8
views
0
recommends
+1 Recommend
0 collections
    0
    shares
      • Record: found
      • Abstract: found
      • Article: found
      Is Open Access

      2017 FDA Peptide Harvest

      review-article

      Read this article at

      Bookmark
          There is no author summary for this article yet. Authors can add summaries to their articles on ScienceOpen to make them more accessible to a non-specialist audience.

          Abstract

          2017 was an excellent year in terms of new drugs (chemical entities and biologics) approved by the FDA, with a total of 46. In turn, one of the highlights was the number of peptides (six) included in this list. Here, the six peptides are analyzed in terms of chemical structure, synthetic strategy used for their production, source, therapeutic use, and mode of action.

          Related collections

          Most cited references42

          • Record: found
          • Abstract: found
          • Article: not found

          Semaglutide versus dulaglutide once weekly in patients with type 2 diabetes (SUSTAIN 7): a randomised, open-label, phase 3b trial

          Despite common mechanisms of actions, glucagon-like peptide-1 receptor agonists differ in structure, pharmacokinetic profile, and clinical effects. This head-to-head trial compared semaglutide with dulaglutide in patients with inadequately controlled type 2 diabetes.
            Bookmark
            • Record: found
            • Abstract: found
            • Article: not found

            The ABC protein turned chloride channel whose failure causes cystic fibrosis.

            CFTR chloride channels are encoded by the gene mutated in patients with cystic fibrosis. These channels belong to the superfamily of ABC transporter ATPases. ATP-driven conformational changes, which in other ABC proteins fuel uphill substrate transport across cellular membranes, in CFTR open and close a gate to allow transmembrane flow of anions down their electrochemical gradient. New structural and biochemical information from prokaryotic ABC proteins and functional information from CFTR channels has led to a unifying mechanism explaining those ATP-driven conformational changes.
              Bookmark
              • Record: found
              • Abstract: found
              • Article: not found

              PTH increases FGF23 gene expression and mediates the high-FGF23 levels of experimental kidney failure: a bone parathyroid feedback loop.

              Parathyroid hormone (PTH) and fibroblast growth factor 23 (FGF23) target the kidney to cause a phosphaturia. FGF23 also acts on the parathyroid to decrease PTH expression, but in chronic kidney disease (CKD) there are high-serum PTH and FGF23 levels and resistance of the parathyroid to FGF23. We now report that PTH acts on bone to increase FGF23 expression and characterize the signal transduction pathway whereby PTH increases FGF23 expression. Remarkably, we show that PTH is necessary for the high-FGF23 levels of early kidney failure due to an adenine high-phosphorus diet. Parathyroidectomy before the diet totally prevented the fivefold increase in FGF23 levels in kidney failure rats. Moreover, parathyroidectomy of early kidney failure rats corrected their high-FGF23 levels. Therefore, in early kidney failure, the high-FGF23 levels are dependent on the high-PTH levels. PTH infusion for 3 days to mice with normal renal function increased serum FGF23 and calvaria FGF23 mRNA levels. To demonstrate a direct effect of PTH on FGF23, we added PTH to rat osteoblast-like UMR106 cells. PTH increased FGF23 mRNA levels (4-fold) and this effect was mimicked by a PKA activator, forskolin. PTH also decreased SOST mRNA levels (3-fold). SOST codes for sclerostin, a Wnt pathway inhibitor, which is a PTH receptor (PTH1R) target. The effect of PTH was prevented by added sclerostin. Therefore, PTH increases FGF23 expression which involves the PKA and Wnt pathways. The effect of PTH on FGF23 completes a bone-parathyroid endocrine feedback loop. Importantly, secondary hyperparathyroidism is essential for the high-FGF23 levels in early CKD.
                Bookmark

                Author and article information

                Journal
                Pharmaceuticals (Basel)
                Pharmaceuticals (Basel)
                pharmaceuticals
                Pharmaceuticals
                MDPI
                1424-8247
                07 May 2018
                June 2018
                : 11
                : 2
                : 42
                Affiliations
                [1 ]College of Health Sciences, University of KwaZulu-Natal, Durban 4000, South Africa; musamiau@ 123456gmail.com (O.A.M.); danah.shaer@ 123456gmail.com (D.A.S.)
                [2 ]School of Chemistry, University of KwaZulu-Natal, Durban 4001, South Africa
                [3 ]KRISP, College of Health Sciences, University of KwaZulu-Natal, Durban 4001, South Africa
                [4 ]CIBER-BBN, Networking Centre on Bioengineering, Biomaterials and Nanomedicine, University of Barcelona, 08028 Barcelona, Spain
                [5 ]Department of Organic Chemistry, University of Barcelona, 08028 Barcelona, Spain
                Author notes
                [* ]Correspondence: garciadelatorreb@ 123456ukzn.ac.za (B.G.d.l.T.); albericio@ 123456ukzn.ac.za (F.A.); Tel.: +27-614-009-144 (F.A.)
                [†]

                These authors contributed equally to this work.

                Author information
                https://orcid.org/0000-0003-2421-1825
                https://orcid.org/0000-0001-8488-2706
                https://orcid.org/0000-0001-8521-9172
                https://orcid.org/0000-0002-8946-0462
                Article
                pharmaceuticals-11-00042
                10.3390/ph11020042
                6027222
                29735913
                5322405f-2756-4079-9401-81f6522b6ad5
                © 2018 by the authors.

                Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license ( http://creativecommons.org/licenses/by/4.0/).

                History
                : 09 April 2018
                : 03 May 2018
                Categories
                Review

                pharmaceutical market,drugs,drug discovery,solid-phase peptide synthesis

                Comments

                Comment on this article