Valo SPAC Presentation Deck
Valo is seeking to develop compounds that allow us to drug previously
undruggable targets
OPL-0012: USP7
THERAPEUTIC HYPOTHESIS
A specific, selective targeted
inhibitor designed to unlock p53
biology for treating various
cancers³
OPL-0015: USP28
THERAPEUTIC HYPOTHESIS
A specific, selective targeted
inhibitor designed to unlock
c-Myc biology for treating
various cancers³
USP7 is a clinically validated oncogene implicated
in the p53 pathway¹
Ub Deubiquitination
Ub
Ub
Ub
Ub
USP28
p53
P53 degradation
Skp1
FBW7
USP7
Transcriptional
activation
Ubiquitination
Cul1 Ub
E2
DNA damage
Substrate
C-MYC
LSD1
HIF-1a
Ub
Up
Ub
USP28 has been demonstrated to be required for
c-Myc stability and clinically implicated in cancers²
Proteasome
Deubiquitination
ATM
ATR
PIRH2
MDM2
Claspin
[1] Wang, Zhiru, et al. "USP7: Novel Drug Target in Cancer Therapy." Frontiers in Pharmacology. V-10, 427, (Apr 2019)
Valo [2] Wang, Xiaofang, et al. "Targeting Deubiquitinase USP28 for Cancer Therapy." Cell Death Dis, V-9, 186 (2018)
[3] Reflects management's current expectations
ULUb
Ub
Ub
CHK2
Ub
MDM2 degradation
CHK1
Ub
Ub
Self-ubiquitination
↑
Ub
Ub
Ub
p53
In vivo: Complete responses to established
tumors in mouse models
Tumor Volume (mm³)
Tumor volume (mm³)
1800
1500-
1200-
900-
600-
300-
2000
0
1600
0
1200
800
400
0
4
Dose
Strong anti-tumor signals demonstrated by lung
squamous cell carcinoma (LSCC) model in mice
Established tumor model:
LSCC (NCI-H520) Human Cells
12 416
Dose
→ Vehicle
→OPAL-0015
1
Dose
Days post treatment initiation (Day)
I
20 424
Dose
Control
Drug
2
3
Time of Treatment (d)
28
4
2Q21
P<0.0001
30View entire presentation