* . *
  • About
  • Advertise
  • Privacy & Policy
  • Contact
Thursday, July 10, 2025
Earth-News
  • Home
  • Business
  • Entertainment
    Immersive sports and entertainment venue Cosm set to build its 5th location in Cleveland – WKYC

    Cosm Reveals Exciting Vision for Its 5th Immersive Sports and Entertainment Venue in Cleveland

    Monumental Sports & Entertainment’s Samantha Brady on the Power of the RSN’s Direct-to-Consumer Streaming Service Monumental+ – Sports Video Group

    Samantha Brady Reveals How Monumental+ is Transforming Sports Streaming with Direct-to-Consumer Access

    Moses Singer Welcomes Entertainment and Intellectual Property Partner Frederick Bimbler – Yahoo Finance

    Moses Singer Expands Team with New Entertainment and Intellectual Property Partner Frederick Bimbler

    Longhua District and Max-Matching Entertainments, supported by RWS Global forge strategic partnership to develop international IP-themed entertainment complex – Amusement Today

    Longhua District and Max-Matching Entertainments, supported by RWS Global forge strategic partnership to develop international IP-themed entertainment complex – Amusement Today

    Government whip to withdraw Entertainment Complex Bill on July 9 – Nation Thailand

    Government whip to withdraw Entertainment Complex Bill on July 9 – Nation Thailand

    Magicians and Battlebots light up Las Vegas entertainment scene – KSNV

    Magicians and Battlebots Take Las Vegas Entertainment by Storm

  • General
  • Health
  • News

    Cracking the Code: Why China’s Economic Challenges Aren’t Shaking Markets, Unlike America’s” – Bloomberg

    Trump’s Narrow Window to Spread the Truth About Harris

    Trump’s Narrow Window to Spread the Truth About Harris

    Israel-Gaza war live updates: Hamas leader Ismail Haniyeh assassinated in Iran, group says

    Israel-Gaza war live updates: Hamas leader Ismail Haniyeh assassinated in Iran, group says

    PAP Boss to Niger Delta Youths, Stay Away from the Protest

    PAP Boss to Niger Delta Youths, Stay Away from the Protest

    Court Restricts Protests In Lagos To Freedom, Peace Park

    Court Restricts Protests In Lagos To Freedom, Peace Park

    Fans React to Jazz Jennings’ Inspiring Weight Loss Journey

    Fans React to Jazz Jennings’ Inspiring Weight Loss Journey

    Trending Tags

    • Trump Inauguration
    • United Stated
    • White House
    • Market Stories
    • Election Results
  • Science
  • Sports
  • Technology
    SMPTE Opens Early Bird Registration for Media Technology Summit – TVTechnology

    SMPTE Launches Early Bird Registration for Exciting Media Technology Summit

    Google Fiber puts Nokia network slicing technology to the test – Fierce Network

    Google Fiber Puts Nokia’s Network Slicing Technology to the Ultimate Test

    Kaseya Extends Community Investment with Addition of Technology Marketing Toolkit – Kaseya

    Kaseya Extends Community Investment with Addition of Technology Marketing Toolkit – Kaseya

    AI and the Trust Revolution: How Technology Is Transforming Human Connections – Foreign Affairs

    AI and the Trust Revolution: How Technology Is Transforming Human Connections – Foreign Affairs

    Technology And Construction Names Join Top Stock Lists: Check Out Additions To IBD 50, Big Cap 20 And More – Investor’s Business Daily

    Technology and Construction Leaders Surge Into Top Stock Rankings: See the Latest Additions to IBD 50, Big Cap 20, and More

    Column: Teach kupuna new technology skills – Honolulu Star-Advertiser

    Empowering Kupuna: Unlocking New Technology Skills for a Connected Future

    Trending Tags

    • Nintendo Switch
    • CES 2017
    • Playstation 4 Pro
    • Mark Zuckerberg
No Result
View All Result
  • Home
  • Business
  • Entertainment
    Immersive sports and entertainment venue Cosm set to build its 5th location in Cleveland – WKYC

    Cosm Reveals Exciting Vision for Its 5th Immersive Sports and Entertainment Venue in Cleveland

    Monumental Sports & Entertainment’s Samantha Brady on the Power of the RSN’s Direct-to-Consumer Streaming Service Monumental+ – Sports Video Group

    Samantha Brady Reveals How Monumental+ is Transforming Sports Streaming with Direct-to-Consumer Access

    Moses Singer Welcomes Entertainment and Intellectual Property Partner Frederick Bimbler – Yahoo Finance

    Moses Singer Expands Team with New Entertainment and Intellectual Property Partner Frederick Bimbler

    Longhua District and Max-Matching Entertainments, supported by RWS Global forge strategic partnership to develop international IP-themed entertainment complex – Amusement Today

    Longhua District and Max-Matching Entertainments, supported by RWS Global forge strategic partnership to develop international IP-themed entertainment complex – Amusement Today

    Government whip to withdraw Entertainment Complex Bill on July 9 – Nation Thailand

    Government whip to withdraw Entertainment Complex Bill on July 9 – Nation Thailand

    Magicians and Battlebots light up Las Vegas entertainment scene – KSNV

    Magicians and Battlebots Take Las Vegas Entertainment by Storm

  • General
  • Health
  • News

    Cracking the Code: Why China’s Economic Challenges Aren’t Shaking Markets, Unlike America’s” – Bloomberg

    Trump’s Narrow Window to Spread the Truth About Harris

    Trump’s Narrow Window to Spread the Truth About Harris

    Israel-Gaza war live updates: Hamas leader Ismail Haniyeh assassinated in Iran, group says

    Israel-Gaza war live updates: Hamas leader Ismail Haniyeh assassinated in Iran, group says

    PAP Boss to Niger Delta Youths, Stay Away from the Protest

    PAP Boss to Niger Delta Youths, Stay Away from the Protest

    Court Restricts Protests In Lagos To Freedom, Peace Park

    Court Restricts Protests In Lagos To Freedom, Peace Park

    Fans React to Jazz Jennings’ Inspiring Weight Loss Journey

    Fans React to Jazz Jennings’ Inspiring Weight Loss Journey

    Trending Tags

    • Trump Inauguration
    • United Stated
    • White House
    • Market Stories
    • Election Results
  • Science
  • Sports
  • Technology
    SMPTE Opens Early Bird Registration for Media Technology Summit – TVTechnology

    SMPTE Launches Early Bird Registration for Exciting Media Technology Summit

    Google Fiber puts Nokia network slicing technology to the test – Fierce Network

    Google Fiber Puts Nokia’s Network Slicing Technology to the Ultimate Test

    Kaseya Extends Community Investment with Addition of Technology Marketing Toolkit – Kaseya

    Kaseya Extends Community Investment with Addition of Technology Marketing Toolkit – Kaseya

    AI and the Trust Revolution: How Technology Is Transforming Human Connections – Foreign Affairs

    AI and the Trust Revolution: How Technology Is Transforming Human Connections – Foreign Affairs

    Technology And Construction Names Join Top Stock Lists: Check Out Additions To IBD 50, Big Cap 20 And More – Investor’s Business Daily

    Technology and Construction Leaders Surge Into Top Stock Rankings: See the Latest Additions to IBD 50, Big Cap 20, and More

    Column: Teach kupuna new technology skills – Honolulu Star-Advertiser

    Empowering Kupuna: Unlocking New Technology Skills for a Connected Future

    Trending Tags

    • Nintendo Switch
    • CES 2017
    • Playstation 4 Pro
    • Mark Zuckerberg
No Result
View All Result
Earth-News
No Result
View All Result
Home Science

Molecular insights into GPCR structure, a vital drug target

January 1, 2024
in Science
Molecular insights into GPCR structure, a vital drug target
Share on FacebookShare on Twitter

In a collaboration, St. Jude scientists studied the adrenaline receptor at an atomic level. They identified amino acids controlling critical properties of the ligand. This receptor, part of the GPCR family, is crucial for many FDA-approved drugs. 

Understanding how GPCRs respond to natural or therapeutic ligands is vital for precise therapies. The study, published in Science, used a detailed approach, replacing one amino acid at a time in the β2-adrenergic receptor to understand each one’s role in mediating signaling responses. This research could pave the way for developing new therapies with specific effects on receptor activity.

Co-corresponding author M. Madan Babu, Ph.D., from St. Jude’s Department of Structural Biology, Center of Excellence for Data-Driven Discovery director and the George J. Pedersen Endowed Chair in Biological Data Science said, “Scientists learn how genes contribute to cell function by disrupting them one at a time. We asked, ‘Why don’t we take this one level deeper? Let’s understand how every amino acid contributes to the functioning of a receptor by mutating them, one amino acid at a time. Through evolution, every amino acid in the receptor has been sculpted somehow to ensure that it binds the natural ligand, in this case adrenaline, and elicits the appropriate physiological response.” 

GPCRs are cell membrane proteins that transmit signals from outside to inside. In β2AR, adrenaline binds out, causing shape changes. These changes activate G proteins, triggering responses inside the cell. Adrenaline, acting on GPCRs like β2AR, can induce the fight-or-flight response across various tissues.

To understand amino acids in GPCR, Dr. Heydenreich mutated each of the 412 in β2AR. Testing each mutant’s response to adrenaline, she assessed efficacy and potency, measuring the maximum response and ligand amount needed for half the answer. 

Surprisingly, only 80 amino acids affected these properties, with one-third located where ligand or G protein binds. Some amino acids control efficacy, some potency, and others both. This insight can guide the design of more potent and efficacious drugs by influencing specific residues in new ligands, providing opportunities for fine-tuning drug responses.

“We’ve measured efficacy and potency for years. However, now we understand how specific amino acids in a protein influence these properties,” explained Dr. Babu. The results show that distinct mechanisms can independently regulate potency and efficacy. This insight forms a basis for understanding how genetic variation affects drug responses in individuals, as Dr. Bouvier from the University of Montreal noted.

Previous research showed the structure of active and inactive states of β2AR. Building on this, researchers investigated the role of amino acids not involved in binding. They systematically examined residues unique to the active state to understand their importance. Using a data science framework, they integrated pharmacological and structural data, revealing a comprehensive picture of GPCR signaling. 

This provided insights into the allosteric network governing efficacy and potency. The study aims to explore transient sub-states and the conformational landscape of proteins, delving even deeper into understanding GPCR signaling at the atomic level.

“We now target mutants affecting efficacy, potency, or both,” said Heydenreich. Molecular dynamics and experiments will uncover mechanisms influencing signaling response in the mutants. 

Babu explains they’re exploring this through a St. Jude Research Collaborative on GPCRs. Beyond “driver” residues mediating active state contacts, they’ll study “passenger” amino acids and “modulator” residues, expanding insights. Their data science approach, not limited to β2AR, can extend to any GPCR, enhancing our understanding of these vital drug targets’ mechanics.

In conclusion, this research sheds light on the molecular intricacies of GPCR structure. It provides insights that can revolutionize the development of new and more effective therapeutic drugs.

Journal reference:

FRANZISKA M. HEYDENREICH ,MARIA MARTI-SOLANO et al., Molecular determinants of ligand efficacy and potency in GPCR signaling. Science. DOI:10.1126/science.adh1859. 

>>> Read full article>>>
Copyright for syndicated content belongs to the linked Source : Tech Explorist – https://www.techexplorist.com/molecular-insights-gpcr-structure-vital-drug-target/79174/

Tags: Insightsmolecularscience
Previous Post

Scientists developed a new family of polymers that can kill bacteria

Next Post

Chinese satellite internet mission rounds off record year for global launches

SMPTE Opens Early Bird Registration for Media Technology Summit – TVTechnology

SMPTE Launches Early Bird Registration for Exciting Media Technology Summit

July 10, 2025
Barstool Sports announces roster for Internet Invitational at Big Cedar Lodge – Springfield News-Leader

Barstool Sports announces roster for Internet Invitational at Big Cedar Lodge – Springfield News-Leader

July 10, 2025
Embedding information flows within ecological networks – Nature

Discovering the Hidden Dynamics of Information Flow in Ecological Networks

July 10, 2025
Mass layoffs can move forward, with devastating impacts for conservation and science – High Country News

Mass layoffs can move forward, with devastating impacts for conservation and science – High Country News

July 10, 2025
The Boar War: Michigan accused of harassing pig farmers using faulty science – Michigan Capitol Confidential

The Boar War: Michigan accused of harassing pig farmers using faulty science – Michigan Capitol Confidential

July 10, 2025
I took my daughter to meet my girlfriend — and what she found changed everything – VegOut

I took my daughter to meet my girlfriend — and what she found changed everything – VegOut

July 9, 2025
See photos of FIFA Club World Cup semifinal: PSG defeats Real Madrid at MetLife Stadium – Bergen Record

PSG Clinches Exciting Victory Over Real Madrid in FIFA Club World Cup Semifinal – Stunning Photos Inside!

July 9, 2025
The Economic Consequences of the Big Odious Bill – The New Yorker

The Economic Consequences of the Big Odious Bill – The New Yorker

July 9, 2025
Immersive sports and entertainment venue Cosm set to build its 5th location in Cleveland – WKYC

Cosm Reveals Exciting Vision for Its 5th Immersive Sports and Entertainment Venue in Cleveland

July 9, 2025
Why 1.5 Million New Yorkers Could Lose Health Insurance Under Trump Bill – The New York Times

How 1.5 Million New Yorkers Could Face Losing Health Insurance Under Trump’s Proposed Bill

July 9, 2025

Categories

Archives

July 2025
MTWTFSS
 123456
78910111213
14151617181920
21222324252627
28293031 
« Jun    
Earth-News.info

The Earth News is an independent English-language daily published Website from all around the World News

Browse by Category

  • Business (20,132)
  • Ecology (713)
  • Economy (737)
  • Entertainment (21,626)
  • General (15,806)
  • Health (9,774)
  • Lifestyle (743)
  • News (22,149)
  • People (738)
  • Politics (746)
  • Science (15,954)
  • Sports (21,236)
  • Technology (15,722)
  • World (719)

Recent News

SMPTE Opens Early Bird Registration for Media Technology Summit – TVTechnology

SMPTE Launches Early Bird Registration for Exciting Media Technology Summit

July 10, 2025
Barstool Sports announces roster for Internet Invitational at Big Cedar Lodge – Springfield News-Leader

Barstool Sports announces roster for Internet Invitational at Big Cedar Lodge – Springfield News-Leader

July 10, 2025
  • About
  • Advertise
  • Privacy & Policy
  • Contact

© 2023 earth-news.info

No Result
View All Result

© 2023 earth-news.info

No Result
View All Result

© 2023 earth-news.info

Go to mobile version