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Lead identification and characterization of hTrkA type 2 inhibitors.
Subramanian G, Zhu Y, Bowen SJ, Roush N, White JA, Huczek D, Zachary T, Javens C, Williams T, Janssen A, Gonzales A. Subramanian G, et al. Among authors: zachary t. Bioorg Med Chem Lett. 2019 Nov 15;29(22):126680. doi: 10.1016/j.bmcl.2019.126680. Epub 2019 Sep 13. Bioorg Med Chem Lett. 2019. PMID: 31610943
The type 2 binding mode with the DFG-out and alphaC-helix out hTrkA kinase domain conformation was confirmed from X-ray crystallographic solution of a representative inhibitor analog, 1b. ...
The type 2 binding mode with the DFG-out and alphaC-helix out hTrkA kinase domain conformation was confirmed from X-ray crystallograp …
Type 2 inhibitor leads of human tropomyosin receptor kinase (hTrkA).
Subramanian G, Bowen SJ, Zhu Y, Roush N, Zachary T, Javens C, Williams T, Janssen A, Gonzales A. Subramanian G, et al. Among authors: zachary t. Bioorg Med Chem Lett. 2019 Oct 1;29(19):126624. doi: 10.1016/j.bmcl.2019.126624. Epub 2019 Aug 16. Bioorg Med Chem Lett. 2019. PMID: 31444087
Additional experimental validation using the Caliper technology with either the active or inactive kinase conditions demonstrated the leads, 1a and 2a, to preferentially bind the kinase inactive state. X-ray structural analysis of the kinase domain of hTrkA1a/2a complexes …
Additional experimental validation using the Caliper technology with either the active or inactive kinase conditions demonstrated the leads, …
In Pursuit of an Allosteric Human Tropomyosin Kinase A (hTrkA) Inhibitor for Chronic Pain.
Subramanian G, Duclos B, Johnson PD, Williams T, Ross JT, Bowen SJ, Zhu Y, White JA, Hedke C, Huczek D, Collard W, Javens C, Vairagoundar R, Respondek T, Zachary T, Maddux T, Cox MR, Kamerling S, Gonzales AJ. Subramanian G, et al. Among authors: zachary t. ACS Med Chem Lett. 2021 Oct 25;12(11):1847-1852. doi: 10.1021/acsmedchemlett.1c00483. eCollection 2021 Nov 11. ACS Med Chem Lett. 2021. PMID: 34795875 Free PMC article.
Herein, we report the pharmacological properties of a selective hTrkA allosteric inhibitor, 1. 1 was shown to be active against the full length hTrkA, showing preferential binding for the inactive kinase, and was confirmed through the X-ray of hTrkA...1 bound complex. 1 wa …
Herein, we report the pharmacological properties of a selective hTrkA allosteric inhibitor, 1. 1 was shown to be active against the full len …
Synthetic inhibitor leads of human tropomyosin receptor kinase A (hTrkA).
Subramanian G, Vairagoundar R, Bowen SJ, Roush N, Zachary T, Javens C, Williams T, Janssen A, Gonzales A. Subramanian G, et al. Among authors: zachary t. RSC Med Chem. 2020 Jan 10;11(3):370-377. doi: 10.1039/c9md00554d. eCollection 2020 Mar 1. RSC Med Chem. 2020. PMID: 33479642 Free PMC article.
In silico virtual screening followed by in vitro biochemical, biophysical, and cellular screening resulted in the identification of distinctly different hTrkA kinase domain inhibitor scaffolds. X-ray structural analysis of representative inhibitors bound to hTrkA kinase do …
In silico virtual screening followed by in vitro biochemical, biophysical, and cellular screening resulted in the identification of distinct …