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Kisspeptin-10, human 是一种有效的血管收缩剂和血管生成抑制剂。Kisspeptin-10, human 通过其受体 GPR54 来抑制肿瘤转移作用。Kisspeptin-10-GPR54 系统在胚胎肾脏发育中起重要作用。Kisspeptin-10/GPR54 信号通过 NFATc4 介导的 BMP2 表达来诱导成骨细胞分化。
Kisspeptin-10, human is a potent vasoconstrictor and inhibitor of angiogenesis. Kisspeptin-10, human acts as a tumor metastasis suppressor via its receptor GPR54. Kisspeptin-10-GPR54 system plays an important role in embryonic kidney development. Kisspeptin-10/GPR54 signaling induces osteoblast differentiation via NFATc4-mediated BMP2 expression[1].

Kisspeptin-10, human TFA is a potent vasoconstrictor and inhibitor of angiogenesis, it acts as a tumor metastasis suppressor via its receptor GPR54. Kisspeptin-10/GPR54 signaling induces osteoblast differentiation via NFATc4-mediated BMP2 expression. Kisspeptin-10 (KP-10) and its receptor GPR54 are key components in the regulation of GnRH secretion in humans and other mammals. Kisspeptin-10 protein binds to GPR54. Activation of Kisspeptin-10 suppresses pulmonary human melanoma and Kisspeptin-10 is a metastasis suppressor in breast cancer cells.

In vivo, intravenous infusion of kisspeptin-10 (7.5, 35, and 100 nM) induces a dose-dependent increase in LH secretion. The stimulatory effect of kisspeptin-10 (100 n nM) on LH secretion is blocked by the GnRH antagonist cetrorelix, precluding a singular action on gonadotropes. Kisspeptin-10 inhibits angiogenesis in vivo. Kp-10 inhibits tumor growth in SCID mice xenografted with human prostate cancer cells (PC-3) through inhibiting tumor angiogenesis.

Peptide H-YNWNSFGLRF-NH2 is a Research Peptide with significant interest within the field academic and medical research. Recent citations using H-YNWNSFGLRF-NH2 include the following: Acid-Resistant BODIPY Amino Acids for Peptide-Based Fluorescence Imaging of GPR54 Receptors in Pancreatic Islets L Mendive-Tapia , L Miret-Casals - Angewandte Chemie , 2023 - Wiley Online Libraryhttps://onlinelibrary.wiley.com/doi/abs/10.1002/anie.202302688 Characterizing the relationship between gonadotropin releasing hormone (GnRH), kisspeptin, and RFamide related peptide 3 (RFRP-3) neurons in the BM McGrath, ST Norman, CA Gaspardis, JL Rose - Theriogenology, 2024 - Elsevierhttps://www.sciencedirect.com/science/article/pii/S0093691X24000955

Metastin is a peptide that activates the Kisspeptin receptor. It has been shown to inhibit protein interactions, activate ligands and receptors, and act as a research tool in cell biology. Metastin is an inhibitor of the G-protein coupled receptor, KISS1R. Metastin has been shown to activate the LGR5 receptor.

Kisspeptin-10 is a peptide hormone that belongs to the family of kisspeptins. It is an intracellular regulator of calcium, which plays an important role in the regulation of cell growth and differentiation. The effect of kisspeptin-10 on cytosolic calcium levels can be used as a potential drug target for cancer treatment. It has been shown that kisspeptin-10 inhibits ovarian activity by reducing the production of luteinizing hormone (LH) and follicle stimulating hormone (FSH). Kisspeptin-10 also regulates bone metabolism by inhibiting osteoblasts and promoting osteoclasts, leading to increased bone resorption.

多肽H2N-Tyr-Asn-Trp-Asn-Ser-Phe-Gly-Leu-Arg-Phe-NH2的合成步骤：

1、合成MBHA树脂：取若干克的MBHA树脂（如初始取代度为0.5mmol/g）和1倍树脂摩尔量的Fmoc-Linker-OH加入到反应器中，加入DMF，搅拌使氨基酸完全溶解。再加入树脂2倍量的DIEPA，搅拌混合均匀。再加入树脂0.95倍量的HBTU，搅拌混合均匀。反应3-4小时后，用DMF洗涤3次。用2倍树脂体积的10%乙酸酐/DMF 进行封端30分钟。然后再用DMF洗涤3次，甲醇洗涤2次，DCM洗涤2次，再用甲醇洗涤2次。真空干燥12小时以上，得到干燥的树脂{Fmoc-Linker-MHBA Resin}，测定取代度。这里测得取代度为 0.3mmol/g。结构如下图：

2、脱Fmoc：取2.11g的上述树脂，用DCM或DMF溶胀20分钟。用DMF洗涤2遍。加3倍树脂体积的20%Pip/DMF溶液，鼓氮气30分钟，然后2倍树脂体积的DMF 洗涤5次。得到 H2N-Linker-MBHA Resin 。（此步骤脱除Fmoc基团，茚三酮检测为蓝色，Pip为哌啶）。结构图如下：

3、缩合：取1.9mmol Fmoc-Phe-OH 氨基酸，加入到上述树脂里，加适当DMF溶解氨基酸，再依次加入3.8mmol DIPEA，1.8mmol HBTU。反应30分钟后，取小样洗涤，茚三酮检测为无色。用2倍树脂体积的DMF 洗涤3次树脂。（洗涤树脂，去掉残留溶剂，为下一步反应做准备）。得到Fmoc-Phe-Linker-MBHA Resin。氨基酸：DIPEA：HBTU：树脂=3：6：2.85：1（摩尔比）。结构图如下：

4、依次循环步骤二、步骤三，依次得到

H2N-Phe-Linker-MBHA Resin

Fmoc-Arg(Pbf)-Phe-Linker-MBHA Resin

H2N-Arg(Pbf)-Phe-Linker-MBHA Resin

Fmoc-Leu-Arg(Pbf)-Phe-Linker-MBHA Resin

H2N-Leu-Arg(Pbf)-Phe-Linker-MBHA Resin

Fmoc-Gly-Leu-Arg(Pbf)-Phe-Linker-MBHA Resin

H2N-Gly-Leu-Arg(Pbf)-Phe-Linker-MBHA Resin

Fmoc-Phe-Gly-Leu-Arg(Pbf)-Phe-Linker-MBHA Resin

H2N-Phe-Gly-Leu-Arg(Pbf)-Phe-Linker-MBHA Resin

Fmoc-Ser(tBu)-Phe-Gly-Leu-Arg(Pbf)-Phe-Linker-MBHA Resin

H2N-Ser(tBu)-Phe-Gly-Leu-Arg(Pbf)-Phe-Linker-MBHA Resin

Fmoc-Asn(Trt)-Ser(tBu)-Phe-Gly-Leu-Arg(Pbf)-Phe-Linker-MBHA Resin

H2N-Asn(Trt)-Ser(tBu)-Phe-Gly-Leu-Arg(Pbf)-Phe-Linker-MBHA Resin

Fmoc-Trp(Boc)-Asn(Trt)-Ser(tBu)-Phe-Gly-Leu-Arg(Pbf)-Phe-Linker-MBHA Resin

H2N-Trp(Boc)-Asn(Trt)-Ser(tBu)-Phe-Gly-Leu-Arg(Pbf)-Phe-Linker-MBHA Resin

Fmoc-Asn(Trt)-Trp(Boc)-Asn(Trt)-Ser(tBu)-Phe-Gly-Leu-Arg(Pbf)-Phe-Linker-MBHA Resin

H2N-Asn(Trt)-Trp(Boc)-Asn(Trt)-Ser(tBu)-Phe-Gly-Leu-Arg(Pbf)-Phe-Linker-MBHA Resin

Fmoc-Tyr(tBu)-Asn(Trt)-Trp(Boc)-Asn(Trt)-Ser(tBu)-Phe-Gly-Leu-Arg(Pbf)-Phe-Linker-MBHA Resin

以上中间结构，均可在专肽生物多肽计算器-多肽结构计算器中，一键画出。

最后再经过步骤二得到 H2N-Tyr(tBu)-Asn(Trt)-Trp(Boc)-Asn(Trt)-Ser(tBu)-Phe-Gly-Leu-Arg(Pbf)-Phe-Linker-MBHA Resin，结构如下：

5、切割：6倍树脂体积的切割液（或每1g树脂加8ml左右的切割液），摇床摇晃 2小时，过滤掉树脂，用冰无水乙醚沉淀滤液，并用冰无水乙醚洗涤沉淀物3次，最后将沉淀物放真空干燥釜中，常温干燥24小试，得到粗品H2N-Tyr-Asn-Trp-Asn-Ser-Phe-Gly-Leu-Arg-Phe-NH2。结构图见产品结构图。

切割液选择：1）TFA：H2O=95%：5%

2）TFA：H2O：TIS=95%：2.5%：2.5%

3）三氟乙酸：茴香硫醚：1，2-乙二硫醇：苯酚：水=87.5%：5%：2.5%：2.5%：2.5%

（前两种适合没有容易氧化的氨基酸，例如Trp、Cys、Met。第三种适合几乎所有的序列。）

6、纯化冻干：使用液相色谱纯化，收集目标峰液体，进行冻干，获得蓬松的粉末状固体多肽。不过这时要取小样复测下纯度 是否目标纯度。

7、最后总结：

杭州专肽生物技术有限公司（ALLPEPTIDE https://www.allpeptide.com）主营定制多肽合成业务，提供各类长肽，短肽，环肽，提供各类修饰肽，如：荧光标记修饰（CY3、CY5、CY5.5、CY7、FAM、FITC、Rhodamine B、TAMRA等），功能基团修饰肽（叠氮、炔基、DBCO、DOTA、NOTA等），同位素标记肽（N15、C13），订书肽（Stapled Peptide）,脂肪酸修饰肽（Pal、Myr、Ste），磷酸化修饰肽（P-Ser、P-Thr、P-Tyr），环肽（酰胺键环肽、一对或者多对二硫键环），生物素标记肽，PEG修饰肽，甲基化修饰肽

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