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  • Pegvisomant is the active ingredient in Somavert, consisting of recombinant protein component and polyethylene glycol (PEG).
    Pegvisomant is the active ingredient in Somavert, consisting of recombinant protein component and polyethylene glycol (PEG). December 8,2023.
    Acromegaly is a rare debilitating endocrine disease characterised by hypersecretion of growth hormone (GH). It is generally accepted that the clinical manifestations of acromegaly are mediated through elevations in serum IGF-I concentrations. Somavert is indicated for the treatment of patients with acromegaly who have had an inadequate response to surgery and/or radiation therapy and in whom an appropriate medical treatment with somatostatin analogues did not normalize IGF-I concentrations or was not tolerated. Pegvisomant, the active substance in Somavert, is a 40-50 kDa molecular variant of the human growth hormone (hGH) consisting of recombinant protein component and polyethylene glycol (PEG). The protein molecule (B2036) is modified by covalent addition of  polyethylene glycol (PEG) molecules resulting in a pegylated protein (B2036-PEG) with 4 and 5 PEG groups per B2036-PEG molecule. The purpose of direct pegylation of the protein was used to prolong half-life of B2036 and to reduce a potential immunogenicity. B2036-PEG showed decreased binding at the site 2 of the HGHR compared with B2036. Despite the reduced affinity for the receptor, work on the protein had shown increased potency of the pegylated form due to the prolonged circulating half-life . The pharmacodynamic studies presented showed that pegvisomant is a potent competitive and specific antagonist of hGH binding in vitro and in vivo. Reference: https://www.ema.europa.eu/en/documents/scientific-discussion/somavert-epar-scientific-discussion_en.pdf Linear Monofunctional PEGs Linear Bifunctional PEGs Linear Heterofunctional PEGs 2-arm (LYS) Polyethylene Glycol 2-arm (PTO2) Polyethylene Glycol 2-arm (GLY) Polyethylene Glycol 2-arm (Fluorene) Polyethylene glycol Y type (Y1PTO2) Polyethylene Glycol 3-arm Polyethylene Glycol 4-arm Polyethylene Glycol 6-arm (DP) Polyethylene Glycol 8-arm (TP) Polyethylene Glycol 8-arm (HG) Polyethylene Glycol 8-arm (SUC) Polyethylene Glycol
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  • An upconversion nanoplatform for simultaneous photodynamic therapy and Pt chemotherapy to combat cisplatin resistance
    An upconversion nanoplatform for simultaneous photodynamic therapy and Pt chemotherapy to combat cisplatin resistance December 4,2023.
    Dalton Trans. 2016 Aug 16;45(33):13052-60. doi: 10.1039/c6dt01404f. An upconversion nanoplatform for simultaneous photodynamic therapy and Pt chemotherapy to combat cisplatin resistance Fujin Ai 1, Tianying Sun 2, Zoufeng Xu 1, Zhigang Wang 1, Wei Kong 2, Man Wai To 3, Feng Wang 4, Guangyu Zhu 1 Abstract Platinum-based antineoplastic drugs are among the first-line chemotherapeutic agents against a variety of solid tumors, but toxic side-effects and drug resistance issues limit their clinical optimization. Novel strategies and platforms to conquer cisplatin resistance are highly desired. Herein, we assembled a multimodal nanoplatform utilizing 808 nm-excited and biocompatible core-shell-shell upconversion nanoparticles (UCNPs) [NaGdF4:Yb/Nd@NaGdF4:Yb/Er@NaGdF4] that were covalently loaded with not only photosensitizers (PSs), but also Pt(iv) prodrugs, which were rose bengal (RB) and c,c,t-[Pt(NH3)2Cl2(OCOCH2CH2NH2)2], respectively. The UCNPs had the capability to convert near infrared (NIR) light to visible light, which was further utilized by RB to generate singlet oxygen. At the same time, the nanoplatform delivered the Pt(iv) prodrug into cancer cells. Thus, this upconversion nanoplatform was able to carry out combined and simultaneous photodynamic therapy (PDT) and Pt chemotherapy. The nanoplatform was well characterized and the energy transfer efficiency was confirmed. Compared with free cisplatin or UCNPs loaded with RB only, our nanoplatform showed significantly improved cytotoxicity upon 808 nm irradiation in both cisplatin-sensitive and -resistant human ovarian cancer cells. A mechanistic study showed that the nanoparticles efficiently delivered the Pt(iv) prodrug into cancer cells, resulting in Pt-DNA damage, and that the nanoplatform generated cellular singlet oxygen to kill cancer cells. We, therefore, provide a comprehensive strategy to use UCNPs for combined Pt chemotherapy and PDT against cisplatin resistance, and our nanoplatform can also be used as a theranostic tool due to its NIR bioimaging capacity. Related products Abbreviation: mPEG-SC Name: Methoxypoly(ethylene glycol) succinimidyl carbonate For more product information, please contact us at: US Tel: 1-844-782-5734 US Tel: 1-844-QUAL-PEG CHN Tel: 400-918-9898 Email: sales@sinopeg.com
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  • A core-shell-shell nanoplatform upconverting near-infrared light at 808 nm for luminescence imaging and photodynamic therapy of cancer
    A core-shell-shell nanoplatform upconverting near-infrared light at 808 nm for luminescence imaging and photodynamic therapy of cancer November 24,2023.
    Sci Rep. 2015 Jun 2:5:10785.  doi: 10.1038/srep10785. A core-shell-shell nanoplatform upconverting near-infrared light at 808 nm for luminescence imaging and photodynamic therapy of cancer Fujin Ai 1, Qiang Ju 2, Xiaoman Zhang 3, Xian Chen 2, Feng Wang 4, Guangyu Zhu 1 Abstract Upconversion nanoparticles (UCNPs) have been extensively explored for photodynamic therapy (PDT) and imaging due to their representative large anti-Stokes shifts, deep penetration into biological tissues, narrow emission bands, and high spatial-temporal resolution.  Conventional UCNP-based PDT system, however, utilizes exitation at 980 nm, at which water has significant absorption, leading to a huge concern that the cell killing effect is from the irradiation due to overheating effect.  Here we report an efficient nanoplatform using 808-nm excited NaYbF4:Nd@NaGdF4:Yb/Er@NaGdF4 core-shell-shell nanoparticles loaded with Chlorin e6 and folic acid for simultaneous imaging and PDT.  At this wavelength, the absorption of water is minimized.  High energy transfer efficiency is achieved to generate cytotoxic singlet oxygen.  Our nanoplatform effectively kills cancer cells in concentration-, time-, and receptor-dependent manners.  More importantly, our nanoplatform is still able to efficiently generate singlet oxygen beneath 15-mm thickness of muscle tissue but 980 nm excitation cannot, showing that a higher penetration depth is achieved by our system.  These results imply that our nanoplatform has the ability to effectively kill intrinsic tumor or the center of large tumors through PDT, which significantly improves the anticancer efficacy using UCNP-based PDT system and broadens the types of tumors that could be cured. Related products Abbreviation: mPEG-SC Name: Methoxypoly(ethylene glycol) succinimidyl carbonate For more product information, please contact us at: US Tel: 1-844-782-5734 US Tel: 1-844-QUAL-PEG CHN Tel: 400-918-9898 Email: sales@sinopeg.com
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  • Site-specific PEGylation of a mutated-cysteine residue and its effect on tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL)
    Site-specific PEGylation of a mutated-cysteine residue and its effect on tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) November 13,2023.
    Biomaterials. 2013 Dec;34(36):9115-23.   doi: 10.1016/j.biomaterials.2013.08.020.   Epub 2013 Aug 24. Site-specific PEGylation of a mutated-cysteine residue and its effect on tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) Li-Qiang Pan 1, Hai-Bin Wang, Jun Lai, Ying-Chun Xu, Chen Zhang, Shu-Qing Chen Abstract Tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) is a promising antitumor agent that specifically induces apoptosis in broad-spectrum tumor cell lines, meanwhile leaving normal cells unaffected.   Unfortunately, the clinical development of TRAIL was hampered, and could be attributed to its instability, bioavailability or poor delivery.   Although N-terminal specific PEGylation provides a means to improve the pharmacokinetic and stability of TRAIL, it took a bit longer time to accomplish the PEGylation process than expected.   We therefore designed another PEGylation approach, mutated Cys-SH site-specific PEGylation, to conjugate methoxypoly(ethylene glycol) maleimide (mPEG-MAL) with TRAIL (95-281) mutant N109C.   Asn-109 was chosen as the PEGylated site for it is a potential N-linked glycosylation site.   It was shown that ~90% TRAIL mutant N109C could be PEGylated by mPEG-MAL within 40 min. And mPEG(MAL)-N109C was revealed to possess superior in vitro stability and antitumor activity than N-terminal specifically PEGylated TRAIL (114-281) (mPEG(ALD)-TRAIL(114-281)).   What's more, mPEG(MAL)-N109C exhibited more therapeutic potentials than mPEG(ALD)-TRAIL(114-281) in tumor xenograft model, benefitting from better drug delivery and bioavailability.   These results have demonstrated mutated Cys-SH specific PEGylation is an alternative to site-specifically PEGylate TRAIL efficiently and effectively other than N-terminal specific PEGylation. Keywords: Antitumor agent;   Glycosylation site;   PEG-TRAIL;   Protein delivery;   Site-specific PEGylation. Related products Abbreviation: mPEG-pALD Name: Methoxypoly(ethylene glycol) propionaldehyde Abbreviation: mPEG-MAL Name: Methoxypoly(ethylene glycol) maleimide For more product information, please contact us at: US Tel: 1-844-782-5734 US Tel: 1-844-QUAL-PEG CHN Tel: 400-918-9898 Email: sales@sinopeg.com
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  • An Injectable and Instant Self-Healing Medical Adhesive for Wound Sealing
    An Injectable and Instant Self-Healing Medical Adhesive for Wound Sealing November 9,2023.
    ACS Appl Mater Interfaces. 2020 Feb 26;12(8):9132-9140. doi: 10.1021/acsami.0c01022. Epub 2020 Feb 14. An Injectable and Instant Self-Healing Medical Adhesive for Wound Sealing Feifei Sun 1, Yazhong Bu 1, Yourong Chen 2, Fei Yang 1, Jiakuo Yu 2, Decheng Wu 1 3 Abstract Designing versatile functional medical adhesives with injectability, self-healing, and strong adhesion is of great significance to achieve desirable therapeutic effects for promoting wound sealing in healthcare. Herein, a self-healing injectable adhesive is fabricated by physical interaction of polyphenol compound tannic acid (TA) and eight-arm poly(ethylene glycol) end-capped with succinimide glutarate active ester (PEG-SG). The hydrogen bonding induced from the structural unit (-CH2-CH2-O-) of PEG and catechol hydroxyl (-OH) of TA, accompanied by ester exchange between N-hydroxysuccinimide (-NHS) and amino (-NH2) of proteins, contributes to self-healing ability and rapid strong adhesion. Notably, the PEG/TA adhesive can repeatedly adhere to rigid porcine tissues, close the coronary artery under a large incision tension, and bear a heavy load of 2 kg. By exhibiting shear-thinning and anti-swelling properties, the PEG/TA adhesive can be easily applied through single-syringe extrusion onto various wounds. The single-channel toothpaste-like feature of the adhesive ensures its storage hermetically for portable usage. Moreover, in vivo operation and histological H&E staining results indicate that the PEG/TA adhesive greatly accelerates wound healing and tissue regeneration in a rat model. With the specialty of injectability, instant self-healing, and long-lasting strong adhesion to facilitate excellent therapeutic effects, the multifunctional PEG/TA adhesive may provide a new alternative for self-rescue and surgical situations. Keywords: adhesive; poly(ethylene glycol); self-healing; single channel/injectable; wound sealing. Related products Abbreviation: mPEG-OH Name: Methoxypoly(ethylene glycol) Abbreviation: mPEG-NH2 Name: Methoxypoly(ethylene glycol) amine Abbreviation: mPEG-SH Name: Methoxypoly(ethylene glycol) thiol For more product information, please contact us at: US Tel: 1-844-782-5734 US Tel: 1-844-QUAL-PEG CHN Tel: 400-918-9898 Email: sales@sinopeg.com
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  • Tumor Microenvironment Responsive Shape-Reversal Self-Targeting Virus-Inspired Nanodrug for Imaging-Guided Near-Infrared-II Photothermal Chemotherapy
    Tumor Microenvironment Responsive Shape-Reversal Self-Targeting Virus-Inspired Nanodrug for Imaging-Guided Near-Infrared-II Photothermal Chemotherapy November 6,2023.
    ACS Nano. 2019 Nov 26;13(11):12912-12928. doi: 10.1021/acsnano.9b05425. Epub 2019 Oct 29. Tumor Microenvironment Responsive Shape-Reversal Self-Targeting Virus-Inspired Nanodrug for Imaging-Guided Near-Infrared-II Photothermal Chemotherapy Yang Li 1 2 3, Jinyan Lin 2, Peiyuan Wang 1 2 3, Qiang Luo 1 2 3, Huirong Lin 4, Yun Zhang 1 3, Zhenqing Hou 5, Jingfeng Liu 1 2 3, Xiaolong Liu 1 2 3 Abstract Tumor microenvironment responsive multimodal synergistic theranostic strategies can significantly improve the therapeutic efficacy while avoiding severe side effects. Inspired by the fact that special morphology could enhance photothermal conversion efficiency (PCE) and cellular delivery, we developed an acidic tumor microenvironment responsive shape-reversal metal-organic virus-inspired nanodrug for enhancing near-infrared (NIR)-II PCE, increasing cell adhesion, and activating tumor targeting. First, a NIR-I fluorescence probe (IR825), a chemo-drug (pemetrexed, PEM), and a rare-earth metal ion (Nd(III)) were chosen to synthesize a virus-like nanodrug via coordination-driven assembly. Then, the spike-like surface of the nanodrug was further camouflaged by an acidity-sensitive poly(ethylene glycol) "shell" to create virus-core and sphere-shell hierarchical nanoassemblies, which could efficiently prevent immune clearance and prolong systemic circulation. Interestingly, the acidic tumor microenvironment could trigger the shell detachment of nanoassemblies for shape reversal to produce a virus-like surface followed by re-exposure of PEM to synergistically amplify the cellular internalization while enhancing NIR-II PCE. By utilizing the shell-detached virus-like nanodrug core, the tumor microenvironment specific enhanced NIR-II photothermal chemotherapy can be realized under the precise guidance of fluorescence/photoacoustic imaging, thereby achieving complete tumor elimination without recurrence in a single treatment cycle. We envision that integrating the tumor microenvironment responsive ability with "sphere-to-virus" shape reversal will provide a promising strategy for biomimetic targeted cancer therapy. Keywords: NIR-II photothermal therapy; chemotherapy; shape reversal; tumor microenvironment response; virus-inspired nanodrug. Related products Abbreviation: mPEG-OH Name: Methoxypoly(ethylene glycol) For more product information, please contact us at: US Tel: 1-844-782-5734 US Tel: 1-844-QUAL-PEG CHN Tel: 400-918-9898 Email: sales@sinopeg.com
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  • Tumor Microenvironment Cascade-Responsive Nanodrug with Self-Targeting Activation and ROS Regeneration for Synergistic Oxidation-Chemotherapy
    Tumor Microenvironment Cascade-Responsive Nanodrug with Self-Targeting Activation and ROS Regeneration for Synergistic Oxidation-Chemotherapy November 2,2023.
    Nanomicro Lett. 2020 Sep 14;12(1):182. doi: 10.1007/s40820-020-00492-4. Tumor Microenvironment Cascade-Responsive Nanodrug with Self-Targeting Activation and ROS Regeneration for Synergistic Oxidation-Chemotherapy Yang Li # 1 2 3, Jinyan Lin # 2, Peiyuan Wang 1 2 3, Qiang Luo 1 2 3, Fukai Zhu 4, Yun Zhang 1 3, Zhenqing Hou 4, Xiaolong Liu 5 6 7, Jingfeng Liu 8 9 10 Abstract Carrier-free nanodrug with exceptionally high drug payload has attracted increasing attentions. Herein, we construct a pH/ROS cascade-responsive nanodrug which could achieve tumor acidity-triggered targeting activation followed by circularly amplified ROS-triggered drug release via positive-feedback loop. The di-selenide-bridged prodrug synthesized from vitamin E succinate and methotrexate (MTX) self-assembles into nanoparticles (VSeM); decorating acidity-cleavable PEG onto VSeM surface temporarily shields the targeting ability of MTX to evade immune clearance and consequently elongate circulation time. Upon reaching tumor sites, acidity-triggered detachment of PEG results in targeting recovery to enhance tumor cell uptake. Afterward, the VSeM could be dissociated in response to intracellular ROS to trigger VES/MTX release; then the released VES could produce extra ROS to accelerate the collapse of VSeM. Finally, the excessive ROS produced from VES could synergize with the released MTX to efficiently suppress tumor growth via orchestrated oxidation-chemotherapy. Our study provides a novel strategy to engineer cascade-responsive nanodrug for synergistic cancer treatment. Keywords: Circular amplification of ROS; Positive-feedback loop; Synergistic oxidation-chemotherapy; Targeting activation; Vitamin E nanodrug. Related products Abbreviation: mPEG-OH Name: Methoxypoly(ethylene glycol) For more product information, please contact us at: US Tel: 1-844-782-5734 US Tel: 1-844-QUAL-PEG CHN Tel: 400-918-9898 Email: sales@sinopeg.com
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  • PEGylation of cytochrome c at the level of lysine residues mediated by a microbial transglutaminase
    PEGylation of cytochrome c at the level of lysine residues mediated by a microbial transglutaminase October 30,2023.
    Biotechnol Lett. 2016 Jul;38(7):1121-9. doi: 10.1007/s10529-016-2083-6. Epub 2016 Mar 29. PEGylation of cytochrome c at the level of lysine residues mediated by a microbial transglutaminase Jian Qin Zhou 1, Ting He 1, Jian Wen Wang 2 Abstract Objectives: To establish a method for microbial transglutaminase (mTG)-mediated PEGylation of proteins at the level of lysine (Lys) residues. Results: Carboxybenzyl-glutaminyl-glycinyl-methoxypolyethylene glycol (CBZ-QG-mPEG) was prepared by introducing carboxybenzyl-glutaminyl-glycine (CBZ-QG) to mPEG amine. The analysis by Fourier transform infrared spectroscopy and SDS-PAGE showed that CBZ-QG-mPEG was successfully synthesized and can be recognized by mTG as an acyl donor to modify therapeutic protein, cytochrome c (cyt c). Finally, under an optimized condition (cyt c 0.5 mg/ml, CBZ-QG-mPEG 11.25 mg/ml, mTG 0.5 mg/ml, 37 °C, 2 h), the PEGylation yield reached 76.5 %. Conclusions: This is the first study regarding the PEGylation of protein at the level of Lys residues catalyzed by mTG. The novel method could be employed to immobilize active proteins and modify therapeutic proteins. Keywords: Lysine residue; Microbial transglutaminase; PEGylation; Therapeutic protein; Transglutaminase. Related products Abbreviation: mPEG-NH2 Name: Methoxypoly(ethylene glycol) amine Abbreviation: mPEG-SPA Name: Methoxypoly(ethylene glycol) succinimidyl propionate For more product information, please contact us at: US Tel: 1-844-782-5734 US Tel: 1-844-QUAL-PEG CHN Tel: 400-918-9898 Email: sales@sinopeg.com
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