Drug Discovery Department Metrics

• New Reagents for C-C and C-N Bond Formation
  Award Number:
  Sponsor: Nat Institutes of Health
  PI:Lopchuk, J.
• Developing CDK12 inhibitors to overcome therapy resistance in HER2+ and KRAS driven breast and lung cancers
  Award Number:
  Sponsor: Nat Institutes of Health
  PI (Contact):Duckett, D.,PI (MPI):Monastyrskyi, A.,PI (MPI):Haura, E.
• Developing CDK12 inhibitors to overcome therapy resistance in HER2+ and KRAS driven breast and lung cancers supplement
  Award Number:
  Sponsor: Nat Institutes of Health
  PI (Contact):Duckett, D.,PI:Monastyrskyi, A.
• Diazirines and diaziridines as nitrogen transfer reagents
  Award Number:
  Sponsor: Nat Science Foundation
  PI:Lopchuk, J.
• Selective Targeting of TAF1 Function in Acute Myeloid Leukemia
  Award Number:
  Sponsor: Nat Institutes of Health
  PI (Contact):Schonbrunn, E.,PI (MPI):Chen, J.,PI (MPI):Lopchuk, J.
• Development of bifunctional CDK2 inhibitors for treatment of CCNE1-driven cancers
  Award Number:
  Sponsor: Nat Institutes of Health
  PI (Contact):Schonbrunn, E.,PI (MPI):Lopchuk, J.
• Dual Up- and Downstream Targeting of POU2F3 in Small Cell Lung Cancer
  Award Number:
  Sponsor: US Army
  PI:Rix, U.,CO-PI:Flores, E.
• Novel combination approaches for targeting oncogenic signaling dependencies in POU2F3- driven small cell lung cancer
  Award Number:
  Sponsor: Florida Biomedical Research Program (FBRP)
  PI (Contact):Rix, U.,PI:Flores, E.
• Developing ULK3 inhibitors for the treatment of Multiple Myeloma
  Award Number:
  Sponsor: Florida Biomedical Research Program (FBRP)
  PI:Lawrence, N.,CO-PI:Lynch, C.,CO-PI:Shain, K.
• Development of EWS/FLI targeted therapies for Ewing sarcoma
  Award Number:
  Sponsor: Florida Biomedical Research Program (FBRP)
  PI:Monastyrskyi, A.
• Characterization of Plant-Based Phenolic Alkanones as Next-Generation Sun Protectants for Skin Cancer Prevention
  Award Number:
  Sponsor: US Army
  PI:Lawrence, N.

CLINICAL TRIAL 23556
A Phase 1 Study of MLN7243 (TAK-243) for Either Relapsed/Refractory Acute Myeloid Leukemia or Myelodysplastic Syndrome/Chronic Myelomonocytic Leukemia Refractory to Hypomethylating Agents
Condition: Malignant Hematology
Intervention:

CLINICAL TRIAL 23599
Phase 1a/1b Open-Label Study Evaluating the Safety, Tolerability, Pharmacokinetics, and Efficacy of BBO-11818 in Subjects with Advanced KRAS Mutant Cancers
Condition: Multiple
Intervention: Alimta (Pemetrexed); BBO-11818 (); Cetuximab (); Erbitux (Cetuximab); Paraplatin (carboplatin); Pembrolizumab (Keytruda); Pemetrexed (); carboplatin (); cisplatin ()

CLINICAL TRIAL 23697
A Phase 1/1b, Open-label, Multicenter, First-in-human Dose Escalation and Dose Expansion Study to Evaluate the Safety, Tolerability, Pharmacokinetics, Pharmacodynamics, and Anti-tumor Activity of VVD-159642, a RAS-PI3KA Inhibitor, as a Single Agent and in Combination in Participants With Advanced Solid Tumors
Condition: Multiple
Intervention: AMG 510 (Sotorasib); GSK1120212 (Trametinib); Olomorasib (); Sotorasib (); Trametinib (); VVD-159642 ()

• Chen L, Shultz ZP, Sansone M, Fang B, Liu X, Teng M, Schonbrunn E, Lopchuk JM, Chen J. PROTAC-Mediated Degradation of TAF1 Induces Apoptosis in AML Cells and Inhibits Tumor Growth In Vivo. Mol Cancer Ther. 2025 Nov.24(11):1712-1721. Pubmedid: 40376796. Pmcid: PMC12353786.
• Son J, Remsing Rix LL, Fang B, Welsh EA, Bremer NV, Foglizzo V, Roa P, Sigcha-Coello N, Liao Y, Haura EB, Drilon A, Koomen JM, Cocco E, Rix U. Dual targeting of RET and SRC synergizes in RET fusion-positive cancer cells. Mol Oncol. 2025 Nov. Pubmedid: 41194587.
• Stern YE, Ghosh P, Peroza J, Solanki HS, Imbody D, Bridenstine L, Pandurangan T, Frydman SM, Nickens KN, Walker-Mimms HL, Suvarna K, Chaudhary N, Monastyrskyi A, Duckett D, Haura EB. Targeting CDK12/13 Drives Mitotic Arrest to Overcome Resistance to KRASG12C Inhibitors. Cancer Res. 2025 Oct. Pubmedid: 41165466. Pmcid: PMC12638015.
• Solanki HS, Shah H, Imbody D, Desai B, Kato R, Miroshnychenko D, Stern YE, Majumder A, Sarcar B, Xieraili A, Stewart PA, Fang B, Zhang Y, Yao J, Darville LN, Koomen JM, Rix U, Evans JW, Yang YC, Ahler E, Marusyk A, Singh M, Aronchik I, Haura EB. RAS-GTP Inhibition Overcomes Acquired Resistance to KRASG12C Inhibitors Mediated by Oncogenic and Wildtype RAS Activation in Non-Small Cell Lung Cancer. Cancer Res. 2025 Oct. Pubmedid: 41165456.
• Yadav VK, Srivastava J, Venkatachalam A, Tantak MP, Lawrence NJ, Fisher DE, Lawrence HR, Premi S. Melanin-Driven Delayed CPD Formation Is Independent of Melanin Biosynthesis Pathway. J Invest Dermatol. 2025 Sep. Pubmedid: 40992685. Pmcid: PMC12507450.
• Tauro M, Li T, Sudalagunta PR, Meads M, Canevarolo RR, Nerlakanti N, Alugubelli RR, Lawrence HR, Gunawan S, Ayaz M, Nareddy P, Yun SY, Shay G, Yang K, Tran TH, Bishop RT, Nasr MM, Lawrence NNJ, Schönbrunn E, Cleveland JL, Silva AS, Shain KH, Lynch CC. Unc-51 Like Kinase 3 (ULK3) is essential for autophagy and cell survival in multiple myeloma. Res Sq. 2025 Aug. Pubmedid: 40831505. Pmcid: PMC12363935.
• Jiang J, Liang T, Solberg J, Chan A, Kalra P, Shi R, Pomerantz WCK, Hawkinson JE, Schönbrunn E, Georg GI. Macrocyclic dihydropyridine analogs as pan-BET BD2-preferred inhibitors. Eur J Med Chem. 2025 Jun.290:117504. Pubmedid: 40120495. Pmcid: PMC11993331.
• Junyent M, Noori H, De Schepper R, Frajdenberg S, Elsaigh RKAH, McDonald PH, Duckett D, Maudsley S. Unravelling Convergent Signaling Mechanisms Underlying the Aging-Disease Nexus Using Computational Language Analysis. Curr Issues Mol Biol. 2025 Mar.47(3). Pubmedid: 40136443. Pmcid: PMC11941692.
• McKenna SM, Borsari C, Chin Chan S, Donckele EJ, Faucher FF, Grenier-Davies MC, Haranahalli K, Matagne B, Monastyrskyi A, Petracca R. Highlights from the Lowlands: Early Career Researchers Shine at Medicinal Chemistry Frontiers 2024. Chemmedchem. 2025 Feb.20(4):e202400853. Pubmedid: 39571174.