Medicinal and Biological Chemistry

Kynurenine Pathway
Delta Opioid Receptor
Fluorination in Medicinal Chemistry
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58. Unified Enantioselective Synthesis of 5-Phenylmorphans and cis-Octahydroisoquinolines
58. Unified Enantioselective Synthesis of 5-Phenylmorphans and cis-Octahydroisoquinolines

Mahgoub, A.; Khamrai, J.; Festus, O.; Altman, R. A.*

Org. Lett., 2025, 27, 8941–8945.

56. Discovery of RGS2-FBXO44 interaction inhibitors using a cell-based NanoBit assay
56. Discovery of RGS2-FBXO44 interaction inhibitors using a cell-based NanoBit assay

Aryal, S.; Wong, C. S. Y.; McNabb, H. J.; Junaid, A.; Altman, R. A.; Sjögren, B.*

Mol. Pharmacol. 2025, 107, 100030.

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53. A Phenotypic High-Throughput Screen Identifies Small Molecule Modulators of Endogenous RGS10 in BV-2 Cells

Talele, S.; Gonzalez, S.; Trudeau, J.; Junaid, A.; Loy, C.; Altman, R. A.; Sjogren, J. B.*

J. Med. Chem. 2024, 67, 20343–20352.

52. α-Amino-β-Carboxymuconate-ε-Semialdehyde Decarboxylase Catalyzes Enol/Keto Tautomerization of Oxaloacetate
52. α-Amino-β-Carboxymuconate-ε-Semialdehyde Decarboxylase Catalyzes Enol/Keto Tautomerization of Oxaloacetate

Yang, Y.; Davis, I.; Altman, R. A.; Liu, A.*

J. Biol. Chem. 2024, 300, 107878.

44. Fluoroalkylation of Dextromethorphan Improves CNS Exposure and Metabolic Stability
44. Fluoroalkylation of Dextromethorphan Improves CNS Exposure and Metabolic Stability

Sorrentino, J. P.; Altman, R. A.*

ACS Med. Chem. Lett. 2022, 13, 707–713.

43. Modulating β-Arrestin-2 Recruitment at the δ- and μ-Opioid Receptors
43. Modulating β-Arrestin-2 Recruitment at the δ- and μ-Opioid Receptors

Sharma K. S.; Cassell, R. J.; Meqbil, Y. J.; Su, H.; Blaine, A. T.; Cummins, B. R.; Mores, K. L.; Johnson, D.; van Rijn, R. M.;* Altman, R. A.*

RSC Med. Chem. 2021, 12, 1958–1967.

40. Diflunisal Derivatives as Modulators of ACMS Decarboxylase Targeting the Tryptophan-Kynurenine Pathway
40. Diflunisal Derivatives as Modulators of ACMS Decarboxylase Targeting the Tryptophan-Kynurenine Pathway

Yang, Y.; Borel, T.; de Azambuja, F.; Johnson, D.; Sorrentino, J. P.; Udokwu, C.; Davis, I.; Liu, A.;* Altman, R. A.*

J. Med. Chem. 2021, 64, 797–811.

37. Late-Stage Conversion of a Metabolically Labile Aryl Methyl Ether-Containing Natural Product to Fluoroalkyl Analogues
37. Late-Stage Conversion of a Metabolically Labile Aryl Methyl Ether-Containing Natural Product to Fluoroalkyl Analogues

Sorrentino, J. S.; Ambler, B. R.; Altman, R. A.*

J. Org. Chem. 2020, 85, 5416–5427.

34. The Meta-Position of Phe4 in Leu-enkephalin Regulates Potency, Selectivity, Functional Activity, and Signaling Bias at the Delta and Mu Opioid Receptors
34. The Meta-Position of Phe4 in Leu-enkephalin Regulates Potency, Selectivity, Functional Activity, and Signaling Bias at the Delta and Mu Opioid Receptors

Cassell, R. J.; Sharma K. S.; Su, H.; Cummins, B. R.; Cui, H.; Mores, K. L.; Blaine, A. T.; Altman, R. A.;* van Rijn, R. M.*

Molecules 2019, 24, 4542.

29. Synthesis of Leu-Enkephalin Peptidomimetics Containing Trifluromethylalkenes as Amide Isopolar Mimics
29. Synthesis of Leu-Enkephalin Peptidomimetics Containing Trifluromethylalkenes as Amide Isopolar Mimics

Eeda, V.; Selvaraju, M.; Altman, R. A.*

J. Fluorine Chem. 2019, 218, 90–98.

28. Tyr1-ψ[(Z)CF═CH]-Gly2 Fluorinated Peptidomimetic Improves Distribution and Metabolism Properties of Leu-Enkephalin
28. Tyr1-ψ[(Z)CF═CH]-Gly2 Fluorinated Peptidomimetic Improves Distribution and Metabolism Properties of Leu-Enkephalin

Altman, R. A.*; Sharma, K. K.; Rajewski, L. G.; Toren, P. C.; Baltezor, M. J.; Pal, M.; Karad, S. N.

ACS Chem. Neurosci. 2018, 9, 1735–1742.

27. Stepwise O-Atom Transfer in Heme-based Tryptophan Dioxygenase: The Role of Substrate Ammonium in the Epoxide Ring Opening
27. Stepwise O-Atom Transfer in Heme-based Tryptophan Dioxygenase: The Role of Substrate Ammonium in the Epoxide Ring Opening

Shin, I.; Ambler, B. R.; Wherritt, D.; Griffith, W.; Maldonado, A.; Altman, R. A.;* Liu, A.*

J. Am. Chem. Soc. 2018, 140, 4372–4379.

24. Synthesis and Opioid Activity of Tyr1–ψ[(Z)CF=CH]–Gly2 and Tyr1–ψ[(S)/(R)-CF3CH–NH]–Gly2 Leu-enkephalin Fluorinated Peptidomimetics
24. Synthesis and Opioid Activity of Tyr1–ψ[(Z)CF=CH]–Gly2 and Tyr1–ψ[(S)/(R)-CF3CH–NH]–Gly2 Leu-enkephalin Fluorinated Peptidomimetics

Karad, S. N.; Pal, M.; Crowley, R. S.; Prisinzano, T. E.; Altman, R. A.*

ChemMedChem 2017, 12, 571–576.

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