AGC protein kinases: from structural mechanism of regulation to allosteric drug development for the treatment of human diseases

JM Arencibia, D Pastor-Flores, AF Bauer… - … et Biophysica Acta (BBA …, 2013 - Elsevier
The group of AGC protein kinases includes more than 60 protein kinases in the human genome,
classified into 14 families: PDK1, AKT/PKB, SGK, PKA, PKG, PKC, PKN/PRK, RSK, NDR…

High incidence of receptors for luteinizing hormone-releasing hormone (LHRH) and LHRH receptor gene expression in human prostate cancers

G Halmos, JM Arencibia, AV Schally, R Davis… - The Journal of …, 2000 - Elsevier
PURPOSE: Agonistic analogs of luteinizing hormone-releasing hormone (LHRH) are widely
used for therapy of advanced prostate cancer based upon their ability to suppress …

Expression of growth hormone-releasing hormone (GHRH) messenger ribonucleic acid and the presence of biologically active GHRH in human breast, endometrial …

Z Kahán, JM Arencibia, VJ Csernus… - The Journal of …, 1999 - academic.oup.com
GHRH is produced in a variety of extrahypothalamic tissues, including some neoplasms. We
have previously reported that GHRH antagonists can inhibit the growth of various human …

[PDF][PDF] Substrate-selective inhibition of protein kinase PDK1 by small compounds that bind to the PIF-pocket allosteric docking site

…, PM Alzari, S Neimanis, JM Arencibia, M Engel… - Chemistry & biology, 2012 - cell.com
The PIF-pocket of AGC protein kinases participates in the physiologic mechanism of
regulation by acting as a docking site for substrates and as a switch for the transduction of the …

Improving drug penetrability with iRGD leverages the therapeutic response to sorafenib and doxorubicin in hepatocellular carcinoma

…, B Kakoschky, EA Augusto, AA Ibrahim, JM Arencibia… - Cancer research, 2015 - AACR
iRGD is a derivative of the integrin-binding peptide RGD, which selectively increases the
penetrability of tumor tissue to various coadministered substances in several preclinical models…

Pharmacophore hybridization to discover novel topoisomerase II poisons with promising antiproliferative activity

…, E Minniti, M Borgogno, JM Arencibia… - Journal of medicinal …, 2018 - ACS Publications
We used a pharmacophore hybridization strategy to combine key structural elements of
merbarone and etoposide and generated new type II topoisomerase (topoII) poisons. This first …

Targeting topoisomerase II with trypthantrin derivatives: Discovery of 7-((2-(dimethylamino) ethyl) amino) indolo [2, 1-b] quinazoline-6, 12-dione as an antiproliferative …

E Catanzaro, N Betari, JM Arencibia… - European Journal of …, 2020 - Elsevier
Drugs targeting human topoisomerase II (topoII) are used in clinical practice since decades.
Nevertheless, there is an urgent need for new and safer topoII inhibitors due to the …

Novel, potent, and druglike tetrahydroquinazoline inhibitor that is highly selective for human topoisomerase II α over β

JA Ortega, JM Arencibia, E Minniti… - Journal of medicinal …, 2020 - ACS Publications
We disclose a novel class of 6-amino-tetrahydroquinazoline derivatives that inhibit human
topoisomerase II (topoII), a validated target of anticancer drugs. In contrast to topoII-targeted …

Gene expression profiling reveals overexpression of TSPAN13 in prostate cancer

JM Arencibia, S Martín… - International …, 2009 - spandidos-publications.com
Prostate cancer is one of the most frequent malignancies in the Western world. The identification
of additional molecular markers is needed to refine the diagnosis of prostate cancer …

Design, Synthesis, Dynamic Docking, Biochemical Characterization, and in Vivo Pharmacokinetics Studies of Novel Topoisomerase II Poisons with Promising …

JM Arencibia, N Brindani, S Franco-Ulloa… - Journal of Medicinal …, 2020 - ACS Publications
We previously reported a first set of hybrid topoisomerase II (topoII) poisons whose chemical
core merges key pharmacophoric elements of etoposide and merbarone, which are two well…