ライフサイエンスコーパス: auristatin

1 assays, when the ADC (Trastuzumab-mcVC-PABC-Auristatin-0101) was incubated with plasma over a 144-h

2 in a majority of metastatic cancers, a CXCR4-auristatin ADC may be useful for the treatment of a vari

3 Dual-auristatin ADCs imparted activity in cell line and xenog

4 properties when compared to other synthetic auristatin analogues that are used in the preparation of

5 The design and synthesis of several new auristatin analogues with N-terminal modifications that

6 Conjugates of these multivalent ligands with auristatin and saporin toxins are efficiently internaliz

7 While two classes of potent anti-tubulins, auristatins and maytansinoids, indiscriminately radiosen

8 nes light onto the preferred binding mode of auristatins and serves as a valuable tool for structure-

9 tes of potent tubulin poisons (maytansinoids auristatins and taxoids) are undergoing clinical evaluat

10 A chemically defined anti-CXCR4-auristatin antibody-drug conjugate (ADC) was synthesized

11 kers and payloads other than maytansines and auristatins, are more complex than those examined previo

12 In addition, auristatin cocrystal structures with tubulin are being p

13 fractory to ADCs comprised of the individual auristatin components.

14 and hydroxylamine functionalized monomethyl auristatin D with either protease-cleavable or noncleava

15 selectively and efficiently conjugated to an auristatin derivative through a stable oxime linkage.

16 We exemplify this using hydrophilic auristatin drug linkers and PEGylated ADCs that yield un

17 reparation of ADCs containing two classes of auristatin drug-linkers that have differing physiochemic

18 f the potent synthetic dolastatin 10 analogs auristatin E (AE) and monomethylauristatin E (MMAE), lin

19 DCs, the potent microtubule-disrupting agent auristatin E (AE) was incorporated through the norephedr

20 e microtubule destabilizing agent monomethyl auristatin E (MMAE) conjugated to the humanized anti-CD1

21 linked to the antimitotic agents monomethyl auristatin E (MMAE) or F (MMAF), produces potent and hig

22 jugated with the cytotoxic agents monomethyl auristatin E (MMAE) or monomethyl auristatin F (MMAF).

23 s with VC(S) linkers armed with a monomethyl auristatin E (MMAE) payload.

24 article-drug conjugates (NDCs) of monomethyl auristatin E (MMAE) significantly increase loading on a

25 ting to cAC10 the cytotoxic agent monomethyl auristatin E (MMAE) to create the antibody-drug conjugat

26 ed therapy, the antitubulin agent monomethyl auristatin E (MMAE) was attached to a CD30-specific mono

27 sized that the anti-tubulin agent monomethyl auristatin E (MMAE), a component of a clinically approve

28 cally conjugated duocarmycin- and monomethyl auristatin E (MMAE)-based anti-PSMA ADCs with drug-to-an

29 promising target for antimitotic monomethyl auristatin E (MMAE)-based antibody-drug conjugate (ADC)

30 F (mcMMAF) and valine-citrulline-monomethyl Auristatin E (vcMMAE) at interchain cysteine residues.

31 sosomal release functionality and monomethyl auristatin E as a cytotoxic payload.

32 lectin antibody valine-citrulline monomethyl-auristatin E in vivo, with more than 85% inhibition of t

33 of the ADC conjugated with either monomethyl auristatin E or F (vcMMAE/mcMMAF) displayed the same HDX

34 When conjugated to monomethyl auristatin E, an antibody against the ovarian cancer ant

35 e (ADC) that selectively delivers monomethyl auristatin E, an antimicrotubule agent, into CD30-expres

36 vered the same cytotoxic payload (monomethyl auristatin E, MMAE), and we found that the intracellular

37 al antibody (cAC10) conjugated to monomethyl auristatin E, targets CD30(+) receptors.

38 lectin antibody valine-citrulline monomethyl-auristatin E, was a potent and selective agent against E

39 derivative of the cytotoxic tubulin modifier auristatin E, was covalently coupled to cAC10 through a

40 However, a novel auristatin E-based antibody drug conjugate (ADC), E-sele

41 Brentuximab vedotin is a monomethyl auristatin E-conjugated monoclonal antibody directed aga

42 onjugated to the potent cytotoxin monomethyl auristatin E.

43 the microtubule-disrupting agent monomethyl auristatin E.

44 jugated via a cleavable linker to monomethyl auristatin E.

45 B (gpNMB) to the potent cytotoxin monomethyl auristatin E.

46 o a microtubule-disrupting agent, monomethyl auristatin E.

47 found to correlate with sensitivity to free auristatin E.

48 nticancer drug N-phenyl maleimide monomethyl-auristatin-E (MMAE) maintained high cytotoxicity followi

49 tic agents such as paclitaxel and monomethyl-auristatin-E (MMAE).

50 led Lx, was coordinated to Desferal (DFO) or auristatin F (AF) to provide storable "semifinal" produc

51 conjugated with maleimidocaproyl-monomethyl Auristatin F (mcMMAF) and valine-citrulline-monomethyl A

52 monomethyl auristatin E (MMAE) or monomethyl auristatin F (MMAF).

53 arrying the structurally distinct monomethyl auristatin F were unaffected by SLC46A3 attenuation.

54 of the microtubule-disrupting cytotoxic drug auristatin (FGFR2-ADC).

55 novel derivatives of the anti-tubulin agent auristatin, mediated potent antigen-dependent cytotoxici

56 the dominant mechanism of action in vivo was auristatin-mediated tumor cell killing.

57 An ADC conjugated via hinge-cysteines to an auristatin payload was used as a model in this study to

58 scribed, including the discovery of our lead auristatin, PF-06380101.

59 alanine phenylenediamine (AFP) or monomethyl auristatin phenylalanine (MMAF), two novel derivatives o

60 antibody-drug conjugates (ADC) consisting of auristatin phenylalanine phenylenediamine (AFP) or monom

61 Auristatins, synthetic analogues of the antineoplastic n

62 immunoglobulin G (IgG) and conjugated to an auristatin through a stable, non-cleavable oxime linkage

63 the majority of the deconjugated mc-VC-PABC-auristatin ultimately is transferred to serum albumin, f