Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0699790 (colon cancer)
 28,837 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Several macrocyclic diterpenes with jatrophane or lathyrane skeletons were isolated from methanol extracts of Hungarian Euphorbia species and evaluated for multidrug resistance (MDR)-reversing activity on a human colon cancer cell line. MDR-reversing activity was tested by using a standard functional assay with Rhodamine 123 as a fluorescent substrate analogue of epirubicin. In the model of combination chemotherapy, the interactions between epirubicin and certain resistance modifiers were studied in vitro. Compound 8 proved to be the most active, exhibiting a synergistic interaction. The capacity of the most effective derivative to induce apoptosis was demonstrated by flow cytometric analysis and by staining with ethidium bromide and acridine orange, using human mdrl gene-transfected mouse lymphoma cells and a human cervical adenocarcinoma cell line. The selected diterpene was able to induce moderate apoptosis in the tested cell lines. The data presented here indicate that naturally occurring Euphorbia diterpenes can be regarded as effective lead compounds for the reversal of MDR.
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PMID:New MDR modulators and apoptosis inducers from Euphorbia species. 1797 94

We report a 27-year-old female who was diagnosed with adenocarcinoma of the uterine cervix associated with Peutz- Jeghers syndrome(PJS). She had undergone 5 surgeries for intestinal intussusception and had been diagnosed with PJS. She was referred to our hospital, complaining of watery vaginal discharge, and was diagnosed with adenocarcinoma of the uterine cervix. Following neoadjuvant chemotherapy, radical hysterectomy and small intestinal polypectomy by intraoperative endoscopy were performed. Among the third-degree relatives of her family, 10 had been diagnosed with PJS; of these 10, uterine cervical adenocarcinoma occurred in 3 relatives, pancreatic cancer in 2, cholangiocellular carcinoma in 1, and colon cancer in 1. Patients with PJS are at increased risk of developing malignant tumors in various organs. A recent review of the literature from Japan revealed that the cumulative cancer risk was estimated to be 83%by the age of 70 years, with especially high incidence rates of uterine cervical adenocarcinoma, colorectal cancer, and pancreas cancer. Surveillance for malignant neoplasms in patients with PJS is recommended, focusing on the sex and age of the patients.
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PMID:[A Family with Peutz-Jeghers Syndrome Having Various Malignant Diseases]. 2813 46

Serine plays critically important roles in tumorigenesis. Homo sapiens 3-phosphoglycerate dehydrogenase (PHGDH) catalyzes the first committed step for the synthesis of glucose-derived serine via the phosphoserine pathway and has been associated with a wide variety of cancers, including breast cancer, melanoma, colon cancer, glioma, nasopharyngeal carcinoma, cervical adenocarcinoma, etc. Azacoccone E, an aza-epicoccone derivative from the culture of Aspergillus flavipes, exhibited effective inhibitory activity against PHGDH in vitro. The microscale thermophoresis (MST) method and the cellular thermal shift assay (CETSA) confirmed that azacoccone E directly bound to PHGDH. And the cell-based experiments showed that this compound was selectively toxic to PHGDH-dependent cancer cells and could cause apoptosis. Further biochemical assays revealed that it was a noncompetitive inhibitor with respect to the substrate of 3-PG and exhibited a time-dependent inhibition. Furthermore, molecular docking demonstrated that azacoccone E coordinated in an allosteric site of PHGDH with low binding energy. Therefore, azacoccone E can be considered as a possible drug candidate targeting at PHGDH for treatment of cancers.
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PMID:Azacoccone E inhibits cancer cell growth by targeting 3-phosphoglycerate dehydrogenase. 3085 33