Bibliometric analysis of research trends on the combination of immune checkpoint inhibitors and PARP inhibitors in solid tumors

Heliyon, Год журнала: 2024, Номер 10(2), С. e24452 - e24452

Опубликована: Янв. 1, 2024

Immune checkpoint inhibitors (ICIs) has made significant achievements in the therapeutics of various tumor types, and recently growing evidence from preclinical studies clinical trials indicated that poly-ADP-ribose polymerase (PARPi) are exhibiting encouraging synergism with ICIs. The aim our current study is to explore development pattern literature related combined therapy ICIs PARPi solid tumors a bibliometric perspective.

Язык: Английский

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Zhi Zhu Ma Ren pill relieves constipation in mice through endoplasmic reticulum stress-mediated apoptosis

American Journal of Translational Research, Год журнала: 2024, Номер 16(10), С. 5829 - 5845

Опубликована: Янв. 1, 2024

This study explores the detailed effects and mechanisms of Zhi Zhu Ma Ren Pill (ZZMRP) on constipation.

Язык: Английский

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Design, Synthesis, and Biological Evaluation of a Series of Benzofuran [3,2-D]Pyrimidine-4(1h)-Ketone Derivatives Containing Thiosemicarbazone Analogs as Novel Parp-1 Inhibitors

Опубликована: Янв. 1, 2023

Poly ADP ribose polymerase-1 (PARP-1) plays a crucial role in processes such as DNA damage repair, gene transcription, and cell apoptosis cancer cells. Therefore, PARP-1 represents promising target to develop anticancer drugs. By summarizing the structure-activity relationship of inhibitors, series benzofuran [3,2-D]pyrimidine-4(1H)-ketone derivatives containing thiosemicarbazide or its analogs were designed, synthesized biologically evaluated on their inhibition PARP enzyme activity. Among all compounds, 19c exhibited superior biological activity with IC50 values 22 nM 4.98 μM for exogenous SK-OV-3 cells, respectively, better than Olaparib. In addition, showed low toxicity normal liver Anti-cancer mechanism studies revealed that could inhibit repair single-strand breakage aggravate double-strand by inhibiting activity, promote cells through mitochondrial pathway. all, these complexes may have potential novel inhibitors.

Язык: Английский

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Targeted Protein Degraders- The Druggability Perspective

Journal of Pharmaceutical Sciences, Год журнала: 2023, Номер 113(3), С. 539 - 554

Опубликована: Ноя. 4, 2023

Язык: Английский

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