Results 91 to 100 of about 382,520 (299)

Discovery of novel and highly potent XIAP-targeted peptide inhibitors using virtual screening

Journal of Enzyme Inhibition and Medicinal Chemistry
Lung cancer, a globally prevalent fatal malignancy, remains a major therapeutic challenge. X-linked inhibitor of apoptosis protein (XIAP) is overexpressed in various cancers, driving uncontrolled proliferation, while its specific inhibition suppresses ...
Xiaoliang Wang, Mengting Lou, Yuting Wang, Miao-Miao Niu, Dongli Zhang   +4 more
doaj   +1 more source

TRAIL‐PEG‐Apt‐PLGA nanosystem as an aptamer‐targeted drug delivery system potential for triple‐negative breast cancer therapy using in vivo mouse model

Molecular Oncology, EarlyView.
Aptamers are used both therapeutically and as targeting agents in cancer treatment. We developed an aptamer‐targeted PLGA–TRAIL nanosystem that exhibited superior therapeutic efficacy in NOD/SCID breast cancer models. This nanosystem represents a novel biotechnological drug candidate for suppressing resistance development in breast cancer.
Gulen Melike Demirbolat, Aslihan Kucuk, Omer Erdogan, Samed Ozer, Bensu Kozan, Tugba Cuceli, Erkan Gumus, Evrim Cevik, Ozge Cevik   +8 more
wiley   +1 more source

X-linked inhibitor of apoptosis protein inhibitor Embelin induces apoptosis via PI3K/Akt pathway and inhibits invasion in osteosarcoma cells

Journal of Cancer Research and Therapeutics, 2018
Embelin is an active compound identified as a novel X-linked inhibitor of apoptosis protein (XIAP) inhibitor from the Embelia ribes that exhibits various medicinal effects including anti-inflammatory and anticancer activities. However, the therapeutic effect of Embelin to human osteosarcoma is not yet determined.In this study, we evaluated the ...
Hao, Qian, Tao, Huang, Yao, Chen, Xiucheng, Li, Weihua, Gong, Guangjian, Jiang, Wei, Zhang, Shuo, Cheng, Xuhui, Li, Pengcheng, Li   +9 more
openaire   +2 more sources

The PI3Kδ inhibitor roginolisib (IOA‐244) preserves T‐cell function and activity

Molecular Oncology, EarlyView.
Identification of novel PI3K inhibitors with limited immune‐related adverse effects is highly sought after. We found that roginolisib and idelalisib inhibit chronic lymphocytic leukemia (CLL) cells and Treg suppressive functions to similar extents, but roginolisib affects cytotoxic T‐cell function and promotion of pro‐inflammatory T helper subsets to a
Elise Solli, Alessio Bevilacqua, Mathias Wenes, Denis Migliorini, Lars van der Veen, Sigrid S Skånland, Giusy Di Conza, Kjetil Taskén   +7 more
wiley   +1 more source

The survivin/XIAP suppressant YM155 impairs clonal growth and induces apoptosis in JAK2V617F cells

Hematology, Transfusion and Cell Therapy
The central role of the control of apoptosis in the pathophysiology of Philadelphia chromosome-negative myeloproliferative neoplasms has recently been reinforced in genetic and pharmacological studies.
Jorge Antonio Elias Godoy Carlos, Keli Lima, Eduardo Magalhães Rego, Leticia Veras Costa-Lotufo, João Agostinho Machado-Neto   +4 more
doaj   +1 more source

Interaction of a Cyclic, Bivalent Smac Mimetic with the X-Linked Inhibitor of Apoptosis Protein [PDF]

Biochemistry, 2008
We have designed and synthesized a cyclic, bivalent Smac mimetic (compound 3) and characterized its interaction with the X-linked inhibitor of apoptosis protein (XIAP). Compound 3 binds to XIAP containing both BIR2 and BIR3 domains with a biphasic dose-response curve representing two binding sites with IC 50 values of 0.5 and 406 nM, respectively ...
Zaneta, Nikolovska-Coleska, Jennifer L, Meagher, Sheng, Jiang, Chao-Yie, Yang, Su, Qiu, Peter P, Roller, Jeanne A, Stuckey, Shaomeng, Wang   +7 more
openaire   +2 more sources

Ageing alters the severity of Sunitinib-induced cardiotoxicity: Investigating the mitogen activated kinase kinase 7 pathway association [PDF]

, 2019
Anti-cancer drug Sunitinib is linked to adverse cardiovascular events, which have shown to involve mitogen activated kinase kinase 7 (MKK7) pathway. Sunitinib-induced cardiotoxicity in 3, 12 and 24 months old male Sprague-Dawley rats and MKK7 expression ...
Cooper, Samantha, Hussain, Afthab, Maddock, Helen, Mee, Christopher, Sandhu, Hardip   +4 more
core   +1 more source

Tumour–host interactions in Drosophila: mechanisms in the tumour micro‐ and macroenvironment

Molecular Oncology, EarlyView.
This review examines how tumour–host crosstalk takes place at multiple levels of biological organisation, from local cell competition and immune crosstalk to organism‐wide metabolic and physiological collapse. Here, we integrate findings from Drosophila melanogaster studies that reveal conserved mechanisms through which tumours hijack host systems to ...
José Teles‐Reis, Tor Erik Rusten
wiley   +1 more source

Caspase 3 attenuates XIAP (X-linked inhibitor of apoptosis protein)–mediated inhibition of caspase 9 [PDF]

Biochemical Journal, 2007
During apoptosis, the initiator caspase 9 is activated at the apoptosome after which it activates the executioner caspases 3 and 7 by proteolysis. During this process, caspase 9 is cleaved by caspase 3 at Asp330, and it is often inferred that this proteolytic event represents a feedback amplification loop to accelerate apoptosis.
Jean-Bernard, Denault, Brendan P, Eckelman, Hwain, Shin, Cristina, Pop, Guy S, Salvesen   +4 more
openaire   +2 more sources

ATM in focus:a damage sensor and cancer target [PDF]

, 2012
The ability of a cell to conserve and maintain its native DNA sequence is fundamental for the survival and normal functioning of the whole organism and protection from cancer development.
Khalil, Hilal S., Tummala, Hemanth, Zhelev, Nikolai   +2 more
core   +4 more sources