創薬プログラム

Activity	Outline	Objective
In-house program	We aim at optimization of inhibitors for IL-6, tumor angiogenesis, Notch1, IgE, and tubulin polymerization. We have identified IL-6 inhibitors that bind to IL-6 and modulate IL-6/IL-6R interaction, and hope to accelerate its optimization with a research partner.	Lead optimization with an alliance partner
Collaborative drug discovery researches of small molecules for new targets	We conduct drug discovery researches of small molecules for new targets proposed by Pharma or Interprotein in collaboration with Pharma. Now, we are seeking partners that conduct drug discovery researches for TIM-3, KIR, and NKG2A (immune checkpoints), Runx1 (leukemia-related transcription factor), and gp130 (key molecule in IL-6 signaling) in collaboration.	Conduct of drug discovery researches in collaboration with alliance partners
Collaborative drug discovery researches of HLHP for new targets	We conduct drug discovery researches of HLHP for new targets proposed by Pharma or Interprotein in collaboration with Pharma. Now, we are seeking partners that conduct drug discovery researches for TIM-3, KIR, NKG2A, and gp130 in collaboration. HLHP is also applicable to substitution for antibody in antibody-drug conjugate (ADC).	Conduct of drug discovery researches in collaboration with alliance partners

自社研究プロジェクト

Project	Domain	Stage	Note
Tumor angiogenesis inhibitor	Oncology (tumor angiogenesis)	Lead optimization	We have identified compounds that inhibit VEGF-induced proliferation of HUVEC and suppress tumor growth in xenograft models. MOA is now being verified.
IL-6 inhibitor	Autoimmune Inflammation Oncology	Lead generation	We have identified compounds that modulate IL-6/IL-6R interaction in a cell-free system (MOA has been almost fully verified).
IgE inhibitor	Allergy	Hit validation	We have identified compounds that inhibit IgE-induced degranulation of basophils. MOA has been partly verified.
Notch1 inhibitor	Oncology Hematology	Lead generation	We have identified compounds that inhibit Notch1-relevant transcription and suppress tumor growth in a xenograft model. MOA has been partly verified.
Tubulin polymerization inhibitor	Oncology Hematology	Lead generation	We have identified compounds that inhibit tubulin polymerization in a cell-free system and suppress tumor growth in xenograft models. MOA has been almost fully verified.

Project	Domain	Note
TIM-3 inhibitor	Oncology Immune Check Point	We have identified TIM-3 binding peptides and are investigating those effects on TIM-3 binding to HMGB1, galectin-9 and CEACAM1.
NKG2A/HLA-E/CD94 inhibitor	Oncology Immune Check Point	We have designed peptides that are expected to bind NKG2A and inhibit NKG2A binding to HLA-E/CD94.
KIR/HLA-C inhibitor	Oncology Immune Check Point	We have designed peptides that are expected to bind KIR and inhibit KIR binding to HLA-C.
gp130 inhibitor	Autoimmune Inflammation Oncology	We have selected hit candidates for small molecule gp130/IL-6 interaction (intra-trimer) modulator, and also designed peptide gp130/IL-6 binding (inter-trimer) inhibitor.
RUNX1/CBFβ inhibitor	Onco-hematology	We have identified the compounds that bind to RUNX1 and inhibit RUNX1/CBFβ binding to DNA with IC50 values of less than 1μM.