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   Articles with "novel allosteric" as a keyword



Screening herbal and natural product libraries to aid discovery of novel allosteric modulators of human P2X7

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recommendations! Published in 2024 at "Purinergic Signalling"

DOI: 10.1007/s11302-024-10055-6

Abstract: P2X7 is an emerging therapeutic target for several disorders and diseases due to its role in inflammatory signalling. This study aimed to exploit the unique chemical libraries of plants used in traditional medicinal practices to… read more here.

Keywords: allosteric modulators; natural product; plant; human p2x7 ... See more keywords

Molecular modelling approaches predicted 1,2,3-triazolyl ester of ketorolac (15K) to be a novel allosteric modulator of the oncogenic kinase PAK1

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recommendations! Published in 2021 at "Scientific Reports"

DOI: 10.1038/s41598-021-96817-3

Abstract: P21-activated kinases (PAKs) are serine/threonine protein kinase which have six different isoforms (PAK1–6). Of those, PAK1 is overexpressed in many cancers and considered to be a major chemotherapeutic target. Most of the developed PAK1 inhibitor… read more here.

Keywords: novel allosteric; inhibitor; ester ketorolac; triazolyl ester ... See more keywords

A novel allosteric GCase modulator prevents Tau accumulation in GBA1WT and GBA1L444P/L444P cellular models

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recommendations! Published in 2025 at "Scientific Reports"

DOI: 10.1038/s41598-025-02346-8

Abstract: A slow decline in the autophagy-lysosomal pathway is a hallmark of the normal aging brain. Yet, an acceleration of this cellular function may propel neurodegenerative events. In fact, mutations in genes associated with the autophagy-lysosomal… read more here.

Keywords: gcase modulator; tau accumulation; accumulation; allosteric gcase ... See more keywords

Abstract 1176: Preclinical characterization of the pharmacokinetic-pharmacodynamics-efficacy relationship of novel allosteric SHP2 inhibitors

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recommendations! Published in 2017 at "Cancer Research"

DOI: 10.1158/1538-7445.am2017-1176

Abstract: SHP2 is a non-receptor protein tyrosine phosphatase downstream of receptor tyrosine kinases (RTK). Mutations yielding constitutive activation of SHP2 primarily lead to activation of the MAPK pathway and have been found in multiple tumor types.… read more here.

Keywords: novel allosteric; shp2; allosteric shp2; shp2 inhibitors ... See more keywords

Abstract P5-06-16: Preclinical Characterization of LAE118, a Novel Allosteric Pan-mutant Selective PI3Kα Inhibitor

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recommendations! Published in 2025 at "Clinical Cancer Research"

DOI: 10.1158/1557-3265.sabcs24-p5-06-16

Abstract: PIK3CA is one of the most frequently mutated oncogenes in cancer, found in approximately 13% human cancers. PI3Kα mutations are prevalent in patients with breast, colorectal, lung, endometrial, and numerous other cancers. Three hotspot mutations… read more here.

Keywords: lae118; allosteric pan; lae118 novel; mutant selective ... See more keywords

Dissecting a novel allosteric mechanism of cruzain: A computer-aided approach

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recommendations! Published in 2019 at "PLoS ONE"

DOI: 10.1371/journal.pone.0211227

Abstract: Trypanosoma cruzi is the causative agent of Chagas disease, a neglected infection affecting millions of people in tropical regions. There are several chemotherapeutic agents for the treatment of this disease, but most of them are… read more here.

Keywords: novel allosteric; allosteric inhibitors; site; allosteric mechanism ... See more keywords

Discovery of Novel Allosteric Inhibitors of Deoxyhypusine Synthase

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recommendations! Published in 2020 at "Journal of Medicinal Chemistry"

DOI: 10.2210/pdb6p4v/pdb

Abstract: Deoxyhypusine synthase (DHPS) utilizes spermidine and NAD as cofactors to incorporate a hypusine modification into the eukaryotic translation initiation factor 5A (eIF5A). Hypusine is essential for... read more here.

Keywords: discovery novel; novel allosteric; inhibitors deoxyhypusine; allosteric inhibitors ... See more keywords

A Novel Allosteric Inhibitor Targeting IMPDH at Y233 Overcomes Resistance to Tyrosine Kinase Inhibitors in Lymphoma

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recommendations! Published in 2025 at "Cancers"

DOI: 10.3390/cancers17203389

Abstract: Simple Summary Cancer cells often rely on altered metabolism to support their rapid growth. We discovered that two cancer-driving proteins, ALK and SRC, directly modify and activate a key metabolic enzyme called IMPDH2. This modification… read more here.

Keywords: cancer; targeting impdh; cancer cells; allosteric inhibitor ... See more keywords