摘要:
The invention relates to small molecules having biological and therapeutic activity. Particularly, the invention relates to small molecules having lipolytic and anti-adipogenic activity. Two examples of such molecules are 4-methyl-2-(octanoylamino) pentanoic acid and N-isopentyloctanamide. The invention further relates to methods of preventing or treating skin conditions such as cellulite using small molecules having lipolytic and anti-adipogenic activity.
摘要:
Short peptides having biological and therapeutic activity are disclosed. Specifically, the activity of the disclosed peptides is directed to reducing or protecting against mutagen-induced cellular/tissue toxicity (i.e., chemopreventive). For example, the disclosed peptides protect against skin toxicity and/or mutagenesis that occurs from ultraviolet (UV) light exposure. The disclosed peptides also block the activation of certain cell cycle regulatory proteins such as Chk2. An example of such a peptide is Ser-Leu-Tyr-Gln-Ser (SEQ ID NO: 10). The disclosed peptides are also useful for methods of reducing or protecting against cellular toxicity and mutation accumulation that would otherwise occur following mutagen exposure. One such method is drawn to applying a peptide to the skin to prevent or reduce mutagenic damage resulting from UV light (e.g., sunlight) exposure.
摘要翻译:公开了具有生物和治疗活性的短肽。 具体地,所公开的肽的活性是针对减少或防止诱变剂诱导的细胞/组织毒性(即化学预防)。 例如,所公开的肽可防止由紫外线(UV)光照射而发生的皮肤毒性和/或诱变。 所公开的肽还阻断某些细胞周期调节蛋白如Chk2的活化。 这种肽的实例是Ser-Leu-Tyr-Gln-Ser(SEQ ID NO:10)。 所公开的肽也可用于减少或防止细胞毒性和突变积累的方法,否则在诱变剂暴露后会发生。 绘制一种这样的方法以将肽施加到皮肤上以防止或减少由UV光(例如阳光)暴露引起的诱变性损伤。
摘要:
Peptides having four to fourteen residues are disclosed that possess biological activity. These peptides constitute short fragments of the peptide HB-107 (SEQ ID NO:1), which itself is a fragment of the antimicrobial protein cecropin B, and exhibit cell stimulatory, migratory and anti-inflammatory properties. As keratinocytes are especially sensitive to these effects, the disclosed peptides comprise a useful agent for the medical treatment of injury to the skin, such as from diabetic ulcers. The peptides also are effective in preventing and reversing skin surface damage resulting from various environmental insults. Importantly, the therapeutic effects of the peptides manifest at concentrations equal to or greater than those of peptide HB-107, and thus represent a less expensive, more versatile means for developing effective therapies. Methods for the production and use of these peptides are also disclosed.
摘要翻译:披露具有四至十四个残基的肽具有生物活性。 这些肽构成肽HB-107(SEQ ID NO:1)的短片段,其本身是抗微生物蛋白质天蚕素B的片段,并且具有细胞刺激性,迁移性和抗炎性质。 由于角质形成细胞对这些作用特别敏感,所公开的肽包括用于治疗皮肤损伤(例如糖尿病性溃疡)的有用试剂。 这些肽也有效地预防和逆转由各种环境污染引起的皮肤表面损伤。 重要的是,肽的治疗效果以等于或大于肽HB-107的浓度表现,因此代表开发有效疗法的较便宜,更通用的手段。 还公开了生产和使用这些肽的方法。
摘要:
A novel class of cationic peptides having antimicrobial activity is disclosed. These peptides can be encompassed by the formulas: X1X1PX2X3X2P(X2X2P)nX2X3(X5)0;(SEQ ID NO:23) X1X1PX2X3X4(X5)rPX2X3X3;(SEQ ID NO:24) X1X1X3(PW)uX3X2X5X2X2X5X2(X5)0; and(SEQ ID NO:25) X1X1X3X3X2P(X2X2P)nX2(X5)m;(SEQ ID NO:26) wherein: m is 1 to 5; n is 1 or 2; o is 2 to 5; r is 0 to 8; u is 0 or 1; X1 is Isoleucine, Leucine, Valine, Phenylalanine, Tyrosine, Tryptophan or Methionine; X2 represents Tryptophan or Phenylalanine X3 represents Arginine or Lysine; X4 represents Tryptophan or Lysine; and X5 represents Phenylalanine, Tryptophan, Arginine, Lysine, or Proline. The invention also provides a method of producing a cationic peptide variant having antimicrobial activity.
摘要:
Short biologically active tetrapeptides are disclosed that are comprised of the sequences GxxG and PxxP where G (glycine) and P (proline) are maintained and x is a variable amino acid. The peptides can be used singly or in combination to stimulate production of extracellular matrix proteins in skin. A rapid, low-cost method of producing heterogenous formulations of tetrapeptides is disclosed.
摘要:
Short peptides having biological and therapeutic activity are disclosed. Specifically, the activity of the disclosed peptides is directed to reducing or protecting against mutagen-induced cellular/tissue toxicity (i.e., chemopreventive). For example, the disclosed peptides protect against skin toxicity and/or mutagenesis that occurs from ultraviolet (UV) light exposure. The disclosed peptides also block the activation of certain cell cycle regulatory proteins such as Chk2. An example of such a peptide is Ser-Leu-Tyr-Gln-Ser (SEQ ID NO: 10). The disclosed peptides are also useful for methods of reducing or protecting against cellular toxicity and mutation accumulation that would otherwise occur following mutagen exposure. One such method is drawn to applying a peptide to the skin to prevent or reduce mutagenic damage resulting from UV light (e.g., sunlight) exposure.
摘要翻译:公开了具有生物和治疗活性的短肽。 具体地,所公开的肽的活性是针对减少或防止诱变剂诱导的细胞/组织毒性(即化学预防)。 例如,所公开的肽可防止由紫外线(UV)光照射而发生的皮肤毒性和/或诱变。 所公开的肽还阻断某些细胞周期调节蛋白如Chk2的活化。 这种肽的实例是Ser-Leu-Tyr-Gln-Ser(SEQ ID NO:10)。 所公开的肽也可用于减少或防止细胞毒性和突变积累的方法,否则在诱变剂暴露后会发生。 绘制一种这样的方法以将肽施加到皮肤上以防止或减少由UV光(例如阳光)暴露引起的诱变性损伤。
摘要:
Short biologically active tetrapeptides are disclosed that are comprised of the sequences GxxG and PxxP where G (glycine) and P (proline) are maintained and x is a variable amino acid. The peptides can be used singly or in combination to stimulate production of extracellular matrix proteins in skin. A rapid, low-cost method of producing heterogenous formulations of tetrapeptides is disclosed.
摘要:
Peptides having four to fourteen residues are disclosed that possess biological activity. These peptides constitute short fragments of the peptide HB-107 (SEQ ID NO:1), which itself is a fragment of the antimicrobial protein cecropin B, and exhibit cell stimulatory, migratory and anti-inflammatory properties. As keratinocytes are especially sensitive to these effects, the disclosed peptides comprise a useful agent for the medical treatment of injury to the skin, such as from diabetic ulcers. The peptides also are effective in preventing and reversing skin surface damage resulting from various environmental insults. Importantly, the therapeutic effects of the peptides manifest at concentrations equal to or greater than those of peptide HB-107, and thus represent a less expensive, more versatile means for developing effective therapies. Methods for the production and use of these peptides are also disclosed.
摘要翻译:披露具有四至十四个残基的肽具有生物活性。 这些肽构成肽HB-107(SEQ ID NO:1)的短片段,其本身是抗微生物蛋白质天蚕素B的片段,并且具有细胞刺激性,迁移性和抗炎性质。 由于角质形成细胞对这些作用特别敏感,所公开的肽包括用于治疗皮肤损伤(例如糖尿病性溃疡)的有用试剂。 这些肽也有效地预防和逆转由各种环境污染引起的皮肤表面损伤。 重要的是,肽的治疗效果以等于或大于肽HB-107的浓度表现,因此代表开发有效疗法的较便宜,更通用的手段。 还公开了生产和使用这些肽的方法。
摘要:
The disclosed invention provides tetrapeptides with the amino acid sequence proline-glutamine-glutamate-X (P-Q-E-X), where X can be either lysine (K) or isoleucine (I). These tetrapeptides inhibit ultraviolet light (UV)-induced expression of the pro-inflammatory cytokine interleukin-6 (IL-6) by skin epithelial cells and fibroblasts. Furthermore, the tetrapeptides repress the upregulation of matrix metalloproteinase-1 (MMP-1) by skin fibroblasts induced by either direct exposure to UV rays or treatment with media conditioned by UV-treated keratinocytes. The small size and bio-activity of the tetrapeptides render them suitable for use in therapies directed to inflammatory skin disorders and as active ingredients in skin care products.
摘要:
The invention encompasses hexapeptides consisting of alternating hydrophobic residues (B) at positions 2, 4, and 6, hydrophilic, charged residues (X) at positions 1 and 3, and a naphthylalanine (Nal), an aliphatic or aromatic residue (O) at position five, represented generally by the formula XBXBOB, which exhibit antimicrobial activity against infections caused by a variety of pathogens. These pathogens may include gram positive or negative bacteria, acid-fast bacteria such as mycobacteria, parasites, dermatophytes, or fungal pathogens. Typical fungal pathogens include Candida albicans and typical dermatophytes include Trichophyton rubrum and Trichophyton mentagrophytes. The hexapeptides of the present invention exhibit antifungal activity, antibacterial activity, desirable stability, and lack toxicity to the mammal receiving treatment.