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1.
Molecules ; 28(14)2023 Jul 21.
Artigo em Inglês | MEDLINE | ID: mdl-37513440

RESUMO

Matrix metalloproteinases (MMPs) are identifiable members of proteolytic enzymes that can degrade a wide range of proteins in the extracellular matrix (ECM). MMPs can be categorized into six groups based on their substrate specificity and structural differences: collagenases, gelatinases, stromelysins, matrilysins, metalloelastase, and membrane-type MMPs. MMPs have been linked to a wide variety of biological processes, such as cell transformation and carcinogenesis. Over time, MMPs have been evaluated for their role in cancer progression, migration, and metastasis. Accordingly, various MMPs have become attractive therapeutic targets for anticancer drug development. The first generations of broad-spectrum MMP inhibitors displayed effective inhibitory activities but failed in clinical trials due to poor selectivity. Thanks to the evolution of X-ray crystallography, NMR analysis, and homology modeling studies, it has been possible to characterize the active sites of various MMPs and, consequently, to develop more selective, second-generation MMP inhibitors. In this review, we summarize the computational and synthesis approaches used in the development of MMP inhibitors and their evaluation as potential anticancer agents.


Assuntos
Antineoplásicos , Neoplasias , Humanos , Inibidores de Metaloproteinases de Matriz/farmacologia , Inibidores de Metaloproteinases de Matriz/uso terapêutico , Neoplasias/metabolismo , Metaloproteinases da Matriz/metabolismo , Antineoplásicos/farmacologia , Antineoplásicos/uso terapêutico , Antineoplásicos/metabolismo , Matriz Extracelular/metabolismo
2.
Int J Clin Pract ; 2022: 9443884, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35685597

RESUMO

Background: Despite being the first-line treatment for severe or moderate acne, isotretinoin has several serious side effects that necessitate the evaluation of patients' knowledge about isotretinoin side effects and its proper use. Objective: The current study aim was to explore information needs about isotretinoin by evaluating patients' knowledge about the appropriate use of isotretinoin and its associated side effects. Methods: In addition to the sociodemographic variables, a validated online questionnaire was adopted from the literature to evaluate patients' knowledge about isotretinoin use and its potential side effects. Independent t-test and one-way analysis of variance (ANOVA) test were implemented to find the correlation between the study variables and the knowledge score. Results: The most recognized side effect of isotretinoin therapy was dryness (98.1%). The study patients showed good knowledge about isotretinoin use with a mean knowledge score of 8.1 (SD = 0.7). However, more than half of them (61.0%) mistakenly thought that isotretinoin therapy should be taken continuously for more than 6 months without stop, and some of them did not know that isotretinoin is recommended to be taken with fatty meal (24%) and sunblock (24.6%). Female gender (8.2 (SD = 0.8)) and using isotretinoin for more than 6 months (8.3 (SD = 1.2)) were significantly associated with a higher knowledge score of isotretinoin use (p=0.01), when compared with male patients (7.8 (SD = 0.7)) and less than 6-month use of isotretinoin (7.7 (SD = 0.7)). Conclusions: The lack of patients' information about the potential side effects, duration of therapy, and some instructions on isotretinoin use, such as taking the medication with fatty meal and sunblock, shed the light on the necessity to prepare leaflets, educational brochures, and educational posts via social media in order to improve patients' knowledge about isotretinoin therapy and its optimal use.


Assuntos
Acne Vulgar , Fármacos Dermatológicos , Efeitos Colaterais e Reações Adversas Relacionados a Medicamentos , Acne Vulgar/induzido quimicamente , Acne Vulgar/tratamento farmacológico , Administração Oral , Fármacos Dermatológicos/efeitos adversos , Feminino , Humanos , Isotretinoína/efeitos adversos , Jordânia , Masculino
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