shanghai 200241, China.
The development of dual prostaglandin E receptors 2/4 (EP2/EP4) antagonists represents an attractive strategy for cancer immunotherapy. Herein, a series of 4,7-dihydro-5-thieno[2,3-]pyran derivatives with potent EP2/EP4 dual antagonism were discovered by fine-tuned structural modifications. The biphenyl side chain was found to be the key pharmacophore for the transition from EP4 antagonism to EP2/EP4 dual antagonism.
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