R. M. Borzilleri

Bristol-Myers Squibb (Sweden) — Sweden

Biochemistry, Genetics and Molecular Biology · Life Sciences

33h-index5.3kcitations193works2.02yr avg
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Research Topics

Chemical Synthesis and Analysis(26), Chemical Reaction Mechanisms(16), Cancer Treatment and Pharmacology(14), Organic Chemistry Cycloaddition Reactions(14), Chemical Reactions and Mechanisms(14)

Publications193 total

Covalent inhibitor design confers activity against both GDP- and GTP-bound forms of KRAS G12C
Nature Communications·2026Open Access
Design, Synthesis, and T Cell Checkpoint Combination Potential Of First-In-Class DGKα/ζ Inhibitor BMS-986408
Journal of Medicinal Chemistry·2025
Discovery and Synthesis of Heterobifunctional Degraders of Rearranged during Transfection (RET) Kinase
Journal of Medicinal Chemistry·2024· 6 cited
DGKα/ζ inhibitors combine with PD-1 checkpoint therapy to promote T cell–mediated antitumor immunity
Science Translational Medicine·2023· 23 cited
Long-Acting Tumor-Activated Prodrug of a TGFβR Inhibitor
Journal of Medicinal Chemistry·2021· 6 cited
Development of a Stereoselective and Scalable Synthesis for the Potent Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitor, BMT-297376; <i>N</i>-((<i>R</i>)-1-((<i>cis</i>)-4-(3-(Difluoromethyl)-2-methoxypyridin-4-yl)cyclohexyl)propyl)-6-methoxynicotinamide
Organic Process Research & Development·2021· 5 cited
Conformational-Analysis-Guided Discovery of 2,3-Disubstituted Pyridine IDO1 Inhibitors
ACS Medicinal Chemistry Letters·2021· 5 citedOpen Access
Azatricyclic Inverse Agonists of RORγt That Demonstrate Efficacy in Models of Rheumatoid Arthritis and Psoriasis
ACS Medicinal Chemistry Letters·2021· 7 citedOpen Access
<scp>JAK</scp> Family Inhibitors for Autoimmune Diseases
Burger's Medicinal Chemistry and Drug Discovery·2021
Discovery of Imidazopyridines as Potent Inhibitors of Indoleamine 2,3-Dioxygenase 1 for Cancer Immunotherapy
ACS Medicinal Chemistry Letters·2021· 12 citedOpen Access
TGFβ2 and TGFβ3 mediate appropriate context-dependent phenotype of rat valvular interstitial cells
iScience·2021· 6 citedOpen Access
Discovery and Preclinical Evaluation of BMS-986242, a Potent, Selective Inhibitor of Indoleamine-2,3-dioxygenase 1
ACS Medicinal Chemistry Letters·2021· 26 citedOpen Access
An innovative kinome platform to accelerate small-molecule inhibitor discovery and optimization from hits to leads
Drug Discovery Today·2021· 7 cited
Pharmacodynamics‐based approach for efficacious human dose projection of BMS‐986260, a small molecule transforming growth factor beta receptor 1 inhibitor
Biopharmaceutics & Drug Disposition·2020· 3 cited
Design, Synthesis, and Structure–Activity Relationships of Novel Tetrahydroisoquinolino Benzodiazepine Dimer Antitumor Agents and Their Application in Antibody–Drug Conjugates
Journal of Medicinal Chemistry·2020· 15 cited
Development of a Scalable Synthesis of the Small Molecule TGFβR1 Inhibitor <b>BMS-986260</b>
Organic Process Research & Development·2020· 4 cited
Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGFβR1 Inhibitor as an Immuno-oncology Agent
ACS Medicinal Chemistry Letters·2020· 27 citedOpen Access
Discovery of 4-Azaindole Inhibitors of TGFβRI as Immuno-oncology Agents
ACS Medicinal Chemistry Letters·2018· 28 citedOpen Access
Immune-modulating enzyme indoleamine 2,3-dioxygenase is effectively inhibited by targeting its apo-form
Proceedings of the National Academy of Sciences·2018· 203 citedOpen Access
Heterobicyclic inhibitors of transforming growth factor beta receptor I (TGFβRI)
Bioorganic & Medicinal Chemistry·2018· 35 citedOpen Access
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Frequent Co-authors

Louis J. Lombardo(18), Joseph Fargnoli(18), John T. Hunt(14), Barri Wautlet(13), Gregory D. Vite(12), Amrita V. Kamath(10), John S. Tokarski(10), Zhen‐Wei Cai(10), Donna Wei(10), Rajeev S. Bhide(9), Punit Marathe(7), Robert J. Schmidt(7), Robert Jeyaseelan(7), Jonathan Lippy(7), Xiaoping Zheng(7), Craig R. Fairchild(6), Gretchen M. Schroeder(6), David Williams(6), Ligang Qian(6), Liping Zhang(6)