Anti-Cancer Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Cancer Agents) - Volume 15, Issue 10, 2015

Paraneoplastic pemphigus (PNP) is a debilitating and lethal adult and pediatric autoimmune blistering skin disease that occurs in the setting of a known or occult neoplasm. It is characterized by painful mucosal erosions that are often resistant to therapy. These clinical characteristics, in addition to positive immunohistochemistry findings make the diagnosis of PNP. The ability to recognize and diagnose PNP has dramatical Read More

Oral cancer (OC) is a common and aggressive cancer with poor survival rate. Recent research has investigated in detail the complex network of chemical, viral, and (epi)genetic factors associated with oral carcinogenesis. However, the causal factors that trigger the oral carcinogenesis process and the molecular mechanisms that underlie the tumor progression, and metastasis of OC have not been clarified. The present Read More

Healthy immune repertoire contains a fraction of immunoglobulins that do not possess exquisite antigen specificity but are able to recognize numerous unrelated antigens with similar values of the binding affinity. These antibodies are referred to as polyreactive. Besides natural polyreactive antibodies immune repertoires contain antibodies that acquire polyreactivity post-translationally, upon structural changes i Read More

Evidence is reviewed that complementary proteins and peptides form complexes with increased antigencity and/or autoimmunogenicity. Five case studies are highlighted: 1) diphtheria toxin-antitoxin (antibody), which induces immunity to the normally non-antigenic toxin, and autoimmune neuritis; 2) tryptophan peptide of myelin basic protein and muramyl dipeptide (“adjuvant peptide”), which form a complex that induces Read More

The search for effective methods for detecting cancers at very early stages is currently a top priority of cancer research. While numerous oncogenes have been identified in and associated with human cancers, the last 50 years of molecular and genetic studies have not led to a breakthrough in either the diagnosis or the treatment of cancers. Therefore, the role of oncogenes in carcinogenesis is still unclear, as i Read More

The concept according to which unique, rare and common sequences may define immunogenicity, immunopathogenicity and immunotolerance, respectively, is graphically illustrated using a melanoma-associatedantigen, Melan-A/Mart-1, as a model. The final picture is consolidated by experimentally validated data from the scientific literature and may represent a concrete prelude to effective immunotherapies exempt Read More

Rap2, a member of the GTP-binding proteins, is widely upregulated in many types of tumors. The specific effectors of Rap2 can affect multiple cancer-associated cellular processes, including cytoskeleton reorganization, proliferation, migration, and inflammation. However, the functional role of Rap2 in tumorigenesis and the interplay between different effectors remain to be fully elucidated. A more thorough understanding of Read More

Four suberoylanilide hydroxamic acid (SAHA) derivatives (N34, N4I, N4B, N24) were designed and synthesized on the basis of our previous studies on N25. Assays for anti-proliferative activity and histone deacetylase (HDAC) activity were performed against human lung cancer (SPC-A-1, LTEP-a-2, NCI-H1650) and normal lung cells (MRC-5), which were compared with those of SAHA. Molecular docking was used to theoretically co Read More

The formation of a new blood vessel is stimulated by angiogenic factors. Curcumin, which is the active ingredient of the spice plant Curcuma longa L and is used as food and traditional medicine, has shown anticancer effects against different types of cancers. We evaluated the effects of curcumin on angiogenesis/pro-angiogenic factors in a mouse model of human breast cancer. Cell viability was measured by the MTT ass Read More

Deregulation of the PI3K-Akt-mTOR pathway is unanimously pragmatic in a number of tumors. This pathway pedals proliferation, survival, translation, and coupled with tumorassociated endurance. Current efforts focus on the discovery and development of novel inhibitors of this pathway. We have discovered6-(4-phenoxyphenyl)-N-phenylquinolin-4-amine [PQQ] as a potent mTOR inhibitor with IC50 value of 64nM i Read More

4EGI-1 is the prototype of a novel class of anticancer agents targeting translation. Patented drug-like analogue 1 was synthesized and examined for inhibition of translation and cytotoxicity in cancer cells. Unexpectedly, 1 was found inactive in both assays.

Objective: To investigate the antitumor effects of a mitogen-activated protein kinase (MAPK) kinase fusion protein, TAT-OSBP-MKK6E (MAP2K6-FP), and paclitaxel as single agents and in combination against HO8910 human ovarian cancer cells. Methods: We previously synthesized a MAPK kinase-recombinant fusion protein, MAP2K6-FP, that contains three domains: a protein transduction domain TAT, a human ovarian canc Read More

Objectives: Histone deacetylase inhibitors represent a promising class of potential anticancer agents for the treatment of human malignancies. In this study, the effects of trichostatin A (TSA) on apoptosis, metastasis-associated gene expression, and activation of the Notch pathway in human pancreatic cancer cell lines were investigated. Methods: After treatment with TSA, cell viability and apoptosis were evaluated using the Read More

Under the guidance of our previous work, we synthesized 21 new structures of quinazolines (3a~3u) and evaluated their in vitro anticancer activity against A549, HCT116 and MCF-7 cell lines using the MTT method. Most compounds showed good to excellent anticancer activity. In particular, 3o (regarded as erlotinib analogues) has marked anticancer activity against A549, HCT116 and MCF-7 cell lines (IC50s: 4.26, 3.92 and 0.14 Read More

A novel triazole nucleoside analogue was discovered to exhibit potent anticancer activity in prostate cancer cells via down-regulating heat shock factor 1 (HSF1) and related heat shock proteins, along with the consequential inhibition of androgen receptor (AR) expression and transactivation, arresting the cell cycle in AR-governed phase. This triazole nucleoside therefore constitutes a novel structural paradigm and potential dr Read More