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Energetics of Vanilloid Activation of TRPV1 Ion Channel
Energetics of Vanilloid Activation of TRPV1 Ion Channel
Energetics of Vanilloid Activation of TRPV1 Ion Channel

Detailed Information

Material Type  
 단행본
 
0017161676
Date and Time of Latest Transaction  
20250211151429
ISBN  
9798383608005
DDC  
612
Author  
Li, Shisheng.
Title/Author  
Energetics of Vanilloid Activation of TRPV1 Ion Channel
Publish Info  
[Sl] : University of California, Davis, 2024
Publish Info  
Ann Arbor : ProQuest Dissertations & Theses, 2024
Material Info  
107 p
General Note  
Source: Dissertations Abstracts International, Volume: 86-02, Section: B.
General Note  
Advisor: Zheng, Jie.
학위논문주기  
Thesis (Ph.D.)--University of California, Davis, 2024.
Abstracts/Etc  
요약Ligand activation of the nociceptive TRPV1 ion channel by vanilloids is a proven and powerful pathway for pain management and serves as one of the best model systems for analyzing allosteric coupling in ion channels. However, vanilloid binding and activation have been mostly described only qualitatively in the past. We developed a novel method to isolate channel gating states with a specific number of bound ligands and bound configuration, which allowed direct measurement of binding affinity and gating energetics on a per subunit basis. We determined that capsaicin binds to a rat TRPV1 subunit with an association constant of 2.4X106 M-1 , and found ligand binding to each subunit is nearly independent. Each ligand binding contributes 1.70 to 1.86 kcal/mol activation energy. Subunit contributions are nearly equal as postulated in the MWC model, with a minor deviation that two capsaicin molecules bound to diagonal subunits yield stronger cooperativity (by 0.3 to 0.4 kcal/mol) than those bound to neighboring subunits. 
Subject Added Entry-Topical Term  
Physiology
Subject Added Entry-Topical Term  
Biophysics
Subject Added Entry-Topical Term  
Cellular biology
Subject Added Entry-Topical Term  
Biochemistry
Index Term-Uncontrolled  
Allostery
Index Term-Uncontrolled  
Intermediate states
Index Term-Uncontrolled  
Ligand gating
Index Term-Uncontrolled  
TRPV1
Index Term-Uncontrolled  
Vanilloids
Added Entry-Corporate Name  
University of California, Davis Molecular Cellular and Integrative Physiology
Host Item Entry  
Dissertations Abstracts International. 86-02B.
Electronic Location and Access  
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■035    ▼a(MiAaPQ)AAI31295125
■040    ▼aMiAaPQ▼cMiAaPQ
■0820  ▼a612
■1001  ▼aLi,  Shisheng.
■24510▼aEnergetics  of  Vanilloid  Activation  of  TRPV1  Ion  Channel
■260    ▼a[Sl]▼bUniversity  of  California,  Davis▼c2024
■260  1▼aAnn  Arbor▼bProQuest  Dissertations  &  Theses▼c2024
■300    ▼a107  p
■500    ▼aSource:  Dissertations  Abstracts  International,  Volume:  86-02,  Section:  B.
■500    ▼aAdvisor:  Zheng,  Jie.
■5021  ▼aThesis  (Ph.D.)--University  of  California,  Davis,  2024.
■520    ▼aLigand  activation  of  the  nociceptive  TRPV1  ion  channel  by  vanilloids  is  a  proven  and  powerful  pathway  for  pain  management  and  serves  as  one  of  the  best  model  systems  for  analyzing  allosteric  coupling  in  ion  channels.  However,  vanilloid  binding  and  activation  have  been  mostly  described  only  qualitatively  in  the  past.  We  developed  a  novel  method  to  isolate  channel  gating  states  with  a  specific  number  of  bound  ligands  and  bound  configuration,  which  allowed  direct  measurement  of  binding  affinity  and  gating  energetics  on  a  per  subunit  basis.  We  determined  that  capsaicin  binds  to  a  rat  TRPV1  subunit  with  an  association  constant  of  2.4X106  M-1  ,  and  found  ligand  binding  to  each  subunit  is  nearly  independent.  Each  ligand  binding  contributes  1.70  to  1.86  kcal/mol  activation  energy.  Subunit  contributions  are  nearly  equal  as  postulated  in  the  MWC  model,  with  a  minor  deviation  that  two  capsaicin  molecules  bound  to  diagonal  subunits  yield  stronger  cooperativity  (by  0.3  to  0.4  kcal/mol)  than  those  bound  to  neighboring  subunits. 
■590    ▼aSchool  code:  0029.
■650  4▼aPhysiology
■650  4▼aBiophysics
■650  4▼aCellular  biology
■650  4▼aBiochemistry
■653    ▼aAllostery
■653    ▼aIntermediate  states
■653    ▼aLigand  gating
■653    ▼aTRPV1
■653    ▼aVanilloids
■690    ▼a0719
■690    ▼a0786
■690    ▼a0379
■690    ▼a0487
■71020▼aUniversity  of  California,  Davis▼bMolecular,  Cellular  and  Integrative  Physiology.
■7730  ▼tDissertations  Abstracts  International▼g86-02B.
■790    ▼a0029
■791    ▼aPh.D.
■792    ▼a2024
■793    ▼aEnglish
■85640▼uhttp://www.riss.kr/pdu/ddodLink.do?id=T17161676▼nKERIS▼z이  자료의  원문은  한국교육학술정보원에서  제공합니다.

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