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Review
Biotechnology & Applied Microbiology
Saba S. Shaikh et al.
Summary: Triple negative breast cancer (TNBC), which lacks estrogen receptor, progesterone receptor, or human epidermal growth factor2, accounts for approximately 15% of breast cancer patients. Limited treatment options have historically been available, but recent transcriptomic analyses have revealed the biological heterogeneity of TNBC. Predictive biomarkers based on the distinct biology of TNBC subtypes have been identified to determine which patients will benefit the most from targeted therapies. Two biomarker-driven treatments have been recently approved.
EXPERT OPINION ON BIOLOGICAL THERAPY
(2022)
Review
Medicine, Research & Experimental
Tapan Behl et al.
Summary: Depression is characterized by increased inflammation and oxidative stress. Natural polyphenols play a vital role in regulating cell signaling pathways related to oxidative stress and inflammation, demonstrating their potential in preventing and treating depressive disorder. Understanding the mechanism of polyphenols in cell signaling pathways is essential for developing novel compounds for depression treatment.
BIOMEDICINE & PHARMACOTHERAPY
(2022)
Review
Pharmacology & Pharmacy
Rudradip Das et al.
Summary: Tyrosine kinases are enzymes that regulate the activity of proteins within cells, playing a role in physiological alterations. Research on type IV inhibitors is currently limited, and further efforts are needed to fill in the gaps in knowledge.
DRUG DISCOVERY TODAY
(2022)
Article
Oncology
R. Bradley et al.
Summary: Aromatase inhibitors are more effective than tamoxifen in reducing the risk of breast cancer recurrence in premenopausal women receiving ovarian suppression. The main benefit is observed in the first 4 years of treatment, with no additional benefit or loss of benefit in the following years up to 10.
Article
Chemistry, Medicinal
Bilal Litim et al.
Summary: Novel alpha-aminophosphonates derivatives incorporating quinoline or quinolone, and coumarylthiazole or 5-phenylthiazol-2-amine moieties were synthesized and screened for antimicrobial activity. The compounds showed moderate to strong inhibitory activities against Gram-positive and Gram-negative bacteria, with some exhibiting excellent antifungal inhibition. Structure-activity relationship analysis indicated that certain structural moieties enhanced the inhibitory activity against microbial pathogens, suggesting the synthesized compounds as potential antimicrobial drug candidates.
MEDICINAL CHEMISTRY RESEARCH
(2022)
Review
Biochemistry & Molecular Biology
Asim Najmi et al.
Summary: Natural products are an important source of new lead compounds in drug discovery research, especially those derived from plants. Despite pharmaceutical companies' lack of attention to natural product drug discovery, recent technological advancements have revived scientific interest. This review provides a comprehensive overview of the various approaches used in selecting, authenticating, extracting/isolating, screening, and developing natural products, with a focus on bioactivity-guided fractionation. The integration of interdisciplinary approaches, technological advances, and new methods holds great potential for the future development of therapeutic drugs.
Review
Chemistry, Multidisciplinary
Fakhria A. Al-Joufi et al.
Summary: This article addresses the molecular pathogenesis of colorectal cancer (CRC) and highlights the potential of biomarkers for predicting disease behavior and prognosis. It also provides conceptual knowledge of nanotechnology-based diagnostic techniques and therapeutic approaches for malignant CRC.
Article
Toxicology
R. Raveesha et al.
Summary: A series of new thiazole derivatives were synthesized and their anticancer activities were investigated. The results showed good anticancer effects of these compounds in various cancer cell lines. The anticancer mechanisms were studied and evaluated by molecular docking with the HER2 receptor. The compounds were found to comply with Lipinski's rule of five and showed potential in terms of electronic properties.
COMPUTATIONAL TOXICOLOGY
(2022)
Article
Chemistry, Medicinal
Salah A. Abdel-Aziz et al.
Summary: A new series of pyrimidine/thiazole hybrids 7a-p were synthesized as selective COX-2/sEH inhibitors with analgesic and anti-inflammatory effects, and lower cardiotoxicity effects. Some hybrids showed the greatest COX-2-inhibitory activity and were discovered to be the most potent dual COX-2/sEH inhibitors, with improved ulcerogenic and cardioprotective properties.
ARCHIV DER PHARMAZIE
(2022)
Review
Biochemistry & Molecular Biology
Kurt Engeland
Summary: RB and p53 are central tumor suppressors that play key roles in regulating the cell division cycle. RB downregulates numerous genes by forming complexes with E2F transcription factors, and its repression is released through phosphorylation. p53 activates CDKN1A gene to regulate RB phosphorylation, leading to expression of cell cycle regulators. There is an overlap between RB and DREAM signaling pathways.
CELL DEATH AND DIFFERENTIATION
(2022)
Review
Oncology
Yichen Tian et al.
Summary: Hepatocellular carcinoma (HCC) is the second leading cause of cancer-related death, primarily due to high incidence and late-stage diagnosis. Tyrosine kinase inhibitors (TKIs) have shown significant clinical efficacy and low incidence of adverse reactions in the treatment of HCC. However, resistance to sorafenib and other TKIs presents a major challenge. Recent mechanistic studies have identified several factors involved in apoptosis, angiogenesis, cell proliferation, and TKI resistance in HCC patients. Exploring and overcoming these resistance mechanisms is crucial to extending the therapeutic benefits of TKIs to patients with TKI-resistant HCC.
CURRENT CANCER DRUG TARGETS
(2022)
Review
Biochemistry & Molecular Biology
Santhi Latha Pandrangi et al.
Summary: This paper discusses the importance of iron in regulating cell death in tumor cells and cancer stem cells, as well as the molecular characteristics of iron-induced ferroptosis and apoptosis.
Article
Chemistry, Medicinal
Abdallah E. Abdallah et al.
Summary: In this study, a new series of piperazinylquinoxaline-based derivatives were designed and synthesized to find new effective and safer anticancer agents. The most promising candidate, compound 11, showed better antitumor activity and VEGFR-2 kinase inhibition compared to sorafenib. It also increased apoptosis rate and altered the expression of important proteins in HepG-2 cells.
DRUG DESIGN DEVELOPMENT AND THERAPY
(2022)
Article
Chemistry, Multidisciplinary
Abeer M. El-Naggar et al.
Summary: The synthesis and screening of a series of 5-hydrazinyl-2-(2-(1-(thien-2-yl)ethylidene)hydrazinyl)thiazole derivatives with dual anticancer and antimicrobial properties were conducted. The compounds showed promising in-vitro cytotoxic and enzyme inhibitory activity, as well as significant antimicrobial activity. Compounds 5h, 5j, and 5m demonstrated dual anticancer and antimicrobial effects, making them potential lead compounds for further modification and development of more potent and selective agents.
JOURNAL OF SAUDI CHEMICAL SOCIETY
(2022)
Article
Cell Biology
Chike Osude et al.
Summary: This study elucidated the mechanism of EGFR-TKI resistance mediated by VEGF/VEGFR in NSCLC cell lines with EGFR mutations or acquired resistance to Erlotinib. Combination treatment of Erlotinib with a VEGFR-2 inhibitor showed increased efficacy in Erlotinib-resistant cell lines. NSCLC patients with high expression of VEGFR-2 had shorter survival times. These results suggest that VEGFR-2 may play a key role in EGFR-TKI resistance and that combination treatment may be effective in NSCLC patients with EGFR mutations.
Review
Public, Environmental & Occupational Health
Yasir Osman Ali Abdalla et al.
Summary: This review summarizes the anticancer potential of natural products that have been extensively studied in the past decade, including the analysis of their molecular targets and underlying mechanisms, as well as toxicological screening on animal models. Furthermore, it provides valuable insights for researchers in developing methods and strategies for the development of anticancer drugs.
JOURNAL OF TROPICAL MEDICINE
(2022)
Article
Chemistry, Physical
Islam Zaki et al.
Summary: A new series of pyrimidine-5-carbonitriles have been synthesized and evaluated for their cytotoxic activity against HepG2 cells. Compounds 5a and 6c showed good cytotoxic activity and potent inhibition of VEGFR-2. They also induced apoptosis and cell cycle disturbance through modulation of relevant proteins. These findings suggest that these compounds have potential as anticancer agents against hepatocellular carcinoma.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Review
Biochemistry & Molecular Biology
Mohammed F. Arshad et al.
Summary: Thiazole is an important heterocycle in chemistry, possessing aromatic properties and reactive positions. Molecules with a thiazole ring can have various effects in physiological systems, making them a focus of research for medicinal chemists aiming to develop new therapeutic agents.
Review
Biochemistry & Molecular Biology
Kang Cheng et al.
Summary: Inhibiting angiogenesis, particularly through targeting VEGFR-2, is an effective strategy for tumor growth inhibition. This paper reviews the research progress of VEGFR-2 inhibitors in terms of drug development and chemical synthesis.
CURRENT MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Khaled El-Adl et al.
Summary: The study found that compounds 18, 12, 17, and 16 have strong anticancer activity against HepG2, HCT116, and MCF-7 cancer cells, with MCF-7 being the most sensitive to these new derivatives; the inhibitory activity of these compounds is comparable to classic anticancer drugs such as doxorubicin and sorafenib.
ARCHIV DER PHARMAZIE
(2021)
Review
Oncology
Hany E. Marei et al.
Summary: The p53 protein, known as the guardian of the genome, plays a critical role in preserving genomic integrity, and mutations in the TP53 gene can lead to uncontrolled cell proliferation and cancer formation. With p53 deficiency being common in human cancer, restoring p53 function may be an effective approach for cancer treatment.
CANCER CELL INTERNATIONAL
(2021)
Article
Cell Biology
Feng Ran et al.
Summary: The newly synthesized pyridine-containing compounds have shown significant inhibitory effects on vascular smooth muscle cells and regulatory effects on angiogenesis. Among them, compound 7a exhibited the most promising activity in vitro, inducing apoptosis, suppressing smooth muscle proliferation, and showing an immunomodulatory effect by reducing TNF-alpha levels by 87%.
OXIDATIVE MEDICINE AND CELLULAR LONGEVITY
(2021)
Review
Pharmacology & Pharmacy
Maria L. Formica et al.
Summary: Currently, biological drug therapy for ocular angiogenesis treatment involves administering anti-VEGF agents via the intravitreal route. In order to reduce the number of intravitreal injections required, researchers are exploring the use of nanoparticles as delivery systems for sustained drug release.
PHARMACOLOGY RESEARCH & PERSPECTIVES
(2021)
Review
Oncology
Ciara S. McNevin et al.
Summary: Studies have shown that prostate cancer patients with BRCA2/BRCA1 genetic aberrations are more likely to have worse disease and prognosis. BRCA2 mutation confers the highest risk for prostate cancer in men (8.6 fold in men & LE;65 years). While BRCA genes have garnered significant research attention, their role in the clinical assessment and treatment of prostate cancer remains complex.
Article
Biochemistry & Molecular Biology
Abdelfattah Hassan et al.
Summary: A new series of synthesized compounds showed high anticancer activity, with one dihalogenated derivative exhibiting the best cytotoxicity. Some compounds exhibited VEGFR-2 inhibitory activity similar to sorafenib, indicating potential antiproliferative effects.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
Review
Biochemistry & Molecular Biology
Punit Saraon et al.
Summary: Receptor tyrosine kinases play a significant role in cancer and have been a major class for targeted therapeutics. However, current treatments often lead to acquired resistance. New technologies are being developed to identify novel RTK small molecule therapeutics.
Article
Oncology
Alex M. Li et al.
CANCER BIOLOGY & THERAPY
(2020)
Article
Chemistry, Medicinal
Asmaa E. Kassab et al.
ARCHIV DER PHARMAZIE
(2020)
Article
Biochemistry & Molecular Biology
Dina H. Dawood et al.
BIOORGANIC CHEMISTRY
(2020)
Article
Biochemistry & Molecular Biology
Adel A. Marzouk et al.
BIOORGANIC CHEMISTRY
(2020)
Article
Biochemistry & Molecular Biology
Amal AbdelHaleem et al.
BIOORGANIC CHEMISTRY
(2020)
Article
Biochemistry & Molecular Biology
Mehlika Dilek Altintop et al.
Article
Biochemistry & Molecular Biology
Mohammed K. AbdElhameid et al.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2018)
Review
Oncology
J. Lopez et al.
BRITISH JOURNAL OF CANCER
(2015)
Article
Radiology, Nuclear Medicine & Medical Imaging
Marco Baron Toaldo et al.
MOLECULAR IMAGING AND BIOLOGY
(2015)
