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1.
J Pain Res ; 16: 4393-4404, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-38164227

RESUMO

Objective: Knee osteoarthritis (KOA) is a common chronic degenerative joint disease, and acupuncture is an alternative therapy for KOA. This study aims to detect the effectiveness of acupuncture at LI11 in improving pain and function for KOA patients. Methods: A total of 108 patients with KOA were randomly allocated to Control Group (local points), Treatment Group A (LI11), and Treatment Group B (local points and LI11) with a treatment phase of 4 weeks and a follow-up phase of 4 weeks. Primary outcome was response rate. Secondary outcomes included Visual Analogue Scale (VAS), Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC), and recurrence rate. Study was registered on Chinese Clinical Trial Registry (Registered number: ChiCTR2000034926). Results: The response rate in Treatment Group A, Treatment Group B, and Control Group was 71.43%, 85.29%, and 51.53%, respectively, at Week 4, and Treatment Group B was significantly higher than Control Group (difference[98.3% CI]: 33.86[0.135,0.543], P = 0.003). Although no significant difference was found, Treatment Group A had a better response rate compared with Control Group (difference[98.3% CI]: 20.00 [-0.072, 0.472], P = 0.086). For VAS and WOMAC, there were significant differences within 3 groups at Week 4 compared with the baseline. There was a significant improvement in VAS scores and WOMAC function and pain subscales at Week 4 in Treatment Group B compared with Control Group and Treatment Group A. Conclusion: LI11 is an effective point for patients with KOA, and it could be a selection for young acupuncturists and acupuncturists who work in rural areas; however, large-sample studies are necessary to further verify results in the future.

2.
J Med Chem ; 60(24): 10151-10171, 2017 12 28.
Artigo em Inglês | MEDLINE | ID: mdl-29155580

RESUMO

The epigenetic regulator CBP/P300 presents a novel therapeutic target for oncology. Previously, we disclosed the development of potent and selective CBP bromodomain inhibitors by first identifying pharmacophores that bind the KAc region and then building into the LPF shelf. Herein, we report the "hybridization" of a variety of KAc-binding fragments with a tetrahydroquinoline scaffold that makes optimal interactions with the LPF shelf, imparting enhanced potency and selectivity to the hybridized ligand. To demonstrate the utility of our hybridization approach, two analogues containing unique Asn binders and the optimized tetrahydroquinoline moiety were rapidly optimized to yield single-digit nanomolar inhibitors of CBP with exquisite selectivity over BRD4(1) and the broader bromodomain family.


Assuntos
Ensaios de Triagem em Larga Escala/métodos , Fatores de Transcrição de p300-CBP/antagonistas & inibidores , Animais , Asparagina/química , Asparagina/metabolismo , Sítios de Ligação , Proteínas de Ciclo Celular , Cristalografia por Raios X , Feminino , Transferência Ressonante de Energia de Fluorescência/métodos , Camundongos Endogâmicos , Simulação de Acoplamento Molecular , Proteínas Nucleares/antagonistas & inibidores , Domínios Proteicos , Pirazóis/química , Piridinas/química , Quinolinas/química , Fatores de Transcrição/antagonistas & inibidores , Fatores de Transcrição de p300-CBP/química , Fatores de Transcrição de p300-CBP/metabolismo
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