npi-2358 and Pancreatic-Neoplasms

npi-2358 has been researched along with Pancreatic-Neoplasms* in 2 studies

Other Studies

2 other study(ies) available for npi-2358 and Pancreatic-Neoplasms

Article	Year
Combination of a novel microtubule inhibitor MBRI-001 and gemcitabine synergistically induces cell apoptosis by increasing DNA damage in pancreatic cancer cell lines. Investigational new drugs, 2020, Volume: 38, Issue:5 Pancreatic cancer (PC) is a highly malignant cancer with poor prognosis. Although gemcitabine (GEM; 2',2'-difluoro-deoxycytidine) has been used as the first-line chemotherapeutic agent in PC treatment for decades, its limited efficacy remains a significant clinical issue, which may be resolved by GEM combination therapy. In this study, we aimed to investigate the anti-tumor effects of MBRI-001 in combination with GEM in BxPC-3 and MIA PaCa-2 human PC cell lines. In vitro and in vivo results indicate that MBRI-001 showed synergistic activity with GEM. GEM induced apoptosis by increasing DNA damage (phosphorylated core histone protein H2AX (γ-H2AX)), MBRI-001 activated mitochondrial-apoptotic pathway (cleaved poly-ADP ribose polymerase (PARP)). Thus, the combination of the two intensified both apoptosis and DNA damage and showed significantly superior anti-tumor activity compared to each agent alone. The adoption of combination of MBRI-001 with GEM may be beneficial as they act synergistically and thus, can be a potential therapeutic choice for improving the prognosis of PC patients in the future. Topics: Animals; Antimetabolites, Antineoplastic; Apoptosis; Cell Line; Cell Survival; Deoxycytidine; Diketopiperazines; DNA Damage; Drug Synergism; Female; Gemcitabine; Humans; Mice, Inbred BALB C; Mice, Nude; Pancreatic Neoplasms; Rats, Wistar; Tubulin Modulators	2020
Design, synthesis and biological evaluation of anti-pancreatic cancer activity of plinabulin derivatives based on the co-crystal structure. Bioorganic & medicinal chemistry, 2018, 05-01, Volume: 26, Issue:8 Based on the co-crystal structures of tubulin with plinabulin and Compound 1 (a derivative of plinabulin), a total of 18 novel plinabulin derivatives were designed and synthesized. Their biological activities were evaluated against human pancreatic cancer BxPC-3 cell lines. Two novel Compounds 13d and 13e exhibited potent activities with IC Topics: Antineoplastic Agents; Binding Sites; Cell Line, Tumor; Cell Proliferation; Crystallography, X-Ray; Diketopiperazines; Drug Design; Humans; Molecular Docking Simulation; Pancreatic Neoplasms; Protein Structure, Tertiary; Solubility; Structure-Activity Relationship; Tubulin; Tubulin Modulators	2018

Article

Year

Combination of a novel microtubule inhibitor MBRI-001 and gemcitabine synergistically induces cell apoptosis by increasing DNA damage in pancreatic cancer cell lines.

Investigational new drugs, 2020, Volume: 38, Issue:5

Pancreatic cancer (PC) is a highly malignant cancer with poor prognosis. Although gemcitabine (GEM; 2',2'-difluoro-deoxycytidine) has been used as the first-line chemotherapeutic agent in PC treatment for decades, its limited efficacy remains a significant clinical issue, which may be resolved by GEM combination therapy. In this study, we aimed to investigate the anti-tumor effects of MBRI-001 in combination with GEM in BxPC-3 and MIA PaCa-2 human PC cell lines. In vitro and in vivo results indicate that MBRI-001 showed synergistic activity with GEM. GEM induced apoptosis by increasing DNA damage (phosphorylated core histone protein H2AX (γ-H2AX)), MBRI-001 activated mitochondrial-apoptotic pathway (cleaved poly-ADP ribose polymerase (PARP)). Thus, the combination of the two intensified both apoptosis and DNA damage and showed significantly superior anti-tumor activity compared to each agent alone. The adoption of combination of MBRI-001 with GEM may be beneficial as they act synergistically and thus, can be a potential therapeutic choice for improving the prognosis of PC patients in the future.

Topics: Animals; Antimetabolites, Antineoplastic; Apoptosis; Cell Line; Cell Survival; Deoxycytidine; Diketopiperazines; DNA Damage; Drug Synergism; Female; Gemcitabine; Humans; Mice, Inbred BALB C; Mice, Nude; Pancreatic Neoplasms; Rats, Wistar; Tubulin Modulators

2020

Design, synthesis and biological evaluation of anti-pancreatic cancer activity of plinabulin derivatives based on the co-crystal structure.

Bioorganic & medicinal chemistry, 2018, 05-01, Volume: 26, Issue:8

Based on the co-crystal structures of tubulin with plinabulin and Compound 1 (a derivative of plinabulin), a total of 18 novel plinabulin derivatives were designed and synthesized. Their biological activities were evaluated against human pancreatic cancer BxPC-3 cell lines. Two novel Compounds 13d and 13e exhibited potent activities with IC

Topics: Antineoplastic Agents; Binding Sites; Cell Line, Tumor; Cell Proliferation; Crystallography, X-Ray; Diketopiperazines; Drug Design; Humans; Molecular Docking Simulation; Pancreatic Neoplasms; Protein Structure, Tertiary; Solubility; Structure-Activity Relationship; Tubulin; Tubulin Modulators

2018