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Protein disulfide isomerase: a promising target for cancer therapy.
Current knowledge of the role of PDI in cancer is reviewed and various assays for measuring the activities ofPDI are discussed, highlighting their sensitivities and usefulness for high-throughput screening.
Role of the CXCL8-CXCR1/2 Axis in Cancer and Inflammatory Diseases
A comprehensive analysis of the role of the CXCL8-CXCR1/2 axis and select genes co-expressed in this pathway in disease progression is provided and the latest progress in developing small-molecule drugs targeting this pathway is discussed.
Discovery of a Novel Orally Active Small-Molecule gp130 Inhibitor for the Treatment of Ovarian Cancer
It is shown that gp130 is an attractive drug target in ovarian cancer due to its role in promoting cancer progression via the activation of its downstream Stat3 signaling, and SC144, the first-in-class orally active small-molecule gp130 inhibitor, shows potent inhibition of gp130 ligand–triggered signaling.
Raltegravir, elvitegravir, and metoogravir: the birth of "me-too" HIV-1 integrase inhibitors
It is proposed that most of these me-too MK-0518 analogues may experience a low success rate against raltegravir-resistant HIV strains and the development of drugs with new mechanisms of inhibitory action and/or new active substituents may be a more successful route to take in theDevelopment of second- and third-generation IN inhibitors.
Opportunities in discovery and delivery of anticancer drugs targeting mitochondria and cancer cell metabolism.
This review provides an overview of the potential anticancer agents that act by targeting cancer cell metabolism and mitochondria, and also brings us face to face with the emerging opportunities in cancer therapy.
Integrin Targeted Therapeutics
This review examines and evaluates the various drugs and compounds targeting integrins and the disease states in which they are implicated and concludes that several are showing promise as they advance through preclinical development.
Curcumin analogs with altered potencies against HIV-1 integrase as probes for biochemical mechanisms of drug action.
We have previously reported the inhibitory activity of curcumin against human immunodeficiency virus type one (HIV-1) integrase. In the present study, we have synthesized and tested analogs of
Discovery of an orally active small-molecule irreversible inhibitor of protein disulfide isomerase for ovarian cancer treatment
A class of propynoic acid carbamoyl methyl amides (PACMAs) that are active against a panel of human ovarian cancer cell lines are reported that showed tumor targeting ability and significantly suppressed ovarian tumor growth without causing toxicity to normal tissues.
Copper‐transporting P‐type adenosine triphosphatase (ATP7B) as a cisplatin based chemoresistance marker in ovarian carcinoma: Comparative analysis with expression of MDR1, MRP1, MRP2, LRP and BCRP
ATP7B gene may be considered as a novel chemoresistance marker and that inhibitor(s) of ATP7B might be useful, in patients with ovarian carcinoma treated with cisplatin‐based chemotherapy.