ANNIVERSARY REVIEW: Octreotide, 40 years later

Lamberts, Steven W. J.; Hofland, Leo J.

doi:10.1530/eje-19-0074

Cited by 66 publications

(36 citation statements)

References 79 publications

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“…Injectable octreotide LAR is a well-established treatment for acromegaly [74], and guidance is needed for how a daily oral formulation of octreotide should best be used in practice. Rationale for each recommendation is given in Table 3.…”

Section: Recommendationsmentioning

confidence: 99%

A Pituitary Society update to acromegaly management guidelines

et al. 2020

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Guidelines and consensus statements ensure that physicians managing acromegaly patients have access to current information on evidence-based treatments to optimize outcomes. Given significant novel recent advances in understanding acromegaly natural history and individualized therapies, the Pituitary Society invited acromegaly experts to critically review the current literature in the context of Endocrine Society guidelines and Acromegaly Consensus Group statements. This update focuses on how recent key advances affect treatment decision-making and outcomes, and also highlights the likely role of recently FDA-approved therapies as well as novel combination therapies within the treatment armamentarium.

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Section: Recommendationsmentioning

confidence: 99%

A Pituitary Society update to acromegaly management guidelines

et al. 2020

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“…The endogenous somatostatin that binds five receptors (SSTR1–SSTR5) has a very short biological half-life [ 47 ]. Therefore, many somatostatin derivatives have been developed; the most successful analogue is octreotide (OCT, Figure 2 d) by Sandoz (now Novartis) [ 48 , 49 ]. OCT is able to induce endocytosis by binding to SSTR2 with high affinity which is not affected when its N -terminus is chemically functionalized.…”

Section: Passive and Active Targetingmentioning

confidence: 99%

Forward Precision Medicine: Micelles for Active Targeting Driven by Peptides

et al. 2021

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Precision medicine is based on innovative administration methods of active principles. Drug delivery on tissue of interest allows improving the therapeutic index and reducing the side effects. Active targeting by means of drug-encapsulated micelles decorated with targeting bioactive moieties represents a new frontier. Between the bioactive moieties, peptides, for their versatility, easy synthesis and immunogenicity, can be selected to direct a drug toward a considerable number of molecular targets overexpressed on both cancer vasculature and cancer cells. Moreover, short peptide sequences can facilitate cellular intake. This review focuses on micelles achieved by self-assembling or mixing peptide-grafted surfactants or peptide-decorated amphiphilic copolymers. Nanovectors loaded with hydrophobic or hydrophilic cytotoxic drugs or with gene silence sequences and externally functionalized with natural or synthetic peptides are described based on their formulation and in vitro and in vivo behaviors.

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“…6e). Besides SST, another therapeutic relevant cyclic peptide octreotide, an analogue of somatostatin with a longer biological half-life that is often applied in cancer diagnostics 43 , was also successfully functionalized with a coumarin motif under the similar reaction conditions mentioned above (Scheme S9). The MALDI-Tof-MS data confirmed the successful functionalization with a peak at 1364 corresponding to [M+H] + (Fig.…”

Section: -Chloromethyl Acrylate Reagents For Disulfide Modificationmentioning

confidence: 99%

Chloromethyl Acryl Reagents for Simple and Site-Selective Cysteine and Disulfide Modification

Xu¹,

Kuan²,

Weil

2021

Preprint

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The generation of protein biotherapeutics with improved features compared to the synthetic drugs has received emerging interest. The conjugation of various synthetic functionalities to proteins provides access to new classes of protein conjugates, where the advantages from both the synthetic world and Nature can be combined in a synergistic fashion. Here, we reported that 2-chloromethyl acryl scaffold can serve as a simple yet versatile platform for synthesizing acrylamide or acrylate derivatives by coupling with different end-group functionalities (amino group or hydroxyl group) via a one-pot reaction. The chemical properties of the amide or ester linkage influence their inherent reactivity as bioconjugation reagents, which in turn allows synthetic customization of their features to achieve selective protein modification at cysteine or disulfide sites on demand. 2-Chloromethyl acrylamide reagents with amide linkage favors selective modification at cysteine site with high efficiency and the resultant bioconjugates exhibit superior stability compared to commonly employed maleimide-thiol conjugates. In contrast, 2-chloromethyl acrylate reagents bearing ester linkage can undergo two successive Michael reaction, allowing the selective modification of disulfides with high labelling efficiency and conjugate stability. These reagents could outperform widely applied maleimide reagents in terms of stability of the resultant bioconjugates without compromising on the ease of reagent preparation, reactivity and reaction speed. <br>

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ANNIVERSARY REVIEW: Octreotide, 40 years later

Cited by 66 publications

References 79 publications

A Pituitary Society update to acromegaly management guidelines

A Pituitary Society update to acromegaly management guidelines

Forward Precision Medicine: Micelles for Active Targeting Driven by Peptides

Chloromethyl Acryl Reagents for Simple and Site-Selective Cysteine and Disulfide Modification

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