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solid phase peptide synthesis method preparation linaclotide  (Lonza)


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    Structured Review

    Lonza solid phase peptide synthesis method preparation linaclotide
    Chemical structures of prosecretory agents. (A) Lubiprostone (Amitiza), a bicyclic fatty acid derived from prostaglandin E1 (PGE1), is the first chloride channel-targeted drug that was approved by the US FDA for treatment of constipation. (B) Elobixibat, a first-in-class ileal bile acid transporter (IBAT) inhibitor, accelerates colonic transit through enhancing delivery of bile acids to the colon, and thus increasing stool frequency as well as decreasing constipation-related symptoms in chronic idiopathic constipation (CIC) patients. (C) <t>Linaclotide,</t> a 14-amino acids peptide homologous to bacterial heat-stable enterotoxins, is a first-in-class anti-constipation drug targeting guanylyl cyclase C (GC-C) receptor on the luminal surface of GI enterocytes. Activation of GC-C receptor increases both intracellular and extracellular levels of cyclic guanosine monophosphate (cGMP). The increase in intracellular cGMP level triggers the activation of cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel activity and thereby results in salt and water secretion into the lumen of intestine. (D) Plecanatide, a 16 amino acid GC-C activator, is another synthetic GC-C agonist that activates GC-C receptors located on the luminal surface of intestinal enterocytes, leading to the elevation of intracellular cGMP and subsequent activation of CFTR chloride channel.
    Solid Phase Peptide Synthesis Method Preparation Linaclotide, supplied by Lonza, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
    https://www.bioz.com/product/solid+phase+peptide+synthesis+method+preparation+linaclotide/solid+phase+peptide+synthesis+method+preparation+linaclotide/pmc05491688-122-14-15
    Average 90 stars, based on 1 article reviews
    solid phase peptide synthesis method preparation linaclotide - by Bioz Stars, 2026-09
    90/100 stars

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    1) Product Images from "Luminally Acting Agents for Constipation Treatment: A Review Based on Literatures and Patents"

    Article Title: Luminally Acting Agents for Constipation Treatment: A Review Based on Literatures and Patents

    Journal: Frontiers in Pharmacology

    doi: 10.3389/fphar.2017.00418

    Chemical structures of prosecretory agents. (A) Lubiprostone (Amitiza), a bicyclic fatty acid derived from prostaglandin E1 (PGE1), is the first chloride channel-targeted drug that was approved by the US FDA for treatment of constipation. (B) Elobixibat, a first-in-class ileal bile acid transporter (IBAT) inhibitor, accelerates colonic transit through enhancing delivery of bile acids to the colon, and thus increasing stool frequency as well as decreasing constipation-related symptoms in chronic idiopathic constipation (CIC) patients. (C) Linaclotide, a 14-amino acids peptide homologous to bacterial heat-stable enterotoxins, is a first-in-class anti-constipation drug targeting guanylyl cyclase C (GC-C) receptor on the luminal surface of GI enterocytes. Activation of GC-C receptor increases both intracellular and extracellular levels of cyclic guanosine monophosphate (cGMP). The increase in intracellular cGMP level triggers the activation of cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel activity and thereby results in salt and water secretion into the lumen of intestine. (D) Plecanatide, a 16 amino acid GC-C activator, is another synthetic GC-C agonist that activates GC-C receptors located on the luminal surface of intestinal enterocytes, leading to the elevation of intracellular cGMP and subsequent activation of CFTR chloride channel.
    Figure Legend Snippet: Chemical structures of prosecretory agents. (A) Lubiprostone (Amitiza), a bicyclic fatty acid derived from prostaglandin E1 (PGE1), is the first chloride channel-targeted drug that was approved by the US FDA for treatment of constipation. (B) Elobixibat, a first-in-class ileal bile acid transporter (IBAT) inhibitor, accelerates colonic transit through enhancing delivery of bile acids to the colon, and thus increasing stool frequency as well as decreasing constipation-related symptoms in chronic idiopathic constipation (CIC) patients. (C) Linaclotide, a 14-amino acids peptide homologous to bacterial heat-stable enterotoxins, is a first-in-class anti-constipation drug targeting guanylyl cyclase C (GC-C) receptor on the luminal surface of GI enterocytes. Activation of GC-C receptor increases both intracellular and extracellular levels of cyclic guanosine monophosphate (cGMP). The increase in intracellular cGMP level triggers the activation of cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel activity and thereby results in salt and water secretion into the lumen of intestine. (D) Plecanatide, a 16 amino acid GC-C activator, is another synthetic GC-C agonist that activates GC-C receptors located on the luminal surface of intestinal enterocytes, leading to the elevation of intracellular cGMP and subsequent activation of CFTR chloride channel.

    Techniques Used: Derivative Assay, Activation Assay, Activity Assay

    Luminally acting agents for constipation treatment.
    Figure Legend Snippet: Luminally acting agents for constipation treatment.

    Techniques Used: Inhibition, Injection

    Proposed mechanisms of luminally acting agents for constipation treatment. The prosecretory agents linaclotide and plecanatide activate CFTR chloride channel in the enterocytes by elevating intracellular cGMP level through GC-C receptor and thereby enhancing salt and water secretion. Lubiprostone stimulates CFTR-dependent chloride secretion directly and/or via EP4 receptor pathway. Elobixibat accelerates colonic transit through enhancing delivery of bile acids to the colon, thus increasing stool frequency in CIC patients. The ORL-1 receptor antagonists naloxegol and methylnaltrexone reduce OIC through antagonizing the μ-receptor in the GI tract without reducing its central analgesic effect. Velusetrag, naronapride, prucalopride and tegaserod are selective agonists of 5-HT4 receptor and increase transepithelial secretion of Cl − and HCO 3 - .
    Figure Legend Snippet: Proposed mechanisms of luminally acting agents for constipation treatment. The prosecretory agents linaclotide and plecanatide activate CFTR chloride channel in the enterocytes by elevating intracellular cGMP level through GC-C receptor and thereby enhancing salt and water secretion. Lubiprostone stimulates CFTR-dependent chloride secretion directly and/or via EP4 receptor pathway. Elobixibat accelerates colonic transit through enhancing delivery of bile acids to the colon, thus increasing stool frequency in CIC patients. The ORL-1 receptor antagonists naloxegol and methylnaltrexone reduce OIC through antagonizing the μ-receptor in the GI tract without reducing its central analgesic effect. Velusetrag, naronapride, prucalopride and tegaserod are selective agonists of 5-HT4 receptor and increase transepithelial secretion of Cl − and HCO 3 - .

    Techniques Used:

    Related Articles

    Derivative Assay:

    Article Title: Luminally Acting Agents for Constipation Treatment: A Review Based on Literatures and Patents
    Article Snippet: among these methods mainly include solvent, coupling and decoupling methods and oxidation methods used in the process. .. LONZA AG [CH] claimed a solid phase peptide synthesis method for the preparation of linaclotide (Lonza, ). .. They also provided deprotection, oxidation and purification methods in the application.

    Activation Assay:

    Article Title: Luminally Acting Agents for Constipation Treatment: A Review Based on Literatures and Patents
    Article Snippet: among these methods mainly include solvent, coupling and decoupling methods and oxidation methods used in the process. .. LONZA AG [CH] claimed a solid phase peptide synthesis method for the preparation of linaclotide (Lonza, ). .. They also provided deprotection, oxidation and purification methods in the application.

    Activity Assay:

    Article Title: Luminally Acting Agents for Constipation Treatment: A Review Based on Literatures and Patents
    Article Snippet: among these methods mainly include solvent, coupling and decoupling methods and oxidation methods used in the process. .. LONZA AG [CH] claimed a solid phase peptide synthesis method for the preparation of linaclotide (Lonza, ). .. They also provided deprotection, oxidation and purification methods in the application.

    Inhibition:

    Article Title: Luminally Acting Agents for Constipation Treatment: A Review Based on Literatures and Patents
    Article Snippet: among these methods mainly include solvent, coupling and decoupling methods and oxidation methods used in the process. .. LONZA AG [CH] claimed a solid phase peptide synthesis method for the preparation of linaclotide (Lonza, ). .. They also provided deprotection, oxidation and purification methods in the application.

    Injection:

    Article Title: Luminally Acting Agents for Constipation Treatment: A Review Based on Literatures and Patents
    Article Snippet: among these methods mainly include solvent, coupling and decoupling methods and oxidation methods used in the process. .. LONZA AG [CH] claimed a solid phase peptide synthesis method for the preparation of linaclotide (Lonza, ). .. They also provided deprotection, oxidation and purification methods in the application.

    Purification:

    Article Title: Luminally Acting Agents for Constipation Treatment: A Review Based on Literatures and Patents
    Article Snippet: among these methods mainly include solvent, coupling and decoupling methods and oxidation methods used in the process. .. LONZA AG [CH] claimed a solid phase peptide synthesis method for the preparation of linaclotide (Lonza, ). .. They also provided deprotection, oxidation and purification methods in the application.



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    solid phase peptide synthesis method preparation linaclotide  (Lonza)
    90
    Lonza solid phase peptide synthesis method preparation linaclotide
    Chemical structures of prosecretory agents. (A) Lubiprostone (Amitiza), a bicyclic fatty acid derived from prostaglandin E1 (PGE1), is the first chloride channel-targeted drug that was approved by the US FDA for treatment of constipation. (B) Elobixibat, a first-in-class ileal bile acid transporter (IBAT) inhibitor, accelerates colonic transit through enhancing delivery of bile acids to the colon, and thus increasing stool frequency as well as decreasing constipation-related symptoms in chronic idiopathic constipation (CIC) patients. (C) <t>Linaclotide,</t> a 14-amino acids peptide homologous to bacterial heat-stable enterotoxins, is a first-in-class anti-constipation drug targeting guanylyl cyclase C (GC-C) receptor on the luminal surface of GI enterocytes. Activation of GC-C receptor increases both intracellular and extracellular levels of cyclic guanosine monophosphate (cGMP). The increase in intracellular cGMP level triggers the activation of cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel activity and thereby results in salt and water secretion into the lumen of intestine. (D) Plecanatide, a 16 amino acid GC-C activator, is another synthetic GC-C agonist that activates GC-C receptors located on the luminal surface of intestinal enterocytes, leading to the elevation of intracellular cGMP and subsequent activation of CFTR chloride channel.
    Solid Phase Peptide Synthesis Method Preparation Linaclotide, supplied by Lonza, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
    https://www.bioz.com/product/solid+phase+peptide+synthesis+method+preparation+linaclotide/solid+phase+peptide+synthesis+method+preparation+linaclotide/pmc05491688-122-14-15
    Average 90 stars, based on 1 article reviews
    solid phase peptide synthesis method preparation linaclotide - by Bioz Stars, 2026-09
    90/100 stars
    		  Buy from Supplier

    Image Search Results


    Chemical structures of prosecretory agents. (A) Lubiprostone (Amitiza), a bicyclic fatty acid derived from prostaglandin E1 (PGE1), is the first chloride channel-targeted drug that was approved by the US FDA for treatment of constipation. (B) Elobixibat, a first-in-class ileal bile acid transporter (IBAT) inhibitor, accelerates colonic transit through enhancing delivery of bile acids to the colon, and thus increasing stool frequency as well as decreasing constipation-related symptoms in chronic idiopathic constipation (CIC) patients. (C) Linaclotide, a 14-amino acids peptide homologous to bacterial heat-stable enterotoxins, is a first-in-class anti-constipation drug targeting guanylyl cyclase C (GC-C) receptor on the luminal surface of GI enterocytes. Activation of GC-C receptor increases both intracellular and extracellular levels of cyclic guanosine monophosphate (cGMP). The increase in intracellular cGMP level triggers the activation of cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel activity and thereby results in salt and water secretion into the lumen of intestine. (D) Plecanatide, a 16 amino acid GC-C activator, is another synthetic GC-C agonist that activates GC-C receptors located on the luminal surface of intestinal enterocytes, leading to the elevation of intracellular cGMP and subsequent activation of CFTR chloride channel.

    Journal: Frontiers in Pharmacology

    Article Title: Luminally Acting Agents for Constipation Treatment: A Review Based on Literatures and Patents

    doi: 10.3389/fphar.2017.00418

    Figure Lengend Snippet: Chemical structures of prosecretory agents. (A) Lubiprostone (Amitiza), a bicyclic fatty acid derived from prostaglandin E1 (PGE1), is the first chloride channel-targeted drug that was approved by the US FDA for treatment of constipation. (B) Elobixibat, a first-in-class ileal bile acid transporter (IBAT) inhibitor, accelerates colonic transit through enhancing delivery of bile acids to the colon, and thus increasing stool frequency as well as decreasing constipation-related symptoms in chronic idiopathic constipation (CIC) patients. (C) Linaclotide, a 14-amino acids peptide homologous to bacterial heat-stable enterotoxins, is a first-in-class anti-constipation drug targeting guanylyl cyclase C (GC-C) receptor on the luminal surface of GI enterocytes. Activation of GC-C receptor increases both intracellular and extracellular levels of cyclic guanosine monophosphate (cGMP). The increase in intracellular cGMP level triggers the activation of cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel activity and thereby results in salt and water secretion into the lumen of intestine. (D) Plecanatide, a 16 amino acid GC-C activator, is another synthetic GC-C agonist that activates GC-C receptors located on the luminal surface of intestinal enterocytes, leading to the elevation of intracellular cGMP and subsequent activation of CFTR chloride channel.

    Article Snippet: LONZA AG [CH] claimed a solid phase peptide synthesis method for the preparation of linaclotide (Lonza, ).

    Techniques: Derivative Assay, Activation Assay, Activity Assay

    Luminally acting agents for constipation treatment.

    Journal: Frontiers in Pharmacology

    Article Title: Luminally Acting Agents for Constipation Treatment: A Review Based on Literatures and Patents

    doi: 10.3389/fphar.2017.00418

    Figure Lengend Snippet: Luminally acting agents for constipation treatment.

    Article Snippet: LONZA AG [CH] claimed a solid phase peptide synthesis method for the preparation of linaclotide (Lonza, ).

    Techniques: Inhibition, Injection

    Proposed mechanisms of luminally acting agents for constipation treatment. The prosecretory agents linaclotide and plecanatide activate CFTR chloride channel in the enterocytes by elevating intracellular cGMP level through GC-C receptor and thereby enhancing salt and water secretion. Lubiprostone stimulates CFTR-dependent chloride secretion directly and/or via EP4 receptor pathway. Elobixibat accelerates colonic transit through enhancing delivery of bile acids to the colon, thus increasing stool frequency in CIC patients. The ORL-1 receptor antagonists naloxegol and methylnaltrexone reduce OIC through antagonizing the μ-receptor in the GI tract without reducing its central analgesic effect. Velusetrag, naronapride, prucalopride and tegaserod are selective agonists of 5-HT4 receptor and increase transepithelial secretion of Cl − and HCO 3 - .

    Journal: Frontiers in Pharmacology

    Article Title: Luminally Acting Agents for Constipation Treatment: A Review Based on Literatures and Patents

    doi: 10.3389/fphar.2017.00418

    Figure Lengend Snippet: Proposed mechanisms of luminally acting agents for constipation treatment. The prosecretory agents linaclotide and plecanatide activate CFTR chloride channel in the enterocytes by elevating intracellular cGMP level through GC-C receptor and thereby enhancing salt and water secretion. Lubiprostone stimulates CFTR-dependent chloride secretion directly and/or via EP4 receptor pathway. Elobixibat accelerates colonic transit through enhancing delivery of bile acids to the colon, thus increasing stool frequency in CIC patients. The ORL-1 receptor antagonists naloxegol and methylnaltrexone reduce OIC through antagonizing the μ-receptor in the GI tract without reducing its central analgesic effect. Velusetrag, naronapride, prucalopride and tegaserod are selective agonists of 5-HT4 receptor and increase transepithelial secretion of Cl − and HCO 3 - .

    Article Snippet: LONZA AG [CH] claimed a solid phase peptide synthesis method for the preparation of linaclotide (Lonza, ).

    Techniques: