Table 2 Chemical structures of representative small-molecule PCSK9 inhibitors, natural small molecules with PCSK9 inhibitory potential, and peptidomimetic PCSK9 inhibitors

From: Targeting proprotein convertase subtilisin/kexin type 9 (PCSK9): from bench to bedside

Inhibitor type

Name

Structure

Reference

Small-molecule PCSK9 inhibitor

3 f

412

7030B-C5

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61,409

BRD8518

410

Carboxylic acid 9

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411

CVI-LM001

382

DC371739

414

DFDIM

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408

PF-06446846

413

PF-06815345

382

Natural small molecules with PCSK9 inhibitory potential

5a,6a-epoxy-(22E,24 R)-ergosta-8(14),22-diene-3b,7b-diol

397

(2 R,3 R)-3,7,2’-trihydroxy-5-mathoxy-flavanone

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397

Adenosine

397

Berberine

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415

Curcumin

415

Dihydrocucurbitacin B

420

Erybraedin D

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419

Hanabiratakelide A

397

Manglisin E

397

Moracin C

397

Naringin

424

Neolignan

421

Norsesquiterpene

418

Pinostrobin

397,415

Polydatin

499

Pseurotin A

422

Quercelin-3-glucoside

397

Schisandrin C

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397

Schisandrol B

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397

Skullcapflavone II

397

Sparoside A

397

Tanshinone IIA

397

Vitamin C

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423

Peptidomimetic PCSK9 inhibitors

13PCSK9i

427

Cyclic-tetramer C12

428

LDLL-1dinr

426

MeIm

425

MK-0616

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382

tetra-P9-38

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429

  1. Amax absorption maximum, EC50 half-maximal effective concentration, IC50 half-maximal inhibitory concentration, KD dissociation constant, MW molecular weight