Zileuton, a new efficient and safe systemic anti-acne drug

Zouboulis, Christos C.

doi:10.4161/derm.1.3.8368

Cited by 62 publications

(43 citation statements)

References 27 publications

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“…Moreover, it was also shown that COX inhibitors (indomethacin, diclofenac, etc.) enhanced sebaceous lipid production (Iwata et al, 2005), whereas the lipoxygenase inhibitor Zileuton markedly decreased it (Zouboulis et al, 2005;Zouboulis, 2009). These data suggest that AA metabolites may have opposite roles in the regulation of the sebaceous lipid synthesis; i.e., lipoxygenase products seem to increase sebaceous lipid synthesis, whereas COX products seem to decrease it.…”

Section: Discussionmentioning

confidence: 78%

Protein Kinase C Isoforms Have Differential Roles in the Regulation of Human Sebocyte Biology

Géczy

Oláh

Tóth

et al. 2012

Journal of Investigative Dermatology

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Protein kinase C (PKC) isoforms have crucial roles in cutaneous signaling. Interestingly, we lack information about their involvement in human sebaceous gland biology. Therefore, in this current study, we investigated the functions of the PKC system in human immortalized SZ95 sebocytes. Using molecular biological approaches, imaging, and functional assays, we report that SZ95 sebocytes express the conventional cPKCα; the novel nPKCδ, ɛ, and η; and the atypical aPKCζ. Activation of the PKC system by phorbol 12-myristate 13-acetate (PMA) stimulated lipid synthesis (a hallmark of differentiation) and resulted in translocation and then downregulation of cPKCα and nPKCδ. In good accord with these findings, the effect of PMA was effectively abrogated by inhibitors and short interfering RNA-mediated "silencing" of cPKCα and nPKCδ. Of further importance, molecular or pharmacological inhibition of nPKCδ also prevented the lipogenic and apoptosis-promoting action of arachidonic acid. Finally, we also found that "knockdown" of the endogenous aPKCζ activity markedly increased basal lipid synthesis and apoptosis, suggesting its constitutive activity in suppressing these processes. Collectively, our findings strongly argue for the fact that certain PKCs have pivotal, isoform-specific, differential, and antagonistic roles in the regulation of human sebaceous gland-derived sebocyte biology.

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Section: Discussionmentioning

confidence: 78%

Protein Kinase C Isoforms Have Differential Roles in the Regulation of Human Sebocyte Biology

Géczy

Oláh

Tóth

et al. 2012

Journal of Investigative Dermatology

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“…However, this was attributed to the age of patients that was beyond the age for acne. Zoubolis et al [111] investigated the role of 5-Lipoxygenase inhibitor zileuton in the management of acne vulgaris. Zileuton inhibits LTB4 production, which is an inflammatory mediator and a natural ligand for PPARa.…”

Section: Acne Vulgarismentioning

confidence: 99%

Peroxisome proliferator-activated receptors (PPARs) and PPAR agonists: the ‘future’ in dermatology therapeutics?

Gupta¹,

Mahajan²,

Mehta³

et al. 2015

Arch Dermatol Res

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Peroxisome proliferator-activated receptors (PPARs) are nuclear hormone receptors and comprise three different isoforms namely PPARα, PPARγ, and PPARβ/δ with PPARβ/δ being the predominant subtype in human keratinocytes. After binding with specific ligands, PPARs regulate gene expression, cell growth and differentiation, apoptosis, inflammatory responses, and tumorogenesis. PPARs also modulate a wide variety of skin functions including keratinocyte proliferation, epidermal barrier formation, wound healing, melanocyte proliferation, and sebum production. Recent studies have shown the importance of PPARs in the pathogenesis of many dermatological disorders. Clinical trials have suggested possible role of PPAR agonists in the management of various dermatoses ranging from acne vulgaris, psoriasis, hirsutism, and lipodystrophy to cutaneous malignancies including melanoma. This article is intended to be a primer for dermatologists in their understanding of clinical relevance of PPARs and PPAR agonists in dermatology therapeutics.

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“…Other important receptors are inter alia, melanocortin-1 and -5 receptors, opiate receptors, cannabinoid 1 and 2 receptors, histamine 1 receptors and endothelial growth factor receptors. Other receptors affecting the sebocyte functions are as follows: fibroblast growth factor receptor 2, epidermal growth factor receptor, CD14, TLR2, TLR 4, TLR6 [20][21][22].…”

Section: Sebaceous Gland Vs Acnementioning

confidence: 99%

“…Zouboulis [22] highlighted the importance of classic mediators of the inflammatory reaction in acne. Leukotriene B4 is a main factor of the tissue inflammatory reaction.…”

Section: Inflammatory Reaction Cytokines Mitogensmentioning

confidence: 99%

The aetiopathogenesis of acne vulgaris – what's new?

Bergler‐Czop

2014

Intern J of Cosmetic Sci

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Synopsis Acne vulgaris is the most frequently diagnosed dermatosis in patients between 11 and 30. It is believed that it affects about 80% of persons in this age group or even, taking into account lesions of low intensity, 100% of young people. The aetiopathogenesis of acne is multifactorial. In all patients with acne, the following symptoms occur: excessive sebum production, excessive keratosis of excretory ducts and openings of sebaceous glands, development of bacterial flora and release of inflammatory mediators in the skin. Development of molecular biology, genetics and immunology contributed to a significant progress in studies on the pathogenesis of acne.

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Zileuton, a new efficient and safe systemic anti-acne drug

Cited by 62 publications

References 27 publications

Protein Kinase C Isoforms Have Differential Roles in the Regulation of Human Sebocyte Biology

Protein Kinase C Isoforms Have Differential Roles in the Regulation of Human Sebocyte Biology

Peroxisome proliferator-activated receptors (PPARs) and PPAR agonists: the ‘future’ in dermatology therapeutics?

The aetiopathogenesis of acne vulgaris – what's new?

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