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Chutima Jiarpinitnun. The investigation of multivalent effects to enhance inhibitory activity of cystic fibrosis trans-membrane conductance regulator (CFTR) inhibitor. (). King Mongkut's University of Technology North Bangkok. Central Library. : , 2017.
The investigation of multivalent effects to enhance inhibitory activity of cystic fibrosis trans-membrane conductance regulator (CFTR) inhibitor
Name: Phongsatorn Phongwarut
Organization :
Mahidol University. Faculty of Science
Name: Krittapas Jantarug
Organization :
Mahidol University. Faculty of Science
Name: Chatchai Muanprasat
Organization :
Mahidol University. Faculty of Science
Name: Chutima Jiarpinitnun
Organization :
Mahidol University. Faculty of Science
Email :
chutima.jia@mahidol.ac.th
LCSH:
Cholera
LCSH:
Vibrio cholerae
LCSH:
Adenosine monophosphate
Abstract:
Cholera is a severe diarrhea due to the intestinal infection by Gram-negative
bacterium Vibrio cholerae (V. cholerae). The infection could lead to fluid losses leading to
severe dehydration and shock. Upon the infection by V. cholera, cholera toxin (CT) is
secreted. CT can bind to target molecules on epithelial cells surface of the small intestine,
activating signaling cascade that leads to the increase of intracellular cyclic adenosine
monophosphate (cAMP). The high level of cAMP eventually causes secretion of salts and
fluid through chloride channel called cystic fibrosis transmembrane conductance regulator
or CFTR. One of the effective methods to prevent severe fluid loss is to inhibit CFTR. Here
in, we synthesized small molecules that potentially inhibit CFTR. The design of these
molecules was based on structure of known CFTR inhibitor, glycine hydrazide GlyH-101.
Previous studies suggested that the α-carbon of GlyH-101 could be substituted and still
retained the inhibitory activity. Totally of 4 compounds were synthesized and tested for its
ability to inhibit CFTR activity. Compound 13 was shown to be the most potent inhibitor with
IC50 of 0.196 μM, which is approximately 25-fold more potent than the previously reported
GlyH-101 (IC50 of 5 μM).
King Mongkut's University of Technology North Bangkok. Central Library
Address:
BANGKOK
Email:
library@kmutnb.ac.th
Created:
2017
Modified:
2562-08-21
Issued:
2019-08-21
บทความ/Article
application/pdf
BibliograpyCitation :
In Chemical Society of Thailand under the Patronage of Her Royal Hghness Princess Chulabhorn Mahidol and King Mongkut's University of Technology North Bangkok Faculty of Applied Science. Pure and Applied Chemistry International Conference (PACCON 2017) (pp.1167-1172). Bangkok : Chemical Society of Thailand under the Patronage of Her Royal Hghness Princess Chulabhorn Mahidol
eng
©copyrights King Mongkut's University of Technology North Bangkok
RightsAccess:
ใช้เวลา
0.028793 วินาที
Phongsatorn Phongwarut
| Title | Contributor | Type |
|---|---|---|
| The investigation of multivalent effects to enhance inhibitory activity of cystic fibrosis trans-membrane conductance regulator (CFTR) inhibitor
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Phongsatorn Phongwarut;Krittapas Jantarug;Chatchai Muanprasat;Chutima Jiarpinitnun | บทความ/Article | |
| Development of cystic fibrosis transmembrane conductance regulator inhibitors
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Duangporn Lohawittayanan;Phongsatorn Phongwarut;Nattaphong Akrimajirachoote;Chatchai Muanprasat;Chutima Jiarpinitnun | บทความ/Article |
Krittapas Jantarug
| Title | Contributor | Type |
|---|---|---|
| Synthetic small molecules for isolation of Gram-positive bacteria from contaminated samples
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Krittapas Jantarug;Sakol Warintaraporn;Chutima Jiarpinitnun | บทความ/Article | |
| The investigation of multivalent effects to enhance inhibitory activity of cystic fibrosis trans-membrane conductance regulator (CFTR) inhibitor
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Phongsatorn Phongwarut;Krittapas Jantarug;Chatchai Muanprasat;Chutima Jiarpinitnun | บทความ/Article | |
| Development of small molecules for the detection of Listeria monocytogenes
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Jirapan Saetang;Krittapas Jantarug;Chutima Jiarpinitnun | บทความ/Article |
Chatchai Muanprasat
| Title | Contributor | Type |
|---|---|---|
| Identification and characterization of cftr inhibitors for cholera therapy
มหาวิทยาลัยมหิดล Chatchai Muanprasat | Varanuj Chatsudthipong | วิทยานิพนธ์/Thesis |
| The investigation of multivalent effects to enhance inhibitory activity of cystic fibrosis trans-membrane conductance regulator (CFTR) inhibitor
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Phongsatorn Phongwarut;Krittapas Jantarug;Chatchai Muanprasat;Chutima Jiarpinitnun | บทความ/Article | |
| Development of cystic fibrosis transmembrane conductance regulator inhibitors
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Duangporn Lohawittayanan;Phongsatorn Phongwarut;Nattaphong Akrimajirachoote;Chatchai Muanprasat;Chutima Jiarpinitnun | บทความ/Article |
Chutima Jiarpinitnun
| Title | Contributor | Type |
|---|---|---|
| Synthetic small molecules for isolation of Gram-positive bacteria from contaminated samples
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Krittapas Jantarug;Sakol Warintaraporn;Chutima Jiarpinitnun | บทความ/Article | |
| Hybrid molecule: combination between sulfonamides and trimethoprim to inhibit growth of methicillin-resistant Staphylococcus aureus (MRSA)
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Taechin Nowwarat;Napon Nilchan;Chutima Jiarpinitnun | บทความ/Article | |
| Phenyl acrylate ester derivatives and their therapeutic potentials as anti-bacterial agents
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Angkit Kaidad;Tanawat Charoenkitchatorn;Cholpisit Kiattisewee;Torsak Luanphaisarnnont;Chutima Jiarpinitnun | บทความ/Article | |
| The investigation of multivalent effects to enhance inhibitory activity of cystic fibrosis trans-membrane conductance regulator (CFTR) inhibitor
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Phongsatorn Phongwarut;Krittapas Jantarug;Chatchai Muanprasat;Chutima Jiarpinitnun | บทความ/Article | |
| Development of small molecules for the detection of Listeria monocytogenes
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Jirapan Saetang;Krittapas Jantarug;Chutima Jiarpinitnun | บทความ/Article | |
| Development of cystic fibrosis transmembrane conductance regulator inhibitors
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Duangporn Lohawittayanan;Phongsatorn Phongwarut;Nattaphong Akrimajirachoote;Chatchai Muanprasat;Chutima Jiarpinitnun | บทความ/Article |