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A highly D3R-selective and efficacious partial agonist (S)-ABS01-113 compared to its D3R-selective antagonist enantiomer (R)-ABS01-113 as potential treatments for opioid use disorder.
Galaj E, Bi GH, Klein B, Hempel B, Shaik AB, Gogarnoiu ES, Friedman J, Lam J, Rais R, Reed JF, Bloom SH, Swanson TL, Schmachtenberg JL, Eshleman AJ, Janowsky A, Xi ZX, Newman AH. Galaj E, et al. Among authors: lam j. Neuropsychopharmacology. 2022 Dec;47(13):2309-2318. doi: 10.1038/s41386-022-01379-1. Epub 2022 Jul 25. Neuropsychopharmacology. 2022. PMID: 35879349 Free PMC article.
Investigation of Novel Primary and Secondary Pharmacophores and 3-Substitution in the Linking Chain of a Series of Highly Selective and Bitopic Dopamine D3 Receptor Antagonists and Partial Agonists.
Shaik AB, Kumar V, Bonifazi A, Guerrero AM, Cemaj SL, Gadiano A, Lam J, Xi ZX, Rais R, Slusher BS, Newman AH. Shaik AB, et al. Among authors: lam j. J Med Chem. 2019 Oct 24;62(20):9061-9077. doi: 10.1021/acs.jmedchem.9b00607. Epub 2019 Oct 15. J Med Chem. 2019. PMID: 31526003 Free PMC article.
The Novel Glutamine Antagonist Prodrug JHU395 Has Antitumor Activity in Malignant Peripheral Nerve Sheath Tumor.
Lemberg KM, Zhao L, Wu Y, Veeravalli V, Alt J, Aguilar JMH, Dash RP, Lam J, Tenora L, Rodriguez C, Nedelcovych MT, Brayton C, Majer P, Blakeley JO, Rais R, Slusher BS. Lemberg KM, et al. Among authors: lam j. Mol Cancer Ther. 2020 Feb;19(2):397-408. doi: 10.1158/1535-7163.MCT-19-0319. Epub 2019 Oct 8. Mol Cancer Ther. 2020. PMID: 31594823 Free PMC article.
Structure-Activity Relationships for a Series of (Bis(4-fluorophenyl)methyl)sulfinyl Alkyl Alicyclic Amines at the Dopamine Transporter: Functionalizing the Terminal Nitrogen Affects Affinity, Selectivity, and Metabolic Stability.
Slack RD, Ku TC, Cao J, Giancola JB, Bonifazi A, Loland CJ, Gadiano A, Lam J, Rais R, Slusher BS, Coggiano M, Tanda G, Newman AH. Slack RD, et al. Among authors: lam j. J Med Chem. 2020 Mar 12;63(5):2343-2357. doi: 10.1021/acs.jmedchem.9b01188. Epub 2019 Nov 14. J Med Chem. 2020. PMID: 31661268 Free PMC article.
Structure-activity relationships for a series of (Bis(4-fluorophenyl)methyl)sulfinylethyl-aminopiperidines and -piperidine amines at the dopamine transporter: Bioisosteric replacement of the piperazine improves metabolic stability.
Giancola JB, Bonifazi A, Cao J, Ku T, Haraczy AJ, Lam J, Rais R, Coggiano MA, Tanda G, Newman AH. Giancola JB, et al. Among authors: lam j. Eur J Med Chem. 2020 Dec 15;208:112674. doi: 10.1016/j.ejmech.2020.112674. Epub 2020 Aug 9. Eur J Med Chem. 2020. PMID: 32947229 Free PMC article.
Discovery of DRP-104, a tumor-targeted metabolic inhibitor prodrug.
Rais R, Lemberg KM, Tenora L, Arwood ML, Pal A, Alt J, Wu Y, Lam J, Aguilar JMH, Zhao L, Peters DE, Tallon C, Pandey R, Thomas AG, Dash RP, Seiwert T, Majer P, Leone RD, Powell JD, Slusher BS. Rais R, et al. Among authors: lam j. Sci Adv. 2022 Nov 18;8(46):eabq5925. doi: 10.1126/sciadv.abq5925. Epub 2022 Nov 16. Sci Adv. 2022. PMID: 36383674 Free PMC article.
2,839 results