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  • Open Access

    REVIEW

    Is autophagy induction by PARP inhibitors a target for therapeutic benefit?

    AHMED M. ELSHAZLY1,2, TUONG VI V. NGUYEN1, DAVID A. GEWIRTZ1,*

    Oncology Research, Vol.30, No.1, pp. 1-12, 2022, DOI:10.32604/or.2022.026459 - 06 December 2022

    Abstract PARP inhibitors have proven to be effective in conjunction with conventional therapeutics in the treatment of various solid as well as hematologic malignancies, particularly when the tumors are deficient in DNA repair pathways. However, as the case with other chemotherapeutic agents, their effectiveness is often compromised by the development of resistance. PARP inhibitors have consistently been reported to promote autophagy, a process that maintains cellular homeostasis and acts as an energy source by the degradation and reutilization of damaged subcellular organelles and proteins. Autophagy can exhibit different functional properties, the most prominent being cytoprotective. In More >

  • Open Access

    REVIEW

    Delaying Emergence of Resistance to KRAS Inhibitors with Adaptive Therapy: “Treatment-to-Contain” Instead of “Treatment-to-Cure”

    Amir Imran Faisal Hamdi, Johnson Stanslas*

    Oncologie, Vol.24, No.2, pp. 185-194, 2022, DOI:10.32604/oncologie.2022.023629 - 29 June 2022

    Abstract KRAS mutations are among the most common oncogenic abnormalities in cancer. Until recently, drug discovery pursuing KRAS did not produce therapeutic benefits for patients. Specific KRAS inhibitors, such as sotorasib and adagrasib, which bind covalently to codon 12 of substituted glycine to cysteine residue of the protein (G12C), have been approved by the FDA recently for the treatment of lung cancers. Binding of these drugs to the protein inhibits the activation of the GDP-bound inactive state to the GTP-bound active state. Phase 1/2 trials have shown potential anti-tumor activity, particularly in patients with previously treated More >

  • Open Access

    ARTICLE

    Triterpenoids from Uncaria rhynchophylla and Their PTP1B Inhibitory Activity

    Shuaibin Luo1, Xuemei Zhang2, Kang He1, Juan Zou1,*, Chang-An Geng2,*

    Phyton-International Journal of Experimental Botany, Vol.91, No.8, pp. 1809-1816, 2022, DOI:10.32604/phyton.2022.020935 - 14 April 2022

    Abstract Uncaria rhynchophylla (Gouteng) is a famous traditional Chinese medicine used for psychiatric and hypotensive purposes in China. In this study, the ethyl acetate (EtOAc) part of U. rhynchophylla was revealed with protein tyrosine phosphatase 1B (PTP1B) inhibitory activity. Subsequent investigation on the EtOAc part yielded one new triterpenoid, 3β-formyloxy-6β,19α-dihydroxyurs-12-en-28-oic acid (1) and four known ones, 3β,6β,19α-trihydroxyurs-12-en-28-oic acid (2), 2-oxopomolic acid (3), 3β,19α-dihydroxy-6-oxo-olean-12-en-28-oic acid (4) and sumaresinolic acid (5). The structure of compound 1 was determined by extensive HRESIMS, IR, 1D and 2D NMR spectroscopic analyses. Two ursane-type triterpenoids (2 and 3) showed selective inhibition on PTP1B with IC50 values of 48.2 and 178.7 μM. More >

  • Open Access

    REVIEW

    Ubiquitin Specific Protease 2: Structure, Isoforms, Cellular Function, Related Diseases and Its Inhibitors

    Hao Luo1,#,*, Yanjie Ji2,#, Xinrong Gao1, Xinying Liu1, Yunzhao Wu3, Yingli Wu3,*

    Oncologie, Vol.24, No.1, pp. 85-99, 2022, DOI:10.32604/oncologie.2022.021705 - 31 March 2022

    Abstract The ubiquitin-proteasome system (UPS) is an important pathway for cellular protein degradation. The components of this pathway, including the proteasome, ubiquitinase, and deubiquitinase, are highly specialized and strictly regulated. The ubiquitin-specific protease 2 (USP2) belongs to the ubiquitin-specific proteases, a subgroup of deubiquitinating enzymes. USP2 plays essential roles in regulating cell survival, cell cycle, circadian rhythm, cell metabolism, inflammatory response, antiviral response, and metastasis by interacting with certain proteins such as Cyclin D1, PER1, CRY1, HDM2/p53, FASN, LDLR, TRAF6, TBK1, and TGFBR1-TGFBR2 complex. Elevation of USP2 has been observed in a variety of cancers, including… More >

  • Open Access

    ARTICLE

    miR-181b promotes the oncogenesis of renal cell carcinoma by targeting TIMP3

    YUHUA ZOU1,#, LEI ZHANG2,#, XIN ZHONG3,*

    BIOCELL, Vol.46, No.5, pp. 1309-1317, 2022, DOI:10.32604/biocell.2022.018167 - 06 January 2022

    Abstract Renal cell carcinoma (RCC) has a poor prognosis due to limited diagnosis and treatment. Thus, it is necessary to find novel prognostic biomarkers and therapeutic targets. The aberrant expression of microRNAs plays an important role in RCC oncogenesis. Tissue inhibitors of metalloproteinase 3 (TIMP3) acts as a downstream target of miR-181b. The aim of this study was to understand the role and molecular mechanism of miR-181b in RCC oncogenesis. The results showed that miR-181b expression was significantly higher in RCC tumour tissues, especially in those with significant invasion or metastasis. miR-181b overexpression promoted proliferation and… More >

  • Open Access

    ARTICLE

    Performance Evaluation of a Novel and Effective Water-Soluble Aldehydes as Corrosion Inhibitor for Carbon Steel in Aggressive Hydrochloric Medium

    Yun Wang1, Tiantian Wang2, Bei Wang1, Wei Chang3, Jiangli Cao1, Lihua Hu3, Minxu Lu1, Lei Zhang1,*

    Journal of Renewable Materials, Vol.10, No.2, pp. 301-327, 2022, DOI:10.32604/jrm.2021.015518 - 30 August 2021

    Abstract A novel and effective water-soluble aldehydes (β-HA) as corrosion inhibitor was synthesized for N80 steel corrosion in 15% HCl solution, and the corrosion inhibition performance was evaluated by using weight loss, electrochemical measurements, scanning electron microscope (SEM), quantum chemical calculation and molecular dynamics simulation (MDS). The results show that synthesized β-HA showed excellent corrosion performance compared with MHB and PE for carbon steel in 15% HCl solution compared with MHB and PE, and the inhibition efficiency increased with increasing concentration of the inhibitor. The inhibition efficiency of β-HA at 8 mmol/L reached the maximum value 94.08%. The More >

  • Open Access

    ARTICLE

    Biological and molecular studies on specific immune cells treated with checkpoint inhibitors for the thera-personal approach of breast cancer patients (ex-vivo study)

    MOTAWA E. EL-HOUSEINI1, MOSTAFA S. ARAFAT2, AHMED M. EL-HUSSEINY3, ISLAM M. KASEM2, MAHMOUD M. KAMEL4, AHMED H. EL-HABASHY5, MEDHAT M. KHAFAGY6, ENAS M. RADWAN4, MAHA H. HELAL7, MONA S. ABDELLATEIF1,*

    Oncology Research, Vol.29, No.5, pp. 319-329, 2021, DOI:10.32604/or.2022.025249 - 10 October 2022

    Abstract Immunotherapy becomes a promising line of treatment for breast cancer (BC) however, its success rate is still limited. Methods: The study was designed to optimize the condition for producing an effective dendritic cell (DCs) based immunotherapy by using DCs and T lymphocytes together with tumor-infiltrating lymphocytes (TILs) and tumor-infiltrating DCs (TIDCs), treated with anti-PD1 and anti-CTLA4 monoclonal antibodies. This mixture of immune cells was co-cultured with autologous breast cancer cells (BCCs) isolated from 26 BC females. Results: There was a significant upregulation of CD86 and CD83 on DCs (P = 0.001 and 0.017, respectively), similarly upregulation of… More >

  • Open Access

    ARTICLE

    Synthesis, Pharmacological Evaluation, and In-Silico Studies of Thiophene Derivatives

    Raghav Mishra1,2,*, Nitin Kumar3, Neetu Sachan2

    Oncologie, Vol.23, No.4, pp. 493-514, 2021, DOI:10.32604/oncologie.2021.018532 - 31 December 2021

    Abstract The relevance of Retinoic acid receptor-related orphan receptors in cancer progression has sparked interest in developing multifunctional therapeutics. In the search for potentially active novel compounds with anticancer characteristics, the Gewald reaction was employed to develop different thiophene derivatives (8a–8i). Physicochemical and spectroanalytical investigations verified the molecular structures of the synthesized derivatives. Using an in vitro primary anticancer assay, NCI chose all of the synthesized molecules as prototypes and assessed their anticancer efficacy against a panel of various cancer cell lines representing nine distinct neoplasms. The compounds were found to have a wide range of anticancer… More >

  • Open Access

    REVIEW

    Dynamic Monitoring of Immunotherapy Effectiveness with Different Biomarkers in the Patients with Non-Small Cell Lung Cancer

    Sridha Ganesh1, Rui Wang1, Honglei Chen1,2

    Oncologie, Vol.23, No.3, pp. 335-350, 2021, DOI:10.32604/oncologie.2021.018610 - 26 September 2021

    Abstract Non-small cell lung cancer (NSCLC) constitutes about 84% of lung cancer. Hence, increased efforts have been fueled into immunotherapy of NSCLC with immune checkpoint inhibitors (ICIs). ICIs have recently taken off as promising immune-therapeutic methods that have slowed down the progress of NSCLC and equipped patients with survival advantages. However, the long-term respondents tally is less than 20% of the population. This low response rate warrants the need for dynamic biomarkers which will provide insight into the possible response of patients to ICIs. Biomarkers are biological molecules that predict the pathologic state of patients and… More >

  • Open Access

    ARTICLE

    Identification of potential inhibitors for Sterol C-24 reductase of Leishmania donovani through virtual screening of natural compounds

    FAZLUR RAHMAN1,#, SHAMS TABREZ1,#, RAHAT ALI1, SAJJADUL KADIR AKAND1, MOHAMMED A. ALAIDAROUS2,3, MOHAMMED ALSAWEED2, BADER MOHAMMED ALSHEHRI2, SAEED BANAWAS2,3, ABDUR RUB1,*, ABDUL AZIZ BIN DUKHYIL2,*

    BIOCELL, Vol.45, No.6, pp. 1601-1610, 2021, DOI:10.32604/biocell.2021.016682 - 01 September 2021

    Abstract Leishmaniasis is a vector-borne parasitic neglected tropical disease caused by a group of about 30 different species of the genus Leishmania. It is transmitted by the bite of female phlebotomies sand fly. Three main clinical manifestations of leishmaniasis include cutaneous, visceral, and mucocutaneous leishmaniasis. Visceral leishmaniasis (VL) caused by Leishmania donovani, is an infection of reticuloendothelial system and fatal if untreated. Cholesterol, a sterol that is prominent in the mammalian cell membranes whereas stigmasterol and ergosterol are more prevalent in plants, yeast, and protozoa, respectively. Ergosterols which is absent in human being, is an important constituent of… More >

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