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Table 1 HIF-1-related drugs applied in cancer therapy

From: Systematic and comprehensive insights into HIF-1 stabilization under normoxic conditions: implications for cellular adaptation and therapeutic strategies in cancer

HIF1’s regulatory mechanism

More detailed mechanism

Agents

Current study phase

Clinical trial identifier

Refs.

Transcriptional level

NS

Alvocidib (Flavopiridol)

II

NCT00445341

[244, 290]

Translational level

Antisense oligonucleotide

EZN-2968

I

NCT01120288

NCT02564614

[252, 291, 292]

  

RX-0047

None

NS

[293]

 

Blocking mTOR/p70S6K/4E-BP1 pathway

Silibinin

II

NCT00487721

NCT01129570

NCT06187220

[249, 294, 295]

  

KC7F2

None

NS

[296]

 

PI3K inhibitors

Buparlisib

III

NCT04338399

[297, 298]

 

Blocking mTOR

Rapamycin

Approved

NCT03500367

[299]

  

Everolimus

Approved

NCT02842749

[300]

  

Temsirolimus/CCI-779

Approved

NCT03500367

[301]

 

ATR inhibition

AZD6738

II

NCT05514132

[302,303,304]

  

VX-970 (M6620)

II

NCT03718091

[305, 306]

 

Microtubule depolymerization

2ME2 and ENMD-1198

II

NCT00592579

NCT00444314

 

Inhibiting HIF-1α mRNA translation

2-Phenethyl isothiocyanate

II

NCT00691132

[307]

 

Inhibiting Na+/K+ ATPase

Digoxin

I/II

NCT06030622

[308, 309]

PHDs

Possibly zinc deprivation

Metallothioneins (MTs)

None

NS

[253]

 

Promoting the interaction between HIF1 and PHD

GYY4137

None

NS

[254, 310]

Ubiquitination

Related to proteasome

Cetuximab

Approved

NCT00044863

NCT00392769

[255]

 

Inducing pVHL expression

LW6

None

NS

[311]

 

Increasing HIF-1a and pVHL interaction

Wondonin

None

NS

[312]

Trans-activation

Hsp90 inhibition

Lonafarnib

III

NCT00773474

NCT00050336

[257]

  

GA (geldanamycin) and analogs/tanespimycin

II

NCT00093405

NCT00087386

[258, 313]

  

Ganetespib

III

NCT01562015

NCT01039519

[314, 315]

  

Apigenin

II

NCT00609310

[316]

  

Radicicol and its derivatives

None

NS

[317, 318]

 

HDAC inhibition

SAHA and FK228 (vorinostat and romidepsin)

Approved

NCT00801151

[261, 318]

  

Trichostatin A (TSA)

I

NCT03838926

[319]

  

LAQ824

None

NS

[320]

 

Inhibiting FIH-1 or the p300 recruitment

Bortezomib

Approved

NCT00512798

[262]

  

Amphotericin B

None

NCT01615809

[263]

  

Chetomin

None

NS

[321]

 

Disturbing HIF1-HRE binding

Anthracycline

Approved

NCT04182568

[264]

  

Polyamides

None

NS

[322]

  

Echinomycin (NSC-13502)

None

NS

[323, 324]

 

Inhibiting the recruitment of RNA polymerase II

Metformin

None

NCT05921942

NCT03684707

[265, 266]

 

Disturb the dimerization of HIF-1α and HIF-1β

Anti-HIF-1a VHH and hetero-bivalent VHH nanobodies (AG1-5)

None

NS

[267]

  

Acriflavine

None

NS

[268, 325]

Multitarget medicines

Inhibiting transcriptional initiation of the HIF-1α gene

Suppressing transactivation activity of HIF-1α protein

Disturbing the dimerization of HIF-1α and HIF-1β

Aminoflavone (AF)

II

NCT01015521

[326, 327]

 

HIF-1α translation

HIF-1α protein accumulation

HIF-1 transcriptional activity

Camptothecin analogs (TPT, EZN-2208)

II

NCT01601184

NCT01036113

[328,329,330]

 

Increasing pVHL activity

Activating PHDs’ activity

Impairing HIF-1 protein translation

Melatonin, NB-5-MT

None

NCT04137627

NCT04530097

[331,332,333]