Targets

40 pages, 2145 KiB

Open AccessReview

Pathology and Therapeutic Significance of Fibroblast Growth Factors

by Oshadi Edirisinghe, Gaëtane Ternier and Thallapuranam Krishnaswamy Suresh Kumar

Targets 2025, 3(1), 5; https://doi.org/10.3390/targets3010005 - 2 Feb 2025

Viewed by 162

The fibroblast growth factor (FGF) family includes 22 proteins in humans. Based on their mode of action, there are three families of FGFs: paracrine FGFs (FGF 1–10, 16, 17, 18, 20, and 22), intracrine FGFs (FGF 11–14), and endocrine FGFs (FGF 19, 21, and 23). FGF signaling plays critical roles in embryonic development, tissue repair, regeneration, angiogenesis, and metabolic regulation. They exert their cellular functions by binding, dimerization, and activation of transmembrane FGF receptors (FGFRs). Aberrant FGF signaling is associated with various human diseases. Thus, understanding the unique properties of FGF signaling will help to explore new therapeutic interventions against FGF-mediated pathological conditions. This review will discuss the differential expression and regulation of each FGF under normal human physiological and pathological conditions. Moreover, we will outline current therapeutics and treatment strategies that have been developed against FGF-related pathology. Full article

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30 pages, 2960 KiB

Open AccessReview

A Review of Potential Agents for Colon Cancer Interception in FAP Patients: Evidence from Preclinical Studies in APC^Min/+ Mice

by Karthikkumar Venkatachalam, Krishnendu Goswami, Venkateshwar Madka and Chinthalapally V. Rao

Targets 2025, 3(1), 4; https://doi.org/10.3390/targets3010004 - 17 Jan 2025

Viewed by 683

Abstract

Colorectal cancer (CRC) is one of the major reasons for cancer-related deaths around the world. Constitutive activation of WNT pathway, due to APC gene mutation, is the characteristic feature of most human colon tumors. Familial adenomatous polyposis (FAP) patients inherit APC mutations and pose an absolute risk of developing CRC in their lifetime. The genetically modified APC mouse models have paved the way to study various aspects of the hereditary human CRC, including biochemical, molecular, and histological aspects. Preclinical and clinical data suggest that certain dietary supplements, NSAIDs, natural products, and chemically synthesized compounds, can help in intercepting CRC incidence and progression by modulating various hallmarks of cancer. In this review, we have provided a summary of promising natural and synthetic agents that demonstrated chemopreventive efficacy against CRC in the FAP-mimicking APC^Min/+ mouse model. Full article

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15 pages, 2280 KiB

Open AccessArticle

Uterine Myometrial Distension Augments the Production of Angiogenic and Proinflammatory Factors

by Maurizio Mandalà, Matthew E. Poynter, Benjamin T. Suratt and George Osol

Targets 2025, 3(1), 3; https://doi.org/10.3390/targets3010003 - 15 Jan 2025

Viewed by 387

Abstract

We recently found that myometrial distension stimulates maternal uterine vascular remodeling, and hypothesized that this may be a previously unrecognized mechanism for inducing arterial growth during pregnancy. The aim of this study was to further characterize a recently developed surgical model in which medical-grade silicone was infused into one uterine horn of a non-gravid rat to induce acute myometrial stretch, followed by an additional, gradual distension due to the secretion of an exudate into the uterine lumen. Our objectives were to better understand the effects of stretch on the myometrium and to look for the expression of proangiogenic and proinflammatory factors that may stimulate uterine vascular remodeling. Morphometric analysis showed hypertrophy of the uterine corpus that was primarily due to axial growth since the myometrial cross-sectional area was unchanged due to a thinning of the uterine wall secondary to stretch. This finding was supported by significantly increased myometrial smooth muscle cell mitosis. There was also an increase in the concentration of myometrial elastin but not collagen. The analysis showed modest increases in neutrophils, activated and unactivated macrophages, and the proinflammatory cytokines RANTES, MIP-3α, GRO-KC, and TNFα. The most dramatic change was the extremely high level of VEGF in the exudate, which was increased >900× above circulating levels. Full article

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14 pages, 3404 KiB

Open AccessReview

Application of Machine Learning in Cell Detection

by Xinyue Liu, Xiaoyuan Wang and Ruocan Qian

Targets 2025, 3(1), 2; https://doi.org/10.3390/targets3010002 - 6 Jan 2025

Viewed by 469

Abstract

In recent years, machine learning algorithms have seen extensive application in chemical science, especially in cell detection technologies. Machine learning, a branch of artificial intelligence, is designed to automatically discover patterns in data. This review provides an overview of cell detection methods such as bright-field microscopy (BL), dark-field microscopy (DL), surface-enhanced Raman scattering (SERS), and fluorescence detection (FL). We highlight key computational models like support vector machines and convolutional neural networks that significantly enhance the precision and efficiency of automated cell detection. Relevant research applications are discussed, along with future prospects for machine learning in cell analysis. Full article

(This article belongs to the Special Issue Recent Progress in Bioimaging and Targeted Therapy)

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9 pages, 880 KiB

Open AccessArticle

Aromaticity as a Useful Descriptor of Pharmacological Activity: A Case Study of Quinoline-Based Antimalarial Agents

by Hadi Behzadi and Krzysztof K. Zborowski

Targets 2025, 3(1), 1; https://doi.org/10.3390/targets3010001 - 6 Jan 2025

Viewed by 489

Abstract

Aromatic properties of two series of quinoline derivatives were studied theoretically using the Density Functional Theory (DFT) approach. One series of compounds possesses antimalarial activity while the other does not have such properties. The B3LYP functional and the 6-311++G** basis set were employed in the study. The optimized geometries of the studied compounds were used for aromaticity level determination using several aromaticity indices, like HOMA, NICS, PDI, I₆, FLU, and PLR. It was shown that the level of aromaticity seems to be a feature that differentiates these two series of compounds. This is reasonable because it has been presented, previously in the literature, that this type of drug acts as an antimalarial drug through the formation of the π-π complex with ferriprotoporphyrin. There are two types of rings in the quinoline system, a benzene type, and a pyridine type. The aromaticity of the benzene-type ring in both series of studied compounds is similar while the aromaticity of the pyridine-type ring is lower for compounds that have antimalarial properties. It is derived on the basis of performed research that the properties of the pyridine-type ring are more important for the drug activity of studied compounds. Full article

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Targets, Volume 3, Issue 1 (March 2025) – 5 articles

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