Renato J Aguilera

Renato J Aguilera
University of Texas at El Paso | UTEP · Department of Biological Sciences

Ph.D. in Immunology

About

106
Publications
16,265
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3,223
Citations
Citations since 2017
48 Research Items
1525 Citations
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2017201820192020202120222023050100150200250300
2017201820192020202120222023050100150200250300

Publications

Publications (106)
Article
Full-text available
Two series of novel unsymmetrical 3,5-bis(benzylidene)-4 piperidones 2a–f and 3a–e were designed as candidate antineoplastic agents. These compounds display potent cytotoxicity towards two colon cancers, as well as several oral squamous cell carcinomas. These compounds are less toxic to various non-malignant cells giving rise to large selectivity i...
Article
Full-text available
Cancer remains the second most common cause of death in the US. Due to a recurrent problem with anticancer drug resistance, there is a current need for anticancer drugs with distinct modes of action for combination drug therapy We have tested two novel piperidone compounds, named 2608 (1-dichloroacetyl − 3,5-bis(3,4-difluorobenzylidene)-4-piperidon...
Article
Skin melanoma is one of the most common types of cancer in both the United States and worldwide, and its incidence continues to grow. Primary skin melanoma can be removed surgically when feasible and if detected at an early stage. Anti-cancer drugs can be applied topically to treat skin cancer lesions and used as an adjunct to surgery to prevent th...
Article
Full-text available
In recent years, the thienopyrazole moiety has emerged as a pharmacologically active scaffold with antitumoral and kinase inhibitory activity. In this study, high-throughput screening of 2000 small molecules obtained from the ChemBridge DIVERset library revealed a unique thieno[2,3-c]pyrazole derivative (Tpz-1) with potent and selective cytotoxic e...
Article
Full-text available
In this study, we identified a novel pyrazole-based derivative (P3C) that displayed potent cytotoxicity against 27 human cancer cell lines derived from different tissue origins with 50% cytotoxic concentrations (CC50) in the low micromolar and nanomolar range, particularly in two triple-negative breast cancer (TNBC) cell lines (from 0.25 to 0.49 µM...
Article
Full-text available
A series of 3,5-bis(benzylidene)-4-piperidones 2a-u were prepared as candidate cytotoxic agents. In general, the compounds are highly toxic to human gingival carcinoma (Ca9-22), human squamous carcinoma-2 (HSC-2) and human squamous carcinoma-4 (HSC-4) neoplasms, but less so towards non-malignant human gingival fibroblast (HGF), human periodontal li...
Article
Full-text available
A novel series of 1-[3-{3,5-bis(benzylidene)-4-oxo-1-piperidino}-3-oxopropyl]-4-piperidone oximes 3a–h and related quaternary ammonium salts 4a–h were prepared as candidate antineoplastic agents. Evaluation against neoplastic Ca9-22, HSC-2 and HSC-4 cells revealed the compounds in series 3 and 4 to be potent cytotoxins with submicromolar CC50 value...
Article
Full-text available
Background Breast cancer is the most frequently diagnosed cancer in women worldwide. Pyronaridine (PND), an antimalarial drug, was shown to exert anticancer activity on seventeen different human cancer cells, seven from female breast tissue. Additionally, PND induced apoptosis via mitochondrial depolarization, alteration of cell cycle progression,...
Article
Full-text available
Background: Cancer is an ongoing worldwide health problem. Although chemotherapy remains the mainstay therapy for cancer, it is not always effective and has detrimental side effects. Here, we present piperidone compounds P3, P4, and P5 that selectively target cancer cells via protein- and stress-mediated mechanisms. Methods: We assessed typical...
Article
Recent evidences highlight the usefulness of small molecule (Histone deacetylase 4) HDAC4 inhibitors in the several preclinical paradigms. Major toxicity and mutagenicity issues associated with hydroxamate HDAC inhibitors, stimulated us to develop potent non‐hydroxamate inhibitors. In the present work a novel series of thiazolidinedione (TZD) deriv...
Article
Full-text available
At research-intensive universities in the United States, eligible faculty must generally excel in research, teaching and service in order to receive tenure. To meet these high standards, junior faculty should begin planning for a strong tenure case from their first day on the job. Here, we provide practical information, commentary and advice on how...
Article
Full-text available
A series of novel N2-acryloylhydrazides 1a–m and a related series of compounds 6a–c were prepared as potential chemostimulants. In general, these compounds are cytotoxic to human HCT 116 colon cancer cells, as well as human MCF-7 and MDA-MB-231 breast cancer cell lines. A representative compound N1-(3,4-dimethoxyphenylcarbonyl)-N2-acryloylhydrazine...
Article
e12605 Background: Triple-negative breast cancer (TNBC) is a heterogeneous subtype of breast cancer (BC) characterized by the absence of targetable receptors. Traditionally, neoadjuvant chemotherapy (NACT) has been used to downstage the tumors and increase the chance for breast-conserving surgery. The pathological complete response (pCR) has been t...
Article
Full-text available
By high-throughput chemical library screening for novel therapeutic candidates, athienopyrazole derivative was categorized with cancer-selective cytotoxic effects. This compound exhibited effective and consistent cytotoxicity against arrange of human cancer cell lines at nanomolar to low micromolar concentrations through treatments exposing times o...
Conference Paper
p>Triple-negative breast cancer (TNBC) represents approximately 15-20% of all breast cancer types. It is more common among African American (AA) and Hispanic-Latina (HL) women and has more aggressive course. The biology of TNBC in HL women has been poorly characterized, but some data suggest that molecular drivers of breast cancer might be differen...
Article
Prostate cancer is a common malignancy in men worldwide. In the initial treatment, ADT has been used as the cornerstone, but unfortunately, mainstream patients transition to the refractory state of prostate cancer, i.e., CRPC. Thus, newer therapeutics are required for the treatment of patients un or less responsive to ADT. Epigenetic aberrations, n...
Preprint
At research-intensive universities in the United States, eligible faculty must generally excel in research, teaching and service in order to receive tenure. To meet these high standards, junior faculty should begin planning for a strong tenure case from their first day on the job. Here, we provide practical information, commentary and advice on how...
Article
In this study, we synthesized 22 compounds in a series with various substitution on imidazo[2,1‐ b ][1,3,4]thiadiazoles. The potential cytotoxic activity of these compounds investigated in leukemia cell lines by Differential Nuclear Staining (DNS). Our results identify two compounds 2‐(4‐methoxybenzyl)‐6‐(2‐oxo‐2H‐chromen‐3‐yl)imidazo[2,1‐b][1,3,4]...
Article
Full-text available
Triple-negative breast cancer (TNBC) represents 15%-20% of all breast cancer types. It is more common among African American (AA) and Hispanic-Latina (HL) women. The biology of TNBC in HL women has been poorly characterized, but some data suggest that the molecular drivers of breast cancer might differ. There are no clinical tools to aid medical on...
Conference Paper
Among the main challenges for the treatment of breast cancers is disease spread which is often coupled with resistance to chemotherapy. Furthermore, patients with late stage breast cancer go through first- and second-line therapies before they are candidates for new and/or experimental therapies. At such late stages, tumors that might have responde...
Article
Cancer is a heterogeneous disease, and its treatment requires the identification of new ways to thwart tumor cells. Amongst such emerging targets are glucose transporters (GLUTs, SLC2 family), which are overexpressed by almost all types of cancer cells; their inhibition provides a strategy to disrupt tumor metabolism selectively, leading to antitum...
Article
Cancer cells increase their glucose uptake and glycolytic activity to meet the high energy requirements of proliferation. Glucose transporters (GLUTs), which facilitate the transport of glucose and related hexoses across the cell membrane, play a vital role in tumor cell survival and are overexpressed in various cancers. GLUT1, the most overexpress...
Article
Epigenetics plays a fundamental role in cancer progression, and developing agents that regulate epigenetics is crucial for cancer management. Among Class I and Class II HDACs, HDAC8 is one of the essential epigenetic players in cancer progression. Therefore, we designed, synthesized, purified, and structurally characterized novel compounds containi...
Article
Since cancer cells have different mitochondrial bioenergetics requirements than non-cancerous cells, therapeutic inhibition of its mitochondrial functionality continues to be an important target for anticancer drug discovery. In this study, a series of acylhydroquinones with different acyl-chain length, and their chlorinated derivatives, in the aro...
Article
Full-text available
Promoting diversity and inclusiveness in the STEM academic workforce remains a key challenge and national priority. Scientific societies can play a significant role in this process through the creation and implementation of programs to foster STEM academic workforce diversification, and by providing mentoring and skills development training that em...
Article
Full-text available
Aim: The purpose of this study was to determine the level of adherence to adjuvant aromatase inhibitor (AI) therapy and factors associated with non-adherence among Hispanic/Latino women with hormonal receptor-positive breast cancer (BC) treated at an academic center at the American-Mexican border city of El Paso, TX. Patients and methods: Instit...
Article
Full-text available
AKT1 is emerging as a useful target for treating cancer. Herein, we discovered a new set of hits that inhibit the AKT1, as shown by in vitro binding and cell line studies, using a newly designed virtual screening protocol that combines structure-based pharmacophore and docking screens. Taking together biological data demonstrated reasonable success...
Article
Full-text available
In the last 15 years, pyridazinone derivatives have acquired extensive attention due to their widespread biological activities and pharmacological applications. Pyridazinones are well known for their anti-microbial, anti-viral, anti-inflammatory, anti-cancer, and cardiovascular activities, among others. In this study, we evaluated the anti-cancer a...
Preprint
Full-text available
Promoting diversity and inclusiveness in the STEM academic workforce remains a key challenge and national priority. Scientific societies can play a significant role in this process through the creation and implementation of programs to foster STEM academic workforce diversification, and by providing mentoring and skills development training that em...
Article
Full-text available
Breast cancer is the most frequently diagnosed cancer among women worldwide. Here, recombinant human lactoferrin (rhLf) expressed in Pichia pastoris was tested for its potential cytotoxic activity on a panel of six human breast cancer cell lines. The rhLf cytotoxic effect was determined via a live-cell HTS imaging assay. Also, confocal microscopy a...
Article
Full-text available
1,4‐Triazolyl combretacoumarins have been prepared by linking the trimethoxyarene unit of combretastatin A4 with coumarins, via a 1,2,3‐triazole. For this, 4‐azidocoumarins were accessed by a sequential two‐step, one‐pot reaction of 4‐hydroxycoumarins with (benzotriazol‐1‐yloxy)tris(dimethylamino)phosphonium hexafluorophosphate (BOP), followed by r...
Article
Full-text available
Background: Substantial evidence supports the use of inexpensive β-AR antagonists (beta blockers) against a variety of cancers, and the β-AR antagonist propranolol was recently approved by the European Medicines Agency for the treatment of soft tissue sarcomas. Prospective and retrospective data published by our group and others suggest that non-s...
Article
One biofabrication process that has gained tremendous momentum in the field of tissue engineering and regenerative medicine is cell-printing or most commonly bioprinting. We have shown that thermal inkjet bioprinted human microvascular endothelial cells were recruited or otherwise involved in the formation of microvasculature to form graft-host ana...
Article
Full-text available
Oxidative stress plays a critical role in numerous diseases. Therefore, the pursuit of compounds with antioxidant activity remains critical. Green barley young leaves aqueous extract (GB) was tested for its capacity to ameliorate cellular oxidative stress, and its potential cytoprotective mechanism was partially elucidated. Through Folin-Ciocalteau...
Article
Full-text available
Correction for ‘A new family of fullerene derivatives: fullerene–curcumin conjugates for biological and photovoltaic applications’ by Edison Castro et al., RSC Adv. , 2018, 8 , 41692–41698.
Preprint
Full-text available
AKT1 is emerging as a useful target for treating cancer. Herein, we discovered a new set of ligands that inhibit the AKT1, as shown by in vitro binding and cell line studies, using a newly designed virtual screening protocol that combines structure-based pharmacophore and docking screens. Taking together with the biological data, the combination of...
Preprint
Full-text available
AKT1 is emerging as a useful target for treating cancer. Herein, we discovered a new set of ligands that inhibit the AKT1, as shown by in vitro binding and cell line studies, using a newly designed virtual screening protocol that combines structure-based pharmacophore and docking screens. Taking together with the biological data, the combination of...
Article
Full-text available
The synthesis and characterization of a family of [60]fullerocurcuminoids obtained via Bingel reactions is reported. The new C 60 derivatives include curcumin and curcuminoids with a variety of end groups. Preliminary biological experiments show the potential activity of the compound containing a curcumin addend, which exhibits moderate anti-HIV-1...
Article
Full-text available
The potent antimalarial drug pyronaridine (PND) was tested for its potential as an anticancer drug. After exposing cancerous (17) and non-cancerous (2) cells to PND for 72 hr, PND was found to exhibit consistent and potent cytotoxic activity at low micromolar (μM) concentrations that ranged from 1.6 μM to 9.4 μM. Moreover, PND exerted a significant...
Data
Cell cycle analysis of synchronized MDA-MB-231 and HL-60 cell lines treated with PND. (DOCX)
Data
Cell cycle analysis of MCF-10A cells treated with high and low concentrations of PND. (DOCX)
Article
Purpose: Previously, compounds containing a piperidone structure have been shown to be highly cytotoxic to cancer cells. Recently, we found that the piperidone compound P2 exhibits a potent anti-neoplastic activity against human breast cancer-derived cells. Here, we aimed to evaluate two piperidone compounds, P1 and P2, for their potential anti-ne...
Data
Deoxyribonuclease II (DNase II) is also known as acid deoxyribonuclease because it has optimal activity at the low pH environment of lysosomes where it is typically found in higher eukaryotes. Interestingly, DNase II has also been identified in a few genera of bacteria and is believed to have arisen via horizontal transfer. Here, we demonstrate tha...
Article
Full-text available
Deoxyribonuclease II (DNase II) is also known as acid deoxyribonuclease because it has optimal activity at the low pH environment of lysosomes where it is typically found in higher eukaryotes. Interestingly, DNase II has also been identified in a few genera of bacteria and is believed to have arisen via horizontal transfer. Here, we demonstrate tha...
Article
Full-text available
Previous studies suggest beta-adrenergic receptor (β-AR) antagonists (β-blockers) decrease breast cancer progression, tumor metastasis, and patient mortality; however the mechanism for this is unknown. Immunohistochemical analysis of normal and malignant breast tissue revealed overexpression of β1-AR and β3-AR in breast cancer. A retrospective cros...
Article
Full-text available
Background: A novel series of structurally divergent 1,5-diaryl-3-oxo-1,4-pentadiene analogues 1-10 displayed marked cytotoxic potencies towards a number of human leukemia/lymphoma cells. Objective: To identify novel selective cytotoxic compounds that induce apoptosis. Methods: The Differential Nuclear Staining (DNS) screening protocol was uti...
Article
Full-text available
In the present pre-clinical study, a series of 1-[3-(2-methoxyethylthio)-propionyl]-3,5-bis(benzylidene)-4 piperidones and structurally-related compounds were observed to be cytotoxic in vitro to three human leukemia cell lines, namely Nalm-6, CEM and Jurkat. The 50% cytotoxic concentration (CC50) values of the three cell lines ranged between 0.9-1...
Article
Full-text available
Purpose: According to the World Health Organization (WHO), breast cancer is the most common cancer affecting women worldwide. In the USA ~12.3 % of all women are expected to be diagnosed with various types of breast cancer, exhibiting varying degrees of therapeutic response rates. Therefore, the identification of novel anti-breast cancer drugs is...
Article
Full-text available
Simple glycoside surfactants represent a class of chemicals that are produced from renewable raw materials. They are considered to be environmentally safe and, therefore, are increasingly used as pharmaceuticals, detergents, and personal care products. Although they display low to moderate toxicity in cells in culture, the underlying mechanisms of...
Article
Full-text available
Long-term exposure to arsenic has been linked to cancer in different organs and tissues, including skin. Here, non-malignant human keratinocytes (HaCaT) were exposed to arsenic and its effects on microRNAs (miRNAs; miR) expression were analyzed via miRCURY LNA array analyses. A total of 30 miRNAs were found differentially expressed in arsenic-treat...
Article
Full-text available
Hepatocellular carcinoma (HCC) is a worldwide prevalent cancer with an exremely poor prognosis. Detection of serum α-fetoprotein (AFP) and liver imaging techniques are the conventional methods used clinically for the identification of this malignancy. However, these techniques are not reliable for early diagnosis, and particularly the sensitivity a...
Article
Full-text available
Hepatocellular carcinoma (HCC) is a worldwide prevalent cancer with an exremely poor prognosis. Detection of serum α-fetoprotein (AFP) and liver imaging techniques are the conventional methods used clinically for the identification of this malignancy. However, these techniques are not reliable for early diagnosis, and particularly the sensitivity a...
Article
Full-text available
Drosophila melanogaster flies mount an impressive immune response to a variety of pathogens with an efficient system comprised of both humoral and cellular responses. The fat body is the main producer of the anti-microbial peptides (AMPs) with anti-pathogen activity. During bacterial infection, an array of secreted peptidases, proteases and other e...
Article
Full-text available
Current reports indicated that the gender origin of cells is important in all facets of experimental biology. To explore this matter using an anticancer high throughput screening platform, seven male- and seven female-derived human cell lines, six from cancer patients in each group, were exposed to 81 novel cytotoxins. In this screen, the findings...
Article
Full-text available
Ruthenium-based compounds have intriguing anti-cancer properties, and some of these novel compounds are currently in clinical trials. To continue the development of new metal-based drug combinations, we coupled ruthenium (Ru) with the azole compounds ketoconazole (KTZ) and clotrimazole (CTZ), which are well-known antifungal agents that also display...
Article
Full-text available
Green barley extract (GB) was investigated for possible anti-cancer activity by examining its anti-proliferative and pro-apoptotic properties on human leukemia/lymphoma cell lines. Our results indicate that GB exhibits selective anti-proliferative activity on a panel of leukemia/lymphoma cells in comparison to non-cancerous cells. Specifically, GB...
Article
We are interested in the development of surfactants derived from hemicellulosic biomass, as they are potential components in pharmaceuticals, personal care products, and other detergents. Such surfactants should exhibit low toxicity in mammalian cells. In this study we synthesized a series of alkyl or fluoroalkyl β-xylopyranosides from azides and a...
Conference Paper
The use of plants for medical purposes is an ancient practice and this knowledge has been transferred by oral communication and/or by imitation among various cultures for generations. Green barley (GB) has been proposed to contain an anticancer curative activity and has been actively promoted by producers of natural herbal supplements with little,...
Conference Paper
Full-text available
Larrea tridentata also known as Creosote is a North American shrub, whose leave extracts are proposed to contain anti-cancer properties. The main metabolite in this plant is the nordihydroguaiaretic acid (NDGA) has been shown to have anti-neoplastic, anti-viral and anti-inflammatory properties. NDGA is a strong anti-oxidant that can scavenge or inh...
Article
Full-text available
Academic institutions across the country have long recognized the value of racial integration and have consistently opposed legal challenges to affirmative action policies. Despite these efforts, the percentage of underrepresented minorities in academic positions has not increased in proportion to their representation in society. Recruitment of und...
Article
Little is known about the fate, transport, and bioavailability of CeO(2) nanoparticles (NPs) in soil. Moreover, there are no reports on the effect of surface coating upon NPs uptake by plants. In this study, Zea mays plants were grown for one month in unenriched and organic soils treated with coated and uncoated CeO(2) NPs. In addition, plants were...
Article
The manufacture and multiple uses of zinc oxide (ZnO) nanoparticles (NPs) will represent a possible source of soil contamination. Little is known about how these NPs transport in soil and plants. In this research, the transport of Zn/ZnO NPs in sandy loam soil and the uptake by corn plants (Zea mays) was investigated. Results showed that ZnO NPs ex...
Article
Alkyl β-d-xylopyranosides are highly surface active, biodegradable surfactants that can be prepared from hemicelluloses and are of interest for use as pharmaceuticals, detergents, agrochemicals, and personal care products. To gain further insights into their structure-property and structure-activity relationships, the present study synthesized a se...