The effects of benzylsulfonyl‐D‐Ser‐homoPhe‐(4‐amidino‐benzylamide), a dual plasmin and urokinase inhibitor, on facial skin barrier function in subjects with sensitive skin

Voegeli, R.; Wikstroem, P.; Campiche, Remo; Steinmetzer, Torsten; Jackson, Eileen; Gempeler, Mathias; Imfeld, D.; Rawlings, A. V.

doi:10.1111/ics.12354

Cited by 8 publications

(7 citation statements)

References 52 publications

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“…increased NMF levels. Nevertheless, it has been reported that SC barrier function, recovery and desquamation were impaired at neutral/ alkaline pH's with enhanced serine protease activity contributing to this effect, that was mitigated with acids or serine protease inhibitors [54][55][56][57][58][59]. A lower skin surface pH on volar forearm and dorsal hands of more pigmented subjects was correlated to superior SC barrier functionality.…”

Section: Tewl and Skin Surface Ph Mappingmentioning

confidence: 99%

Facial skin mapping: from single point bio‐instrumental evaluation to continuous visualization of skin hydration, barrier function, skin surface pH, and sebum in different ethnic skin types

Voegeli¹,

Gierschendorf²,

Summers

et al. 2019

Intern J of Cosmetic Sci

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Dry skin is one of the most important concerns of consumers worldwide. Despite huge efforts over several decades, the personal care industry still does not offer a perfect solution to satisfy the unmet needs of consumers for moisturising treatments in different ethnic groups. The paucity of data for the underlying cellular and biochemical problems in, and the effects of moisturisers on photodamaged facial skin may partly explain this. Mainly, single point measurements are used to understand the effects of products on skin physiology even on surrogate skin sites such as the non‐photodamaged volar forearm. Some groups have developed discontinuous facial maps of skin biophysical properties, however, in 2014 a continuous facial analysis of bio‐instrumental evaluations was developed using a heat map approach. These maps enabled a continuous visualization of features that not only revealed an unexpected complexity of facial skin but also indicated that use of surrogate skin sites for facial skin is inappropriate. We have demonstrated that remarkable gradients of skin hydration, TEWL, skin surface pH and sebum exist within short distances across the face and the gradients are distinctive among different ethnic groups. In addition, these studies have demonstrated that darkly‐pigmented individuals do not necessarily have a better skin barrier function than their less‐pigmented counterparts and that Caucasians have a lower facial skin surface pH compared with more pigmented subjects. Overall, there are no correlations between capacitance, TEWL and skin surface pH including individual topology angle values. Novel 3D camera approaches have also been used to facilitate a more precise assignment of measurement sites and visualisation. The 3D facial colour mappings illustrated precisely the local moisturising effects of a moisturising cream. There were subtle ethnic differences in efficacy that may be related to underlying skin biochemistry and/or ethnic differences in product application. A placebo‐controlled study using conductance measurements in Chinese subjects is also reported. Finally, a new whole face statistical approach has been taken to prove differences in skin parameters but also of moisturiser treatment that adds further to our understanding of the ethnic differences in skin physiology and product application. This paper reviews the background of the development and application of this methodology.

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Section: Tewl and Skin Surface Ph Mappingmentioning

confidence: 99%

Facial skin mapping: from single point bio‐instrumental evaluation to continuous visualization of skin hydration, barrier function, skin surface pH, and sebum in different ethnic skin types

Voegeli¹,

Gierschendorf²,

Summers

et al. 2019

Intern J of Cosmetic Sci

Self Cite

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“…An ideal regimen of daytime protection would include reduced exposure to blue light and prevention or minimization of free radical formation (Table 4) [22,34,[46][47][48][49][50][51]. An ideal regimen of night-time repair would include greater protection of the opsin photoreceptors against activation, collagen against degradation, mitochondria against damage, and DNA against oxidation, as well as other methods (Table 4) [11,29,[51][52][53][54][55][56][57][58][59][60][61].…”

Section: Indirect Effects Of Blue Lightmentioning

confidence: 99%

Direct and Indirect Effects of Blue Light Exposure on Skin: A Review of Published Literature

Suitthimeathegorn

Cheng

et al. 2022

Skin Pharmacol Physiol

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The growing use of electronic devices and other artificial light sources in recent decades has changed the pattern of exposure to blue light (400–500 nm). Although some progress has been made in the study of the biological effects of blue light on the skin, many questions in this field remain unexplored. The aim of this article was to review the currently available evidence on the deleterious effects of blue light on the skin, as well as the methods and strategies designed to protect from the detrimental effects of blue light. PubMed and ProQuest databases were searched in January 2022. Search results were supplemented by articles considered relevant by the authors. The results of in vitro, in vivo and clinical studies show that blue light produces direct and indirect effects on the skin. The most significant direct effects are the excessive generation of reactive oxygen and nitrogen species, and hyperpigmentation. Reactive oxygen and nitrogen species cause DNA damage and modulate the immune response. Indirect effects of blue light include disruption of the central circadian rhythm regulation via melatonin signaling and local circadian rhythm regulation via direct effects on skin cells. Antioxidants and sunscreens containing titanium dioxide, iron oxides, and zinc oxide can be used to protect against the detrimental effects of blue light as part of a strategy that combines daytime protection and night-time repair. Blue light produces a wide variety of direct and indirect effects on the skin. As exposure to blue light from artificial sources is likely to continue to increase, this area warrants further investigation.

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“…Compared to healthy skin, significantly enhanced stratum corneum protease activities have been found in lesional skin under these conditions, e.g., 60-fold increased Plm and 8-fold enhanced uPA activities . It is assumed that elevated activities of these proteases contribute to an impaired barrier function, irritation, and reduced hydration of the skin, which suggests the use of this dual Plm and uPA inhibitor in this indication …”

Section: Synthetic Active Site-directed Inhibitorsmentioning

confidence: 99%

“…153 It is assumed that elevated activities of these proteases contribute to an impaired barrier function, irritation, and reduced hydration of the skin, which suggests the use of this dual Plm and uPA inhibitor in this indication. 154 The incorporation of larger aromatic P2 and P3 residues provided a series of potent Plm inhibitors with significantly enhanced PK affinities, like CU-2010 (50, Plm K i = 2.2 nM and PK K i = 0.019 nM 155,156 ). A model of its binding mode in Plm is shown in Figure 19.…”

Section: Synthetic Active Site-directed Inhibitorsmentioning

confidence: 99%

Fibrinolysis Inhibitors: Potential Drugs for the Treatment and Prevention of Bleeding

et al. 2019

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Hyperfibrinolytic situations can lead to lifethreatening bleeding, especially during cardiac surgery. The approved antifibrinolytic agents such as tranexamic acid, εaminocaproic acid, 4-aminomethylbenzoic acid, and aprotinin were developed in the 1960s without the structural insight of their respective targets. Crystal structures of the main antifibrinolytic targets, the lysine binding sites on plasminogen's kringle domains, and plasmin's serine protease domain greatly contributed to the structure-based drug design of novel inhibitor classes. Two series of ligands targeting the lysine binding sites have been recently described, which are more potent than the most-widely used antifibrinolytic agent, tranexamic acid. Furthermore, four types of promising active site inhibitors of plasmin have been developed: tranexamic acid conjugates targeting the S1 pocket and primed sites, substrate-analogue linear homopiperidylalanine-containing 4amidinobenzylamide derivatives, macrocyclic inhibitors addressing nonprimed binding regions, and bicyclic 14-mer SFTI-1 analogues blocking both, primed and nonprimed binding sites of plasmin. Furthermore, several allosteric plasmin inhibitors based on heparin mimetics have been developed.

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The effects of benzylsulfonyl‐D‐Ser‐homoPhe‐(4‐amidino‐benzylamide), a dual plasmin and urokinase inhibitor, on facial skin barrier function in subjects with sensitive skin

Cited by 8 publications

References 52 publications

Facial skin mapping: from single point bio‐instrumental evaluation to continuous visualization of skin hydration, barrier function, skin surface pH, and sebum in different ethnic skin types

Facial skin mapping: from single point bio‐instrumental evaluation to continuous visualization of skin hydration, barrier function, skin surface pH, and sebum in different ethnic skin types

Direct and Indirect Effects of Blue Light Exposure on Skin: A Review of Published Literature

Fibrinolysis Inhibitors: Potential Drugs for the Treatment and Prevention of Bleeding

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