The BASHY Platform Enables the Assembly of a Fluorescent Bortezomib–GV1001 Conjugate

Baldo, Silvia; Antunes, Pedro; Felicidade, João; Santos, Fábio M. F.; Arteaga, Jesús F.; Fernandes, Fábio; Pischel, Uwe; Pinto, Sandra N.; Góis, Pedro M. P.

doi:10.1021/acsmedchemlett.1c00615

Cited by 6 publications

(4 citation statements)

References 30 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The inhibition of FASN in an orlistat-treated mouse caused a decrease in the presence of LDs [49]. Additionally, as described in [50], the addition of oleic acid resulted in a higher content of LDs in HT-29, Hela and MCF-7 cancer cells. Importantly, these cells proved to be more resistant to anti-cancer drugs.…”

Section: Role In Cancermentioning

confidence: 66%

“…This was verified probably because the LDs hydrophobic core offers a compartment able to attract and sequester lipophilic compounds, such as lipophilic drugs [51] (Figure 3B). The entrapment of anticancer drugs makes them unable to reach their targets, which are usually specific genes and proteins in the cell nucleus, reducing their effectiveness [50]. Thus, the inhibition of LDs formation could decrease drug sequestration and, consequently, improve its efficacy.…”

Section: Role In Cancermentioning

confidence: 99%

See 1 more Smart Citation

Lipid Droplets in Cancer: From Composition and Role to Imaging and Therapeutics

et al. 2022

Self Cite

View full text Add to dashboard Cite

Cancer is the second most common cause of death worldwide, having its origin in the abnormal growth of cells. Available chemotherapeutics still present major drawbacks, usually associated with high toxicity and poor distribution, with only a small fraction of drugs reaching the tumour sites. Thus, it is urgent to develop novel therapeutic strategies. Cancer cells can reprogram their lipid metabolism to sustain uncontrolled proliferation, and, therefore, accumulate a higher amount of lipid droplets (LDs). LDs are cytoplasmic organelles that store neutral lipids and are hypothesized to sequester anti-cancer drugs, leading to reduced efficacy. Thus, the increased biogenesis of LDs in neoplastic conditions makes them suitable targets for anticancer therapy and for the development of new dyes for cancer cells imaging. In recent years, cancer nanotherapeutics offered some exciting possibilities, including improvement tumour detection and eradication. In this review we summarize LDs biogenesis, structure and composition, and highlight their role in cancer theranostics.

show abstract

Section: Role In Cancermentioning

confidence: 66%

Section: Role In Cancermentioning

confidence: 99%

Lipid Droplets in Cancer: From Composition and Role to Imaging and Therapeutics

et al. 2022

Self Cite

View full text Add to dashboard Cite

show abstract

“…Supplementation of 1% oleic acid-Albumin from bovine serum to cervical cancer HeLa cells increased the LD content by three- to fourfold, and the potency of doxorubicin against the HeLa cells was considerably reduced in an oleic acid treatment group compared to the control group (IC 50 > 1uM vs = 90 nM). The underlying mechanism of this observed effect may be that the LD hydrophobic core offers a compartment capable of attracting and sequestering lipophilic compounds and lipophilic drugs, thereby inhibiting their cytotoxic effect [ 135 , 136 ]. Likewise, reducing the content of LDs by silencing lysophosphatidylcholine acyltransferase 2 sensitized colorectal cancer HT29 cells and SW620 cells to 5-fluorouracil and oxaliplatin, and similar results were also observed in a colorectal cancer xenograft mouse model [ 81 ].…”

Section: Effects Of Activities Of Dgats On the Response Of Tumor Cell...mentioning

confidence: 99%

The role of DGAT1 and DGAT2 in regulating tumor cell growth and their potential clinical implications

Deng,

Kong,

Shen

et al. 2024

J Transl Med

View full text Add to dashboard Cite

Lipid metabolism is widely reprogrammed in tumor cells. Lipid droplet is a common organelle existing in most mammal cells, and its complex and dynamic functions in maintaining redox and metabolic balance, regulating endoplasmic reticulum stress, modulating chemoresistance, and providing essential biomolecules and ATP have been well established in tumor cells. The balance between lipid droplet formation and catabolism is critical to maintaining energy metabolism in tumor cells, while the process of energy metabolism affects various functions essential for tumor growth. The imbalance of synthesis and catabolism of fatty acids in tumor cells leads to the alteration of lipid droplet content in tumor cells. Diacylglycerol acyltransferase 1 and diacylglycerol acyltransferase 2, the enzymes that catalyze the final step of triglyceride synthesis, participate in the formation of lipid droplets in tumor cells and in the regulation of cell proliferation, migration and invasion, chemoresistance, and prognosis in tumor. Several diacylglycerol acyltransferase 1 and diacylglycerol acyltransferase 2 inhibitors have been developed over the past decade and have shown anti-tumor effects in preclinical tumor models and improvement of metabolism in clinical trials. In this review, we highlight key features of fatty acid metabolism and different paradigms of diacylglycerol acyltransferase 1 and diacylglycerol acyltransferase 2 activities on cell proliferation, migration, chemoresistance, and prognosis in tumor, with the hope that these scientific findings will have potential clinical implications.

show abstract

“…Fourteen Letters and two Viewpoints have been submitted by top researchers in the most relevant areas. Letters cover subjects such as discovery of novel tripeptides as integrin-linked kinase modulating agents (Javier Garcia-Marin, Juan J. Vaquero, Diego Rodrı́guez-Puyol, et al), peptide shuttles for brain delivery (Miquel Vila-Perelló, Vera Neves, et al), triazene hybrids for the treatment of melanoma (Maria Jesus Perry et al), SAR of oxindole–lactam hybrids as selective butyrylcholinesterase inhibitors (Marta Pineiro et al), 2-prenylated alkoxylated benzopyrans with PPARα/γ agonist activity (Nuria Cabedo, Diego Cortes, et al), triple PI3K/mTOR/PIM inhibitors (Joaquı́n Pastor et al), piperazinyl bicyclic derivatives as selective calcium channels ligands (Carmen Almansa et al), indole-containing pyrazino[2,1- b ]quinazoline-3,6-diones active against Plasmodium and trypanosomatids (Fátima Nogueira, Emı́lia Sousa, et al), evaluation of non-orthosteric interactions with potent and selective A 3 antagonists (José Brea, Hugo Gutiérrez-de-Terán, Eddy Sotelo, et al), steroid–quinoline hybrids to prevent protein aggregation (Artur M. S. Silva et al), the BASHY platform for the assembly of a fluorescent bortezomib–GV1001 conjugate (Uwe Pischel, Sandra N. Pinto, Pedro M. P. Gois, et al), pyridazin-3(2 H )-one guanidine-based derivatives as DNA binders (Carmen Terán et al), compounds from Plectranthus mutabilis Codd. leaves as modulators of P-glycoprotein activity (Milica Pešić, Patrı́cia Rijo, et al), and imidazoline- and benzamidine-based trypanosome alternative oxidase inhibitors (Christophe Dardonville et al) .…”

mentioning

confidence: 99%