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The mitochondrial fission protein Drp1 in liver is required to mitigate NASH and prevents the activation of the mitochondrial ISR.
Steffen J, Ngo J, Wang SP, Williams K, Kramer HF, Ho G, Rodriguez C, Yekkala K, Amuzie C, Bialecki R, Norquay L, Nawrocki AR, Erion M, Pocai A, Shirihai OS, Liesa M. Steffen J, et al. Among authors: kramer hf. Mol Metab. 2022 Oct;64:101566. doi: 10.1016/j.molmet.2022.101566. Epub 2022 Aug 6. Mol Metab. 2022. PMID: 35940556 Free PMC article.
A knowledge-based, structural-aided discovery of a novel class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors.
Schulte CA, Deaton DN, Diaz E, Do Y, Gampe RT, Guss JH, Hancock AP, Hobbs H, Hodgson ST, Holt J, Jeune MR, Kahler KM, Kramer HF, Le J, Mortenson PN, Musetti C, Nolte RT, Orband-Miller LA, Peckham GE, Petrov KG, Pietrak BL, Poole C, Price DJ, Saxty G, Shillings A, Smalley TL Jr, Somers DO, Stewart EL, Stuart JD, Thomson SA. Schulte CA, et al. Among authors: kramer hf. Bioorg Med Chem Lett. 2021 Sep 1;47:128113. doi: 10.1016/j.bmcl.2021.128113. Epub 2021 May 13. Bioorg Med Chem Lett. 2021. PMID: 33991628
The exploration of aza-quinolines as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors with low brain exposure.
Cadilla R, Deaton DN, Do Y, Elkins PA, Ennulat D, Guss JH, Holt J, Jeune MR, King AG, Klapwijk JC, Kramer HF, Kramer NJ, Laffan SB, Masuria PI, McDougal AV, Mortenson PN, Musetti C, Peckham GE, Pietrak BL, Poole C, Price DJ, Rendina AR, Sati G, Saxty G, Shearer BG, Shewchuk LM, Sneddon HF, Stewart EL, Stuart JD, Thomas DN, Thomson SA, Ward P, Wilson JW, Xu T, Youngman MA. Cadilla R, et al. Among authors: kramer hf. Bioorg Med Chem. 2020 Dec 1;28(23):115791. doi: 10.1016/j.bmc.2020.115791. Epub 2020 Oct 3. Bioorg Med Chem. 2020. PMID: 33059303
Sustained elevation of MG53 in the bloodstream increases tissue regenerative capacity without compromising metabolic function.
Bian Z, Wang Q, Zhou X, Tan T, Park KH, Kramer HF, McDougal A, Laping NJ, Kumar S, Adesanya TMA, Sermersheim M, Yi F, Wang X, Wu J, Gumpper K, Jiang Q, He D, Lin PH, Li H, Guan F, Zhou J, Kohr MJ, Zeng C, Zhu H, Ma J. Bian Z, et al. Among authors: kramer hf. Nat Commun. 2019 Oct 11;10(1):4659. doi: 10.1038/s41467-019-12483-0. Nat Commun. 2019. PMID: 31604915 Free PMC article.
The discovery of quinoline-3-carboxamides as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors.
Deaton DN, Do Y, Holt J, Jeune MR, Kramer HF, Larkin AL, Orband-Miller LA, Peckham GE, Poole C, Price DJ, Schaller LT, Shen Y, Shewchuk LM, Stewart EL, Stuart JD, Thomson SA, Ward P, Wilson JW, Xu T, Guss JH, Musetti C, Rendina AR, Affleck K, Anders D, Hancock AP, Hobbs H, Hodgson ST, Hutchinson J, Leveridge MV, Nicholls H, Smith IED, Somers DO, Sneddon HF, Uddin S, Cleasby A, Mortenson PN, Richardson C, Saxty G. Deaton DN, et al. Among authors: kramer hf. Bioorg Med Chem. 2019 Apr 15;27(8):1456-1478. doi: 10.1016/j.bmc.2019.02.017. Epub 2019 Feb 11. Bioorg Med Chem. 2019. PMID: 30858025
Correction to: HIF prolyl hydroxylase inhibition protects skeletal muscle from eccentric contraction induced injury.
Billin AN, Honeycutt SE, McDougal AV, Kerr JP, Chen Z, Freudenberg JM, Rajpal DK, Luo G, Kramer HF, Geske RS, Fang F, Yao B, Clark RV, Lepore J, Cobitz A, Miller R, Nosaka K, Hinken AC, Russell AJ. Billin AN, et al. Among authors: kramer hf. Skelet Muscle. 2018 Dec 10;8(1):38. doi: 10.1186/s13395-018-0185-7. Skelet Muscle. 2018. PMID: 30526662 Free PMC article.
HIF prolyl hydroxylase inhibition protects skeletal muscle from eccentric contraction-induced injury.
Billin AN, Honeycutt SE, McDougal AV, Kerr JP, Chen Z, Freudenberg JM, Rajpal DK, Luo G, Kramer HF, Geske RS, Fang F, Yao B, Clark RV, Lepore J, Cobitz A, Miller R, Nosaka K, Hinken AC, Russell AJ. Billin AN, et al. Among authors: kramer hf. Skelet Muscle. 2018 Nov 13;8(1):35. doi: 10.1186/s13395-018-0179-5. Skelet Muscle. 2018. PMID: 30424786 Free PMC article. Clinical Trial.
24 results