Search citation statements

Order By: Relevance

Paper Sections

Select...
2
1
1

Citation Types

0
40
0

Year Published

2020
2020
2021
2021

Publication Types

Select...
7

Relationship

1
6

Authors

Journals

citations
Cited by 61 publications
(40 citation statements)
references
References 93 publications
0
40
0
Order By: Relevance
“…With accumulating evidence of the multiple advantages boosted by allosteric modulation, it has attracted an ever-growing interest in pharmaceutics, and consequently, the combination of orthosteric and allosteric agents is emerging as a revolutionary strategy to overcome resistance, as exemplified by the growing number of successful cases [ 74 , 75 , 76 , 77 , 78 , 79 ]. Accordingly, a series of orthosteric-allosteric drug combinations have proceeded into clinical trials, mostly involving oncology, viruses, and autoimmune disorders [ 17 ]. In addition to BCR-ABL and EGFR, another quintessential example is targeting nonstructural protein 5A (NS5A) for the treatment of hepatitis C virus (HCV).…”
Section: Discussionmentioning
confidence: 99%
See 2 more Smart Citations
“…With accumulating evidence of the multiple advantages boosted by allosteric modulation, it has attracted an ever-growing interest in pharmaceutics, and consequently, the combination of orthosteric and allosteric agents is emerging as a revolutionary strategy to overcome resistance, as exemplified by the growing number of successful cases [ 74 , 75 , 76 , 77 , 78 , 79 ]. Accordingly, a series of orthosteric-allosteric drug combinations have proceeded into clinical trials, mostly involving oncology, viruses, and autoimmune disorders [ 17 ]. In addition to BCR-ABL and EGFR, another quintessential example is targeting nonstructural protein 5A (NS5A) for the treatment of hepatitis C virus (HCV).…”
Section: Discussionmentioning
confidence: 99%
“…Huang et al designed a set of small-molecules that simultaneously block the orthosteric and allosteric pockets of PfHT1, constituting a novel weapon against multidrug-resistant malaria parasites. It was previously reviewed that in dual-targeting therapeutics, allosteric regulators bind to the recalcitrant target and precisely resensitize the orthosteric site in two major pathways: either through microcosmically reshaping the intrinsic residue network within the protein, or macroscopically shifting the conformational ensemble towards a favorable state [ 17 ]. In fact, these abovementioned resensitizing effects discovered in multiple cases imply the traditional allosteric communication pattern where signals propagate from the allosteric site to the orthosteric site.…”
Section: Discussionmentioning
confidence: 99%
See 1 more Smart Citation
“…In analogy to treatment of multidrug resistant cancers with drug transporter inhibitors, most of the previous studies examined the role of environmental chemicals as competitive inhibitors that limit detoxification capabilities of organisms, thereby acting as 'chemosensitizers' [26,36,37]. However, as we will elaborate upon in this review, emerging structural and functional studies of transporters reveal that the interactions of chemicals with drug transporters can be complex, due to the existence of multiple ligand binding sites in these proteins and additional allosteric interactions [38,39]. Indeed, modern drug discovery and development efforts already seek to evaluate and validate transporter substrates, inhibitors, or noninteracting compounds in the context of various confounding factors, including the type of assay system, physicochemical properties of the test compound, and mixture effects on the overall transport kinetics [40][41][42][43][44][45][46].…”
Section: Introduction-evolution and Function Of The Small Molecule Trmentioning
confidence: 99%
“…Comparing the structures of PfHT1 (19,20) and hGLUT1, we identified an additional pocket adjacent to the substrate-binding site. Coadministration of allosteric and orthosteric drugs is generally applied to tackle drug resistance when these two pockets were spatially separated (21). However, this discovery led to a hypothesis that simultaneously targeting the orthosteric and allosteric…”
mentioning
confidence: 99%