Drug Discovery Department Metrics

• 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.
• 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 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-10203 (); BBO-11818 (); Cetuximab (); Erbitux (Cetuximab); FOLFOX (); Gemzar (gemcitabine); NALIRIFOX (); Nab-paclitaxel (Abraxane); Paraplatin (carboplatin); Pembrolizumab (Keytruda); Pemetrexed (); carboplatin (); cisplatin (); gemcitabine (); mFOLFIRINOX (); mFOLFOX6 ()

CLINICAL TRIAL 23650
A Phase 1/2, Open-label, Dose Escalation and Expansion Study to Evaluate the Safety and Tolerability of LBS-007 in Patients with Relapsed or Resistant Acute Leukaemias
Condition: Malignant Hematology
Intervention: Azacitidine (5-azacitidine); GDC-0199 (Venetoclax); LBS-007 (); Venetoclax ()

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 ()

CLINICAL TRIAL 23731
A Phase 2a Multicenter Dose Escalation and Dose Optimization Study of SYNC-T Therapy SV-102 for Patients with Metastatic Castration-Resistant Prostate Cancer (mCRPC) (LEGION-100-2a)
Condition: Genitourinary
Intervention: SV-102 ()

CLINICAL TRIAL 24058
Evaluation of Artificial Sweetener Use Among Patients with Endometrial Cancer
Condition: Gynecological Tumor
Intervention:

CLINICAL TRIAL 24095
Phase 1/2a Open-Label Clinical Trial Evaluating VBC101, an EGFR and cMET Targeted Bi-Specific Antibody Drug Conjugate, in Participants With Advanced Solid Tumor Malignancies
Condition: Multiple
Intervention: VBC101 ()

CLINICAL TRIAL 24394
A Multi-center, Open-label, Phase I Study Evaluating the Safety, Tolerability, Pharmacokinetics and Antitumor Activity of AN9025 in Participants with Advanced or Metastatic Solid Tumors Harboring RAS Mutations
Condition: Multiple
Intervention: AN9025 ()

• Deng O, Nepomuceno TDC, Fang B, Welsh EA, Izumi V, Martin RH, George EM, Koomen JM, Monteiro AN, Rix U. Integrative proteomics reveals MSH6 to modulate PARP inhibitor sensitivity in BRCA1/2-proficient ovarian cancer. PLoS One. 2026 Sep.21(9):e0357365. Pubmedid: 42685115. Pmcid: PMC13537606.
• Tauro M, Li T, Sudalagunta PR, Meads M, Canevarolo RR, Nerlakanti N, Alugubelli RR, Lawrence HR, Tantak MP, Gunawan S, Ayaz M, Nareddy P, Yun SY, Shay G, Yang Y, Tran TH, Atkins R, Locke FL, Bishop RT, Nasr MM, Lawrence NJ, Schönbrunn E, Cleveland JL, Silva AS, Shain KH, Lynch CC. Unc-51 like kinase 3 (ULK3) contributes to autophagy and cell survival in multiple myeloma. Nat Commun. 2026 Aug.17(1). Pubmedid: 42778564.
• Shultz ZP, Lee-Sam A, Chang YP, Sun L, Grassie D, Gabellini A, Pedretty K, Scattolin T, Izumi V, Fang B, Sansil S, Kakumanu R, Wojtas L, Koomen J, Schönbrunn E, Monastyrskyi A, Duckett D, Lopchuk JM. Late-stage functionalization with strain-release warheads enables tunable covalent inhibition. Science. 2026 Jul.393(6809):408-416. Pubmedid: 42490492.
• Galaktionova DV, Maharaj V, Lopchuk JM. Unactivated Photoredox C-H Amination with Diazirines: Access to Acyldiaziridines. Org Lett. 2026 Jun.28(23):7315-7320. Pubmedid: 42234791. Pmcid: PMC13352326.
• Liao Y, Li X, Liu M, Fernandes VC, Duckett D, Haura EB, Monastyrskyi A, Rix U. Targeting GSTZ1 Sensitizes KRASG12C-Mutant Lung Cancer Cells by Overcoming Glutathione and Glycolysis Pathway Rewiring. Cancer Res Commun. 2026 Jun.6(6):1376-1387. Pubmedid: 42240478. Pmcid: PMC13254912.
• Jno Baptiste C, Shultz ZP, Lopchuk JM. Mild Transsulfinamidation Enables Rapid Access to Sulfinamides, Sulfonamides, and Sulfonimidamides. Org Lett. 2026 Jun.28(24):7655-7660. Pubmedid: 42247525. Pmcid: PMC13347854.
• Tagal V, Li T, Kumar R, Shrestha P, Yu X, Miroshnychenko D, Olumoyin K, Marusyk A, Davies M, Maudsley S, El-Naqa I, Gomes AP, Duckett DR, Han HS, Andor N. Ploidy shapes gemcitabine response through altered potency and delayed cell death. bioRxiv. 2026 Jun. Pubmedid: 42282758. Pmcid: PMC13251900.
• Liang T, Guan X, Chan A, Kalra P, Shi R, Solberg J, Sigua LH, Qi J, Pomerantz WCK, Schönbrunn E, Hawkinson JE, Georg GI. Structural Basis for BD1-Preferring 2,4-Disubstituted Pyrimidine BRDT Inhibitors. J Med Chem. 2026 May.69(9):11088-11108. Pubmedid: 41984625. Pmcid: PMC13181795.
• Grygorenko OO, Monastyrskyi A. Drug Discovery in Poland and Ukraine. J Med Chem. 2026 May.69(9):9773-9775. Pubmedid: 42023728.
• 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. 2026 Apr.146(4):1089-1101.e3. Pubmedid: 40992685. Pmcid: PMC12507450.
• 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. 2026 Apr.20(4):1041-1060. Pubmedid: 41194587. Pmcid: PMC13060644.
• Pandurangan T, Zeleke ST, Iermolaieva A, Ghosh P, Mosior J, Sun L, Grassie D, Schmitz M, Kalaga MN, Albritton W, Rodas MM, Chin Chan S, Frydman S, Sansil S, Geyer M, Schönbrunn E, Roush WR, Duckett DR, Monastyrskyi A. Structure-Activity and Structure-Degradation Relationship Studies of 2-Amino-6-(benzimidazol-2-ylmethyl)-N9-heteroarylpurines as Potent and Selective CDK12/13 Inhibitors and Cyclin K Degraders. J Med Chem. 2026 Feb.69(3):2287-2309. Pubmedid: 41533987.
• Hamaidi I, Cheng P, Jun SY, Manna A, Wang MH, Nguyen A, Can I, Zhang MG, Taylor OO, Bailon LUL, Fang B, Perez B, Creelan BC, Marusyk A, Shin D, Hwang TH, Berglund AE, Shapiro VS, Ji HM, Conejo-Garcia JR, Kim S. SIRT2-mediated deacetylation of LCK governs the magnitude of T cell receptor signaling. Nat Immunol. 2026 Feb.27(2):213-224. Pubmedid: 41611868. Pmcid: PMC12864039.
• Craig CJ, Boeringer T, Pardo M, Del Pozo A, Maudsley S. GPCR-Mediated Cell Intelligence: A Potential Mechanism for Survival and Long-Term Health. Curr Issues Mol Biol. 2026 Jan.48(2). Pubmedid: 41751391. Pmcid: PMC12939297.
• 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. 2026 Jan.86(2):485-502. 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 Wild-Type RAS Activation in Non-Small Cell Lung Cancer. Cancer Res. 2026 Jan.86(2):467-484. Pubmedid: 41165456. Pmcid: PMC12962340.
• Maudsley S. Unraveling Oxidative Threads: Stress, Pathology, and Resilience in Biochemistry, Molecular, and Cellular Biology (2023-2025). Curr Issues Mol Biol. 2025 Dec.47(12). Pubmedid: 41614814. Pmcid: PMC12731963.
• Hu Q, Remsing Rix LL, Desai B, Miroshnychenko D, Li X, Welsh EA, Fang B, Wright GM, Chaudhary N, Kroeger JL, Doebele RC, Koomen JM, Haura EB, Marusyk A, Rix U. Cancer-associated fibroblasts confer ALK inhibitor resistance in EML4-ALK-driven lung cancer by concurrent integrin and MET signaling. Sci Signal. 2025 Dec.18(918):eads7662. Pubmedid: 41433419.
• 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.