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FIRST-IN-CLASS ANTI-CANCER DRUG : SMALL MOLECULE WITH NOVEL DUAL ACTION

program pipeline indication
Development Stage
drug
development lead
optimization Pre-clinical Phase 1 Phase 2
NOBLE
ANTICANCER
DRUG
OZ-001LC Lung
cancer PRE-CLINICAL
OZ-001PC Pancreatic
cancer PRE-CLINICAL
OZ-001BC TNBC LEAD OPTIMIZATION
· SECURE PATENT OF OZ-001

FIRST-IN-CLASS ANTI-CANCER DRUG : SMALL MOLECULE FOR NOVEL TARGET

program pipeline indication
Development Stage
drug
development lead
optimization Pre-clinical Phase 1 Phase 2
NOBLE
ANTICANCER
DRUG
OZ-002RS Orphan Disease
(Myosarcoma) LEAD OPTIMIZATION
OZ-002** Additional
Cancer DRUG DEVELOPMENT
· SECURE PATENT OF OZ-002
· ** UNDER DEVELOPMENT FOR ADDITIONAL INDICATION

FIRST-IN-CLASS DRUG : NOVEL CMPD DEGRADER (Chaperone-Medicated Protein Degradation)

program pipeline indication
Development Stage
DRUG
DEVELOPMENT LEAD
OPTIMIZATION Pre-clinical Phase 1 Phase 2
TARGET
PROTEIN
DEGRADATION
OZ-003LC Resistant
NSCLC LEAD OPTIMIZATION
OZ-003* Undisclosed DRUG DEVELOPMENT
OZ-003** Undisclosed DRUG DEVELOPMENT
OZ-003*** Undisclosed DRUG DEVELOPMENT
OZ - 001 OZ - 002 OZ - 003 0Z - 004

OZ-001 MODE OF ACTION
: NOVEL DUAL ACTION (METABOLIC & TARGETED ANTICANCER DRUG)

OZ-001 is small molecule compound which has novel dual action blocking T-type Ca2+ channel and inhibiting STAT3 activation. We confirm that OZ-001 bind excellent to T-type Ca2+ channel . OZ-001 induce cell cycle arrest, inhibitor of cell growth and apoptosis. We confirm that OZ-001 induce cellular signaling pathway related to STAT3.
To characterize the type of STAT3 inhibition by OZ-001, a blind docking study was performed with the whole crystal structure of STAT3 to determine potential binding sites.
The results of the docking study showed OZ-001 could fit exclusively within the SH2 domain.

  • NOVEL DUAL ACTION SMALL MOLECULE (METABOLIC & TARGETED ANTICANCER DRUG)
  • SELECTIVITY (POTENT T-TYPE Ca2+ CHANNEL SELECTIVITY), HIGH POTENCY, SAFETY
  • PATENTED PRODUCT

BLOCKING OF T-TYPE Ca2+ CHANNEL
: INHIBITION OF METABOLIC PROCESS OF CANCER BY CELL CYCLE ARREST

<3D structure : T-type Ca2+ channel>

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3D structure : T-type Ca2+ channel

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<Scheme of T-type Ca2+ channel blocker action>

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Scheme of T-type Ca2+ channel blocker action

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<OZ-001 binding site in T-type Ca2+ channel>

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OZ-001 binding site in T-type Ca2+ channel

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<OZ-001 induced G1 cell cycle arrest via CaMK II inactivation> * calcium-calmodulin dependent protein kinase 2 (CaMK II)

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OZ-001 induced G1 cell cycle arrest via CaMK II inactivation * calcium-calmodulin dependent protein kinase 2 (CaMK II)

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Backgroud of T-type Ca2+ channel Blocker develpoment

Intracellular Ca2+ regulates numerous crucial cellular processes, including cell cycle, proliferation, transcription, exocytosis, hormone release, cell motility, and cell death. A Ca2+ channel is an ion channel which shows selective permeability to calcium ions. Among Ca2+ channel, T-type Ca2+ channels are often overexpressed in different human cancers and participate in the regulation of cell cycle progression, proliferation, migration, and survival. Based on these observations, it has been suggested that T-type Ca2+ channels may play an important role in cancer growth and progression and, therefore, may be a poten tially attractive target for cancer therapy.

Targeting STAT3 Protein
: Inhibition STAT3 (Oncoprotein) Phosphorylation Pathway

<Interaction of OZ-001 with the SH2 domain of STAT3>

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Interaction of OZ-001 with the SH2 domain of STAT3

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<OZ-001 induced apoptosis is associated with the inhibition of STAT3 activation>

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OZ-001 induced apoptosis is associated with the inhibition of STAT3 activation

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IN PROGRESS

  • We confirmed that OZ-001 anti-cancer drug effect in lung cancer cell lines and lung cancer xenograft model.
    The results are published
  • Ongoing, we are studying anti-cancer drug effect of OZ-001 in pancreatic cancer and TNBC.
  • We confirmed that OZ-001 shows anti-cancer effect in T-type Ca2+ channel overexpressed cancer cell line.
    (Lung cancer, Pancreatic cancer, Breast cancer cell line etc.)
  • Also, we anticipate that OZ-001 is novel compounds which has anti-cancer drug effect with dual action.

REFERENCE

  • Pflugers Arch - Eur J Physiol (2014) 466:801–810

New Target for Cancer Therapy : Calponin 3 Protein

The Calponin Family of actin-binding proteins consists of three isoforms:
①Calponin- 1 (CNN1; h1 or basic CNN); ②CNN2 (h2 or neutral CNN); and ③CNN3 (h3 or acidic CNN).
All of them are generally involved in various forms of cell motility.

- Calponin 3 (CNN3)

  • Actin-binding Protein
  • Expressed in Smooth muscle and Non-smooth muscle cells
  • High level expression in Smooth muscle, Placental Trophoblast, Myoblast
  • Required for Cytoskeletal Rearrangement & Wound Healing
  • Paly a role in Cell Differentiation, Proliferation and Migration via stress fibre formation or cytoskeletal remodeling
  • In recent studies of CNN3 for Caner
    Differentially Expressed in Colorectal, Breast, Cervical, Gastric, Ovarian cancer, MALT lymphoma and etc.
    Showed association with EMT Features, increased Cancer cell Invasion and Resistance to chemotherapeutic agents
    High expression is associated with Tumor Size, Tumor Stage and Lymph node and Distant metastases.

IN PROGRESS

  • We confirmed based on our own study that CNN3 is expressed in various cancer cell line and it is overexpressed especially in rhabdomyosarcoma.
  • We confirmed anti-cancer drug effect of OZ-002 in orphan cancer cell line related myosarcoma.
  • Ongoing, rapidly we are identifying correlation with overexpression of CNN3 in various cell line related myosarcoma to develop first-in-class drug targeting CNN3 as biomarker.
  • Ongoing, we are under studying for other various cancer which has differentially expression of CNN3.

REFERENCE

  • World J Gastrointest Oncol 2019 November 15; 11(11): 971-982
  • AGING 2020, Vol. 12, No. 14
  • Hindawi Gastroenterology Research and Practice Volume 2019, Article ID 3024970, 7 pages
  • Scientific RepoRtS 2020, 10:2427

1st TARGET OF OZ-003

IN PROGRESS

  • We conducted structure based drug design for OZ-003LC and validated them by Artificial Intelligence Technique.
  • We performed study of synthesis with chemistry expert for OZ-003LC which is optimized via AI Technique and we are studying anti-cancer drug effect of OZ-003LC in non-small cell lung cancer (MET exon 14 skipping mutation).

NEXT TARGET OF OZ-003

IN PROGRESS

  • Ongoing, we are discovering lead compounds for new target protein and advancing optimized compounds for a variety disease such as cancer, degenerative brain disorder, orphan disease, etc.
    Next Target Protein in On-going project : ALK, WEE1, Akt, etc.
  • We are advancing a broad pipeline of OZ Degrader diversified by chemical composition and clinical indication and will build up expansive pipeline including difficult-to-treat disease, rare cancer, etc.