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• W2893413429 abstract "Identifying ligands of G protein-coupled receptors (GPCRs) that elicit biased downstream signalling is an established strategy for separating the desired and unwanted effects of these receptors. Campbell and Smrcka describe how inhibiting the downstream G proteins themselves could also be used to bias GPCR signalling, as well as block pathways shared by multiple GPCRs involved in complex diseases, and discuss how the currently available G protein ligands could be optimized to generate therapeutic leads. G protein-coupled receptors (GPCRs) are the largest class of drug targets, largely owing to their druggability, diversity and physiological efficacy. Many drugs selectively target specific subtypes of GPCRs, but high specificity for individual GPCRs may not be desirable in complex multifactorial disease states in which multiple receptors may be involved. One approach is to target G protein subunits rather than the GPCRs directly. This approach has the potential to achieve broad efficacy by blocking pathways shared by multiple GPCRs. Additionally, because many GPCRs couple to multiple G protein signalling pathways, blocking specific G protein subunits can 'bias' GPCR signals by inhibiting only a subset of these signals. Molecules that target G protein α or βγ-subunits have been developed and show strong efficacy in multiple preclinical disease models and biased inhibition of G protein signalling. In this Review, we discuss the development and characterization of G protein α and βγ-subunit ligands and the preclinical evidence that this exciting new approach has potential for therapeutic efficacy in a number of indications, such as pain, thrombosis, asthma and heart failure." @default.
• W2893413429 created "2018-10-05" @default.
• W2893413429 creator A5002671842 @default.
• W2893413429 creator A5072207706 @default.
• W2893413429 date "2018-09-28" @default.
• W2893413429 modified "2023-10-05" @default.
• W2893413429 title "Targeting G protein-coupled receptor signalling by blocking G proteins" @default.
• W2893413429 cites W1496654715 @default.
• W2893413429 cites W1498034410 @default.
• W2893413429 cites W1510671746 @default.
• W2893413429 cites W1511887721 @default.
• W2893413429 cites W1514161613 @default.
• W2893413429 cites W1515479627 @default.
• W2893413429 cites W1516430041 @default.
• W2893413429 cites W1518056784 @default.
• W2893413429 cites W1518153787 @default.
• W2893413429 cites W1519582317 @default.
• W2893413429 cites W1528054863 @default.
• W2893413429 cites W1534335694 @default.
• W2893413429 cites W1538946196 @default.
• W2893413429 cites W1560061125 @default.
• W2893413429 cites W1565496454 @default.
• W2893413429 cites W1568965788 @default.
• W2893413429 cites W1570939625 @default.
• W2893413429 cites W1575223177 @default.
• W2893413429 cites W1580968401 @default.
• W2893413429 cites W1582905488 @default.
• W2893413429 cites W1584157616 @default.
• W2893413429 cites W1621683903 @default.
• W2893413429 cites W1655589213 @default.
• W2893413429 cites W1755674448 @default.
• W2893413429 cites W1864418962 @default.
• W2893413429 cites W1914868353 @default.
• W2893413429 cites W1958742527 @default.
• W2893413429 cites W1960199343 @default.
• W2893413429 cites W1964186423 @default.
• W2893413429 cites W1964619469 @default.
• W2893413429 cites W1970069677 @default.
• W2893413429 cites W1971616605 @default.
• W2893413429 cites W1972211504 @default.
• W2893413429 cites W1972370755 @default.
• W2893413429 cites W1972760976 @default.
• W2893413429 cites W1973046803 @default.
• W2893413429 cites W1973138130 @default.
• W2893413429 cites W1975614725 @default.
• W2893413429 cites W1977074371 @default.
• W2893413429 cites W1977558403 @default.
• W2893413429 cites W1984080990 @default.
• W2893413429 cites W1985799046 @default.
• W2893413429 cites W1988300367 @default.
• W2893413429 cites W1993096939 @default.
• W2893413429 cites W1995103905 @default.
• W2893413429 cites W1996542598 @default.
• W2893413429 cites W1998402796 @default.
• W2893413429 cites W2000521278 @default.
• W2893413429 cites W2005614924 @default.
• W2893413429 cites W2008052643 @default.
• W2893413429 cites W2008174039 @default.
• W2893413429 cites W2008635838 @default.
• W2893413429 cites W2008740148 @default.
• W2893413429 cites W2009127368 @default.
• W2893413429 cites W2011309117 @default.
• W2893413429 cites W2015087988 @default.
• W2893413429 cites W2016923687 @default.
• W2893413429 cites W2017316435 @default.
• W2893413429 cites W2022723700 @default.
• W2893413429 cites W2023865340 @default.
• W2893413429 cites W2024177986 @default.
• W2893413429 cites W2025837534 @default.
• W2893413429 cites W2027182286 @default.
• W2893413429 cites W2028965457 @default.
• W2893413429 cites W2029078879 @default.
• W2893413429 cites W2029345540 @default.
• W2893413429 cites W2030185192 @default.
• W2893413429 cites W2033272737 @default.
• W2893413429 cites W2034965587 @default.
• W2893413429 cites W2036168569 @default.
• W2893413429 cites W2043647387 @default.
• W2893413429 cites W2043698693 @default.
• W2893413429 cites W2044775506 @default.
• W2893413429 cites W2045185868 @default.
• W2893413429 cites W2049253479 @default.
• W2893413429 cites W2052280808 @default.
• W2893413429 cites W2053294241 @default.
• W2893413429 cites W2053520756 @default.
• W2893413429 cites W2054007190 @default.
• W2893413429 cites W2056010202 @default.
• W2893413429 cites W2056169996 @default.
• W2893413429 cites W2056523976 @default.
• W2893413429 cites W2057469265 @default.
• W2893413429 cites W2058252463 @default.
• W2893413429 cites W2059759050 @default.
• W2893413429 cites W2062978622 @default.
• W2893413429 cites W2064297593 @default.
• W2893413429 cites W2064483656 @default.
• W2893413429 cites W2065128867 @default.
• W2893413429 cites W2065136899 @default.
• W2893413429 cites W2067917704 @default.

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